Search Result
Results for "
BBB
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
26
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-151657
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ADC Linker
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Others
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Spermine(N3BBB) is a click chemistry reagent containing an azide group and can be used for various biochemical studies . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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- HY-119624
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PIKfyve
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Cancer
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MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB) .
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- HY-137501
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Liposome
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Others
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306-O12B-3 is a lipidoid that can efficiently deliver ASO both in vitro and in vivo. 306-O12B-3 is used to transport small molecule drugs across the blood-brain barrier (BBB) .
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- HY-169782
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P-glycoprotein
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Neurological Disease
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CJZ3 is an reversible inhibitor for P-glycoprotein (P-gp), that accumulates the drug (Rh123) in cells, and improve the permeability of the blood-brain barrier (BBB) .
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- HY-146141
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Ephrin Receptor
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Cancer
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EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB .
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- HY-147982
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GABA Receptor
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Neurological Disease
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GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mouse brain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant .
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- HY-147821
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Cannabinoid Receptor
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Metabolic Disease
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CB1-IN-2 (Compound 4g) is a selective CB1 inhibitor with an IC50 of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant .
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- HY-162277
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Cholinesterase (ChE)
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Neurological Disease
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BuChE-IN-10 (compound 7p) is an inhibitor of BuChE (eqBuChE IC50 = 4.68 nM, huBuChE IC50 = 9.12 nM). BuChE-IN-10 has anti-neuroinflammatory activity and exhibits high BBB permeability .
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- HY-18406
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HSP
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Cancer
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HSP70-IN-4 (Compound YM-01) is an Hsp70 inhibitor with an IC50 of 3.2 μM. HSP70-IN-4 is not BBB permeable .
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- HY-155271
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Carbonic Anhydrase
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Others
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hCAXII-IN-7 (compound 6e) is a hCA XII inhibitor. hCAXII-IN-7 has BBB permeability. hCAXII-IN-7 induces 786-0, SF-539 and HS 578 T cells apoptotic .
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- HY-153434
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RIP kinase
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Cancer
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RIP1 kinase inhibitor 4 (Example 3) is a BBB-penetrable RIP1 kinase inhibitor (EC50: <100 nM). RIP1 kinase inhibitor 4 can be used for the research of cell programming necrosis-related diseases . RIP1 kinase inhibitor 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-126429
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Sodium Channel
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Neurological Disease
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Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant τ of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6 .
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- HY-146668
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity .
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- HY-149820
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor with an IC50 of 0.014 μM. MAO-B-IN-22 has high antioxidant activity, good metal chelating ability, proper BBB permeability and significant neuroprotective effect .
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- HY-150545
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro .
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- HY-136731
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DNA/RNA Synthesis
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Cancer
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APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells .
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- HY-164505
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Drug Intermediate
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Neurological Disease
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NRMA-9 is the amide produrg of the small molecule nuclear receptor modulator. NRMA-9 exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-9 can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .
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- HY-164401
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EAAT
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Cancer
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QBS10072S is a bifunctional chemotherapeutic agent, through combination of a cytotoxin and a selective LAT1 transporter substrate. QBS10072S exhibits cytotoxicity in MDA-MB-231 cell and antitumor efficacy in mice. QBS10072S is blood-brain barrier (BBB) penetrable .
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- HY-147870
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- HY-P1178A
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Trk Receptor
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Neurological Disease
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Cyclotraxin B TFA is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B TFA inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B TFA has analgesic and anxiolytic effects .
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- HY-A0168A
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CVT-3146 hydrate
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Adenosine Receptor
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Cardiovascular Disease
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Regadenoson hydrate (NSC 169186) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson hydrate also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
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- HY-P10502
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LDLR
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Others
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L57 exhibits high affinity to the low-density lipoprotein receptor-related protein 1 (LRP1) with Ki of 45 nM. L57 exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 can be utilized as the carrier for CNS drug delivery .
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- HY-105155
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RMP 7
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Bradykinin Receptor
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Cancer
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Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
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- HY-A0168
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CVT-3146
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Adenosine Receptor
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Cardiovascular Disease
Cancer
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Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
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- HY-134494
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GPR68
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Neurological Disease
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MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .
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- HY-D2343
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Biochemical Assay Reagents
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Neurological Disease
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PB0822 can be used for in vivo PET imaging when labeled with [ 18F]fluoride. [ 18F]PB0822 is a PET radioligand. [ 18F]PB0822 has a cLogP value of 1.54, which is a good predictive index for BBB penetration. [ 18F]PB0822 can be used for Alzheimer’s Disease research .
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- HY-P10235
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Amylin Receptor
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Neurological Disease
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Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
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- HY-162757
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GABA Receptor
Sodium Channel
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Neurological Disease
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Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable .
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- HY-146142
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Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB .
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- HY-151152
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD) .
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- HY-122462
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PNU-159548
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DNA/RNA Synthesis
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Cancer
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Ladirubicin (PNU-159548) is a derivative of Daunorubicin (HY-13062A). Ladirubicin exhibits DNA intercalation and DNA alkylating properties, inhibits DNA replication and transcription, causes DNA damage, and thereby exhibits antitumor efficacy. Ladirubicin exhibits the potential to penetrate the blood-brain barrier (BBB) for its high lipophilicity. Ladirubicin exhibits toxicity through suppression of bone marrow activity .
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- HY-109502S
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Isotope-Labeled Compounds
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Neurological Disease
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10-OH-NBP-d4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research[1].
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- HY-146665
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BChE-IN-5 (BMC-16) is a dual AChE and BChE inhibitor with IC50 values of 266 nM and 10.6 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-5 can cross the BBB .
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- HY-146664
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BChE-IN-4 (BMC-3) is a dual AChE and BChE inhibitor with IC50 values of 792 nM and 2.2 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-4 can cross the BBB .
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- HY-A0168R
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Adenosine Receptor
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Cardiovascular Disease
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Regadenoson (Standard) is the analytical standard of Regadenoson. This product is intended for research and analytical applications. Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
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- HY-128868G
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Fluorescent Dye
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Others
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FITC-Dextran (MW 150000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=491 nm; Em=518 nm). FITC-Dextran (MW 150000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 150000) can be used in perfusion studies in animals or in fluorescence microlymphography, to study processes that affect the permeability of the blood brain barrier (BBB) . FITC-Dextran (MW 150000) can be used as fluorescent probe to study cell permeability .
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- HY-101059
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GABA Receptor
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Neurological Disease
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FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .
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- HY-108327
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Potassium Channel
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Neurological Disease
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PF-05020182 is an orally active opener for Kv7 channel, that activates human Kv7.2/7.3, Kv7.4 and Kv7.3/7.5 with EC50 of 334, 625 and 588 nM, respectively. PF-05020182 exhibits anticonvulsant activity in rats corneal electric shock-induced tonic seizure (MES) models. PF-05020182 is blood-brain barrier (BBB) penetrable .
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- HY-13779A
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Monoamine Oxidase
Dopamine Transporter
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Neurological Disease
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J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J147 can pass the blood brain barrier (BBB). J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter. J147 plays an impotant role in Alzheimer’s disease (AD) .
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- HY-B1334
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Mitochondrial Metabolism
Apoptosis
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Cardiovascular Disease
Cancer
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Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina .
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- HY-B1334A
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Mitochondrial Metabolism
Apoptosis
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Cardiovascular Disease
Cancer
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Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina .
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- HY-149941
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Neurotensin Receptor
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Neurological Disease
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hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
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- HY-161846
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Tyrosinase
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Neurological Disease
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Tyrosinase-IN-31 (compound 2-06) is a central-targeting tyrosinase inhibitor (tyrosinase: monophenolase IC50=70.44 μM, diphenolase IC50=1.89 μM). Tyrosinase-IN-31 can inhibit the tyrosinase and melanogenesis. Tyrosinase-IN-31 can penetrate the BBB and enter the central nervous system (CNS). Tyrosinase-IN-31 shows neuroprotective effects and Parkinsonism behavior improving function .
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- HY-108625
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SHA 68
1 Publications Verification
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Neuropeptide S Receptor
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Neurological Disease
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SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
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- HY-147939
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Cholinesterase (ChE)
Amyloid-β
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Cancer
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AChE/BuChE-IN-3 is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC50s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease .
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- HY-144660
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability .
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- HY-151962
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JNK
Apoptosis
GSK-3
p38 MAPK
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Neurological Disease
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JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable .
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- HY-10096
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GSK-3
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Neurological Disease
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TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
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- HY-164284
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Sodium Channel
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Neurological Disease
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LK-2 is an antagonist for ASIC1a with a Kd of 1.9 μM. LK-2 reduces glutamate-induced ASIC1a current-enhancement with an IC50 of 6.6 μM. LK-2 exhibits neuroprotective efficacy in mouse ischemic stroke model, with improved motor and coordination skills. LK-2 is blood-brain barrier (BBB) penetrable .
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- HY-143245
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Monoamine Oxidase
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Neurological Disease
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Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
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- HY-143244
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Monoamine Oxidase
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Neurological Disease
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Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
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- HY-150639
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Raf
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Cancer
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Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
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- HY-146399
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Cholinesterase (ChE)
ROS Kinase
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Neurological Disease
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AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB .
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- HY-151261
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HDAC
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Inflammation/Immunology
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HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity .
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- HY-144388
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Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and Aβ1-42 aggregation inhibitor with IC50s of 0.062, 0.767 and 1.227 µM for AChE, BuChE and Aβ1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent .
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- HY-158148
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c-Fms
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Neurological Disease
Inflammation/Immunology
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CSF1R-IN-23 (Compound 7dri) is a selective inhibitor for colony-stimulating factor-1 receptor (CSF1R), with IC50 of 36.1 nM. CSF1R-IN-23 serves as antineuroinflammatory agent in mouse model. CSF1R-IN-23 is blood brain barrier (BBB) permeable .
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- HY-144389
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Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD) .
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- HY-145833A
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Epoxide Hydrolase
Cholinesterase (ChE)
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Neurological Disease
Cancer
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sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively .
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- HY-33009
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Others
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Neurological Disease
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AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia .
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- HY-145833
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Epoxide Hydrolase
Cholinesterase (ChE)
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Neurological Disease
Cancer
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sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively .
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- HY-132310
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MAGL
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Neurological Disease
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MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
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- HY-115681
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6-Prenylnaringenin; (±)-6-Prenylnaringenin
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Calcium Channel
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Neurological Disease
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(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice .
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- HY-147395
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GPR52
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Neurological Disease
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GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity .
|
-
- HY-163909
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 0.59 μM. AChE-IN-72 inhibits BChE with an IC50 of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC50 of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable .
|
-
- HY-14327
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic .
|
-
- HY-13779
-
|
|
Monoamine Oxidase
Dopamine Transporter
|
Neurological Disease
|
|
(E/Z)-J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. (E/Z)-J147 can readily pass the blood brain barrier (BBB). (E/Z)-J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. (E/Z)-J147 has potential for the treatment of Alzheimer’s disease (AD) .
|
-
- HY-117983
-
|
|
Amyloid-β
|
Neurological Disease
|
|
RU-505 is an effective β-amyloid (Aβ)-fibrinogen interaction inhibitor with IC50s of 5.00 and 2.72 μM in fluorescence polarization (FP) and AlphaLISA assays, respectively. RU-505 is highly permeable to the BBB. RU-505 reduces cerebral amyloid angiopathy (CAA). RU-505 can be used for the research of Alzheimer’s disease (AD) .
|
-
- HY-17368
-
|
ENA 713 free base; SDZ-ENA 713 free base
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
- HY-150700
-
|
|
ERK
|
Metabolic Disease
|
|
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
|
-
- HY-11017
-
|
ENA 713; SDZ-ENA 713
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
- HY-150563
-
|
|
Monoamine Oxidase
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
|
Neuroinflammatory-IN-2 is a potent anti-neuroinflammatory agent with an IC50 value of 10.30 μM for MAO-B, and 96.33% inhibition of Aβ1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 has neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 also has biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activity and appropriate BBB permeability. Neuroinflammatory-IN-2 can be used for researching Alzheimer’s disease .
|
-
- HY-151928
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
|
-
- HY-17368S2
-
|
ENA 713-d3 hydrochloride; SDZ-ENA 713-d3 hydrochloride
|
Cholinesterase (ChE)
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Rivastigmine-d3 hydrochloride is deuterated labeled Rivastigmine (HY-17368). Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
- HY-17368R
-
|
ENA 713 (free base)(Standard); SDZ-ENA 713 (free base)(Standard)
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine (Standard) is the analytical standard of Rivastigmine. This product is intended for research and analytical applications. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
- HY-146383
-
|
|
Histamine Receptor
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB .
|
-
- HY-137499
-
|
|
Liposome
Endogenous Metabolite
|
Neurological Disease
|
|
NT1-O12B, an endogenous chemical and a neurotransmitter-derived lipidoid (NT-lipidoid), is an effective carrier for enhanced brain delivery of several blood-brain barrier (BBB)-impermeable cargos. Doping NT1-O12B into BBB-impermeable lipid nanoparticles (LNPs) gives the LNPs the ability to cross the BBB. NT-lipidoids formulation not only facilitate cargo crossing of the BBB, but also delivery of the cargo into neuronal cells for functional gene silencing or gene recombination .
|
-
- HY-115681R
-
|
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (Standard) is the analytical standard of (2R/S)-6-PNG. This product is intended for research and analytical applications. (2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice .
|
-
- HY-B0303AS1
-
-
- HY-B0303AS
-
-
- HY-162760
-
|
|
COMT
Monoamine Oxidase
|
Neurological Disease
|
|
COMT-IN-1 (compound C12), a nitrophenolic analogue, is an orally active dopamine metabolic enzyme catechol-O-methyltransferase (COMT) inhibitor with IC50s of 0.37 μM, 95.58 μM and 58.82 μM for COMT, MAO-A and MAO-B, respectively. COMT-IN-1 exhibits chelation with a variety of metal ions. COMT-IN-1 exhibits good BBB permeability. COMT-IN-1 improves dopamine levels and ameliorates MPTP (HY-15608)-induced Parkinson's disease (PD) symptoms in mice .
|
-
- HY-131688
-
|
|
PARP
Caspase
|
Inflammation/Immunology
|
|
2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrial membrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3 .
|
-
- HY-155365
-
|
|
Cholinesterase (ChE)
GSK-3
Amyloid-β
|
Neurological Disease
|
|
hAChE-IN-5 (compound 49) is a potent hAChE and hBuChE inhibitor with IC50 values of 0.17 μM and 0.17 μM, respectively. hAChE-IN-5 shows potent GSK3β inhibition with an IC50 value of 0.21 μM. hAChE-IN-5 is used as tau protein aggregation and Aβ1-42 self-aggregation inhibitor. hAChE-IN-5 can bind virtually with the PAS affecting Aβ aggregation, thus preventing Aβ-dependent neurotoxicity. hAChE-IN-5 can penetrate BBB and has the potential for multi-targeted anti-Alzheimer's agents research .
|
-
- HY-147319
-
|
|
Others
|
Neurological Disease
|
|
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .
|
-
- HY-134228
-
-
- HY-18738
-
|
Ammonium pyrrolidinedithiocarbamate; PDTC ammonium; APDC
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate) is a selective and blood-brain barrier (BBB) permeable NF-κB inhibitor.
|
-
- HY-P2342
-
-
- HY-152148
-
|
|
MAGL
|
Neurological Disease
|
|
JZP-MA-11 is a positron emission tomography (PET) ligand targeting the endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. JZP-MA-11 can cross the blood-brain barrier (BBB). [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP) .
|
-
- HY-131340
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
|
-
- HY-173029
-
|
|
Ferroptosis
|
Cancer
|
|
UAMC-4821 is an inhibitor for ferroptosis with an IC50 of 5.2 nM. UAMC-4821 scavenges free radicals, blocks the lipid peroxidation, inhibits ML162 (HY-100002)-induced ferroptosis, and exhibits protective effect in HT-1080 cell. UAMC-4821 exhibits good pharmacokinetics characteristics in mouse with an oral bioavailability of 63%. UAMC-4821 can cross blood-brain barrier .
|
-
- HY-170484
-
|
|
MAP3K
p38 MAPK
|
Neurological Disease
|
|
KAI-11101 is the inhibitor for dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. KAI-11101 inhibits Paclitaxel (HY-B0015)-induced cJun phosphorylation (IC50=95 nM) and thus inhibits the activation of MAPK pathway. KAI-11101 is blood brain barrier penetrable and can be further investigated for its neuroprotective property .
|
-
- HY-N9038
-
|
|
Others
|
Others
|
|
4',4''-Dihydroxyanigorootin is a Phenols product that can be isolated from the rhizomes of Musa cv.“thepanom” (BBB). .
|
-
- HY-169022
-
|
|
Autophagy
mTOR
|
Neurological Disease
|
|
4-FPBUA is a semisynthetic analog of usnic acid (HY-W015883) that can enhance cellular blood-brain barrier (BBB) function and increase the transport of Amyloid β (Aβ) across monolayer cells. 4-FPBUA is also an inhibitor of mTOR, capable of enhancing cellular Autophagy, thereby reversing BBB disruption in vivo and being utilized in research for Alzheimer's disease .
|
-
- HY-167906
-
-
- HY-N6685
-
|
|
Others
|
Cardiovascular Disease
|
|
3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative , is a blood-brain barrier (BBB) permeable mycotoxin .
|
-
- HY-P2297
-
-
- HY-137500
-
|
|
Liposome
|
Neurological Disease
|
|
NT1-014B is a potent NT1-lipidoid encapsulated AmB (amphotericin B). NT1-014B dopes the NT-lipidoids into BBB-impermeable lipid nanoparticles (LNPs) gave the LNPs the ability to cross the BBB. NT1-014B enhances brain delivery through intravenous injection .
|
-
- HY-161666
-
-
- HY-12763
-
GNE-317
1 Publications Verification
|
PI3K
mTOR
|
Cancer
|
|
GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
|
-
- HY-P2297A
-
-
- HY-147151
-
|
|
Biochemical Assay Reagents
|
Others
|
|
AMCPy is a potent electron paramagnetic resonance (EPR) brain imaging agent, possessing excellent lipophilicity for blood−brain barrier (BBB) penetration .
|
-
- HY-137207
-
MK-28
5 Publications Verification
|
PERK
|
Neurological Disease
|
|
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice .
|
-
- HY-157333
-
-
- HY-N9343
-
-
- HY-150972
-
|
|
Fungal
|
Infection
|
|
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration .
|
-
- HY-117501
-
|
|
Histamine Receptor
|
Inflammation/Immunology
Cancer
|
|
Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies .
|
-
- HY-164507
-
|
|
Drug Derivative
|
Neurological Disease
|
|
NRMA-7 is a BBB-penatrable small molecule nuclear receptor modulator. NRMA-7 can be used in the study of central nervous system diseases .
|
-
- HY-171306
-
|
|
Liposome
|
Others
|
|
MK16 is a lipid material that can be used to construct blood-brain barrier penetrable lipid nanoparticles for mRNA delivery .
|
-
- HY-162565
-
|
|
STK33
CDK
RET
|
Endocrinology
|
|
CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC50 of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive .
|
-
- HY-158765
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Leuco ethyl violet is a photooxidation catalyst for amyloid selectivity and blood-brain barrier (BBB) permeability. Leuco ethyl violet can be used in the study of Alzheimer's disease (AD) .
|
-
- HY-17383A
-
|
|
Antifolate
|
Neurological Disease
|
|
Levomefolate disodium is an orally active, BBB-penatrable and active form of folic acid. Levomefolate disodium can be used as a food supplement for folic acid and in the research of neural tube defect diseases .
|
-
- HY-B0303A
-
-
- HY-P0285
-
|
|
RABV
|
Infection
|
|
Rabies Virus Glycoprotein is a 29-amino-acid cell penetrating peptide derived from a rabies virus glycoprotein that can cross the blood-brain barrier (BBB) and enter brain cells.
|
-
- HY-149253
-
|
|
Others
|
Neurological Disease
|
|
OY-201 is a potential and BBB-penetrated anti-ischemic stroke agent. OY-201 shows the good safety and neuroprotective activity in both in vitro and in vivo models .
|
-
- HY-144765
-
|
|
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research .
|
-
- HY-144392
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research .
|
-
- HY-125602
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
MNI-444 is a BBB-penetrable ligand of adenosine 2A receptor (A2AR). A2AR is a potential non-dopaminergic target for the research of Parkinson’s disease .
|
-
- HY-119953
-
|
|
mAChR
|
Neurological Disease
|
|
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
|
-
- HY-155024
-
|
|
Parasite
|
Infection
|
|
HAT-IN-8 (Compound 38) is a BBB-penetrable T. brucei inhibitor (EC50: 0.18 μM). HAT-IN-8 can be used for the research of Human African trypanosomiasis .
|
-
- HY-B0303
-
-
- HY-100475
-
|
|
Apoptosis
MDM-2/p53
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation .
|
-
- HY-13909
-
|
|
HDAC
|
Cancer
|
|
RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
|
-
- HY-P10777
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
ANG1009 is a BBB-penatrable anticancer agent. ANG1009 is cytotoxic to a variety of tumor cells and can induce cell cycle arrest. ANG1009 can be used in the study of brain cancer .
|
-
- HY-18749
-
-
- HY-17383
-
|
|
Antifolate
|
Neurological Disease
|
|
Levomefolate calcium is an orally active, BBB-penatrable and active form of folic acid. Levomefolate calcium can be used as a food supplement for folic acid and in the research of neural tube defect diseases .
|
-
- HY-153432
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
TRV-7019 is a BBB-penetrable radioligand for brain imaging that target butyrylcholinesterase. TRV-7019 can be used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity .
|
-
- HY-158693
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
WLB-87848 is a selective, orally active, and blood-brain barrier (BBB) permeable σ1 receptor agonist with the Ki of 9 nM. WLB-87848 rescues recognition memory impairment .
|
-
- HY-P0285A
-
|
|
RABV
|
Infection
|
|
Rabies Virus Glycoprotein (TFA) is a 29-amino-acid cell penetrating peptide derived from a rabies virus glycoprotein that can cross the blood-brain barrier (BBB) and enter brain cells .
|
-
- HY-145888
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Antioxidant agent-2 (comp 3c), an BBB-penetrated antioxidant agent and a selective metal ions chelator, presents good neuroprotective effect and hepatoprotective effect for the study of Alzheimer’s disease .
|
-
- HY-149097
-
|
|
Phosphatase
|
Neurological Disease
|
|
ITH12711 is a PP2A ligand. ITH12711 is able to cross the blood-brain barrier (BBB). ITH12711 exerts neuroprotection via restoration of PP2A-phosphatase activity .
|
-
- HY-169287
-
|
|
Apoptosis
Ferroptosis
|
Neurological Disease
Cancer
|
|
TriPEX-ClO4 is a cationic fluorescent anticancer agent capable of BBB penetration. TriPEX-ClO4 can induces apoptosis and ferroptosis and can be used for study of cancer and brain diseases .
|
-
- HY-162039
-
|
|
MMP
|
Cancer
|
|
MMP-11-IN-1 (compound 9) is a new class of phosphinate prodrug. MMP-11-IN-1 is a glycosyl ester of RXP03 and improves blood–brain barrier (BBB) behavior .
|
-
- HY-147681
-
|
|
FGFR
|
Neurological Disease
|
|
SUN13837 is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. SUN13837 shows neuroprotective activity. SUN13837 can be used for neurodegenerative diseases research .
|
-
- HY-168915
-
|
|
Akt
PKA
|
Cancer
|
|
ML-B01 is the orally active inhibitor for Akt and PKA with the IC50 of 2 nM and 136 nM. ML-B01 exhibits good ability to penetrate the blood-brain barrier (BBB) in the mouse brain .
|
-
- HY-136430
-
|
JGK037
|
EGFR
|
Cancer
|
|
JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively .
|
-
- HY-15722
-
-
- HY-120874
-
|
|
GABA Receptor
|
Neurological Disease
|
|
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
|
-
- HY-162786
-
-
- HY-161683
-
|
|
JAK
|
Neurological Disease
|
|
Tyk2-IN-19 (compound 1) is an orally active and blood-brain barrier (BBB) permeable Tyk2 inhibitor. Tyk2-IN-19 can be used for study of neurodegenerative diseases .
|
-
- HY-126899
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain .
|
-
- HY-101456
-
|
4-Chloro-DL-phenylalanine methyl ester hydrochloride
|
Tryptophan Hydroxylase
5-HT Receptor
|
Neurological Disease
|
|
PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability .
|
-
- HY-121191
-
|
N1,N8-Bisnorcymserine; (-)-Bisnorcymserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate .
|
-
- HY-P10911
-
|
|
LDLR
|
Others
|
|
IETP2 targets low-density lipoprotein receptor-related protein 1 (LRP1) with a KD of 738 nM and can be used for drug- and imaging agents delivery across the blood-labyrinth barrier (BLB) .
|
-
- HY-170898
-
|
|
iGluR
|
Neurological Disease
|
|
Antidepressant agent 8 (Compound 1f) is a selective antagonist for the NMDA receptor GluN1/2A with an IC50 of 2.94 μmol/L. Antidepressant agent 8 exhibits antidepressant-like effects in Hydrocortisone (HY-N0583)-induced zebrafish depression model. Antidepressant agent 8 can cross blood-brain barrier .
|
-
- HY-B1410
-
|
MP-328
|
Biochemical Assay Reagents
|
Others
Cancer
|
|
Ioversol (MP-328) is a nonionic iodinated contrast medium (CM) that is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal .
|
-
- HY-153773
-
Z4P
2 Publications Verification
|
IRE1
|
Cancer
|
|
Z4P is a BBB-penatrable IRE1 inhibitor with an IC50 of 1.13 μM. Z4P in combination with Temozolomide (HY-17364) inhibits the growth and recurrence of glioblastoma and has anti-tumor activity .
|
-
- HY-P1178
-
|
|
Trk Receptor
p38 MAPK
|
Neurological Disease
|
|
Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects .
|
-
- HY-148787
-
|
SAR443820; DNL788
|
RIP kinase
|
Neurological Disease
Inflammation/Immunology
|
|
Oditrasertib (SAR443820) is an orally active, BBB-penatrable and selective reversible inhibitor of RIPK1. Oditrasertib can be used in the research of chronic inflammatory central nervous system diseases, such as amyotrophic lateral sclerosis and multiple sclerosis .
|
-
- HY-147668
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 6 (compound 3ge) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.70 μM and inhibition ratio at 30 μM of 94.4% .
|
-
- HY-147666
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2% .
|
-
- HY-147669
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 7 (compound 3gf) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.95 μM and inhibition ratio at 30 μM of 85.8% .
|
-
- HY-147667
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.22 μM and inhibition ratio at 30 μM of 94.3% .
|
-
- HY-120946
-
|
|
nAChR
|
Neurological Disease
|
|
VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction .
|
-
- HY-W265961
-
|
ST1859; 1,1′-Methylenedi-2-naphthol
|
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
|
Squoxin (ST1859) is an antiamyloid agent that specifically binds to Aβ1-42 and prevents the aggregation and fibril formation of Aβ. Squoxin crosses the blood-brain barrier (BBB) and has anthelmintic activity and anti-inflammatory properties .
|
-
- HY-147683
-
|
|
FGFR
|
Neurological Disease
|
|
FGFR-IN-3 (compound 6) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-3 shows neuroprotective activity. FGFR-IN-3 can be used for neurodegenerative diseases research .
|
-
- HY-N12171
-
|
|
Bacterial
|
Infection
Neurological Disease
|
|
Isoreserpiline is an orally active and BBB-penatrable indole alkaloids with antibacterial and antipsychotic activity. Isoreserpiline is even more effective when used in combination with antibiotics and inhibits the activity of bacterial efflux pumps. Isoreserpiline improves Amphetamine-induced hyperactivity in mice .
|
-
- HY-143877
-
|
|
HDAC
|
Cancer
|
|
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
|
-
- HY-N6685R
-
|
|
Others
|
Cardiovascular Disease
|
|
3-Acetyldeoxynivalenol (Standard) is the analytical standard of 3-Acetyldeoxynivalenol. This product is intended for research and analytical applications. 3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative , is a blood-brain barrier (BBB) permeable mycotoxin .
|
-
- HY-146313
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species .
|
-
- HY-121599
-
|
SGS-742
|
GABA Receptor
|
Neurological Disease
|
|
CGP 36742 is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a blood-brain barrier (BBB) penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study .
|
-
- HY-110180
-
|
|
mGluR
|
Neurological Disease
|
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
|
-
- HY-151615
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
DCI-Br-3 is a rapid, highly sensitive, and selective probe to monitor thiols in the epileptic brain. (λex=537 nm, λem=675 nm).DCI-Br-3 can effectively cross the blood-brain barrier (BBB) .
|
-
- HY-130630
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .
|
-
- HY-170392
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
Vasorelaxant agent-1 (Compound 2j) is a BBB-penatrable vasodilator. Vasorelaxant agent-1 has excellent vasodilator activity with an EC50 of 0.02916 μM. Vasorelaxant agent-1 is non-carcinogenic and can be used in the study of hypertension .
|
-
- HY-146588
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease .
|
-
- HY-B0303AR
-
|
|
Histamine Receptor
Endogenous Metabolite
Bacterial
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
Diphenhydramine (hydrochloride) (Standard) is the analytical standard of Diphenhydramine (hydrochloride). This product is intended for research and analytical applications. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
|
-
- HY-P10310
-
|
|
HIV
|
Infection
|
|
F9170 is an amphipathic peptide with an activity of inactivate HIV-1 virions. F9170 targets the conserved cytoplasmic tail of HIV-1 env and disrupts the integrity of the viral membrane. F9170 is able to cross the blood-brain barrier (BBB) .
|
-
- HY-135714
-
|
EKZ-001
|
HDAC
Microtubule/Tubulin
|
Neurological Disease
Cancer
|
|
Bavarostat (EKZ-001) is a BBB-penetrable and selective HDAC6 inhibitor (IC50: 0.06 μM). Bavarostat modulates tubulin acetylation selectively over histone acetylation. Bavarostat can be used for research of cancers and central nervous system (CNS) disorders .
|
-
- HY-161256
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 41 (Compd D19), a promising anti-GBM (glioblastoma) lead compound and tublin inhibitor with BBB permeability, induces G2/M phase arrest, resulted in cell apoptosis and inhibits the migration of U87 cells .
|
-
- HY-10358
-
|
MK-2206 (2HCl)
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
|
-
- HY-173142
-
|
|
Drug Derivative
|
Neurological Disease
|
|
Neuroprotective agent 7 (Compound 13) is a BBB-penatrable neuroprotective agent. Neuroprotective agent 7 has a powerful neuroprotective effect and can reduce the cerebral infarct area in the MCAO rat model. Neuroprotective agent 7 can be used in the research of diseases such as cerebral ischemia .
|
-
- HY-50682A
-
|
TTP488 dihydrochloride; PF-04494700 dihydrochloride
|
Amyloid-β
|
Neurological Disease
Cancer
|
|
Azeliragon dihydrochloride (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD) . Azeliragon dihydrochloride also can cross the blood-brain barrier (BBB) .
|
-
- HY-P10359
-
|
|
TGF-beta/Smad
MMP
|
Neurological Disease
|
|
TAT-QFNP12 is a peptide that blocks the NDRG2-PPM1A binding and reduces Smad2/3 phosphorylation, decreases astrocytic MMP-9 production and BBB disruption after subarachnoid hemorrhage (SAH) .
|
-
- HY-P3895
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Substance P (3-11) is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) has contracting activities on guinea pig ileum. Substance P (3-11) also promotes human monocyte chemotaxis .
|
-
- HY-173046
-
-
- HY-50682
-
|
TTP488; PF-04494700
|
Amyloid-β
|
Neurological Disease
|
|
Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD) . Azeliragon also can cross the blood-brain barrier (BBB) .
|
-
- HY-B0303R
-
-
- HY-N6685S1
-
|
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
3-Acetyldeoxynivalenol- 13C17 is the 13C labeled 3-Acetyldeoxynivalenol (HY-N6685) . 3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative , is a blood-brain barrier (BBB) permeable mycotoxin .
|
-
- HY-172419
-
|
GM-1020
|
iGluR
|
Neurological Disease
|
|
Blixeprodil (GM-1020) is the orally active antagonist for NMDA receptor with an affinity of Ki=3.25 µM in rat cortical tissue. Blixeprodil inhibits NR1/2A-NMDAR-mediated currents in HEK293 cell with IC50 of 1.192 µM. Blixeprodil exhibits antidepressant in rats models. Blixeprodil can cross blood-brain barrier .
|
-
- HY-146049
-
|
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively . Antitrypanosomal agent 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-123439
-
|
|
Others
|
Neurological Disease
|
|
FTY720-C2 is a derivative of FTY72 (HY-12005). FTY720-C2 promotes the expression of brain-derived neurotrophic factor (BDNF) and glial cell-derived neurotrophic factor (GDNF) in multiple system atrophy (MSA) models, without causing immunosuppression. FTY720-C2 improves motor dysfunction and reduces the levels of insoluble alpha-synuclein (αSyn) in MSA mouse models. FTY720-C2 is blood-brain barrier penetrate .
|
-
- HY-168966
-
|
|
Phosphodiesterase (PDE)
iGluR
|
Neurological Disease
|
|
PDE2 inhibitor 6 (Compound 1) is the orally active inhibitor for phosphodiesterase (PDE) that inhibits PDE2A, PDE3B, and PDE10A2 with IC50s of 0.95 nM, 6.17 μM (pIC50=5.21) and 87.1 nM (pIC50=7.06), respectively. PDE2 inhibitor 6 modulates the activity of AMPA receptor, enhance the synaptic plasticity and promotes the learning and memory function in rats models. PDE2 inhibitor 6 can cross blood-brain barrier .
|
-
- HY-69019A
-
|
|
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
7-Nitroindazole sodium is a selective and BBB-penatrable inhibitor of nitric oxide synthase (NOS). 7-Nitroindazole sodium can inhibit the activity of central NOS with an IC50 of 0.47 μM in the cerebellum of mice. 7-Nitroindazole sodium has anti-injurious and neuroprotective properties .
|
-
- HY-149212
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
SD-6 is an orally active inhibitor of hAChE and hBChE with IC50 values of 0.907 µM and 1.579 µM, respectively. SD-6 has excellent blood-brain barrier (BBB) permeability and no neurotoxicity, which can be used for research on Alzheimer's disease .
|
-
- HY-105283
-
|
|
Sodium Channel
|
Others
Neurological Disease
|
|
PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain .
|
-
- HY-160168
-
-
- HY-17547
-
|
|
HSP
|
Cancer
|
|
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy .
|
-
- HY-117727A
-
|
MIN-102 hydrochloride; Hydroxypioglitazone hydrochloride
|
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride is an orally active and a BBB-penatrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone hydrochloride, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone hydrochloride can be used in the study of neuroinflammatory and neurodegenerative diseases .
|
-
- HY-170798
-
|
|
Monoamine Oxidase
SOD
Glutathione Peroxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 6 (Compound BT5) is a BBB-penatrable, highly selective, reversible and competitive MAO-B inhibitor, with an IC50 of 0.11 μM. Monoamine Oxidase B inhibitor 6 has antioxidant and neuroprotective effects and can be used in the research of neurodegenerative diseases .
|
-
- HY-117727
-
|
MIN-102; Hydroxypioglitazone
|
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Leriglitazone (MIN-102; Hydroxypioglitazone) is an orally active and a BBB-penatrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
|
-
- HY-155939
-
|
|
TGF-β Receptor
|
Cancer
|
|
M4K2163 dihydrochloride is a potent, selective, blood-brain barrier (BBB) permeable activin receptor-like kinase-2 (ALK2) inhibitor, with an IC50 of 19 nM. M4K2163 dihydrochloride can be used in the research of diffuse intrinsic pontine glioma (DIPG) .
|
-
- HY-168563
-
|
|
Cholinesterase (ChE)
FAAH
|
Neurological Disease
|
|
BuChE-IN-15 (compound D12) is a selective BuChE/FAAH dual inhibitor with and show IC50 values of 81 and 400 nM for hBuChE and hFFAH, respectively. BuChE-IN-15 possesses good BBB penetration, and shows neuroprotection.BuChE-IN-15 can be used for study of Alzheimer .
|
-
- HY-69019
-
|
|
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
7-Nitroindazole is a selective and BBB-penatrable inhibitor of nitric oxide synthase (NOS). 7-Nitroindazole can inhibit the activity of central NOS with an IC50 of 0.47 μM in the cerebellum of mice. 7-Nitroindazole has anti-injurious and neuroprotective properties .
|
-
- HY-147030
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
|
-
- HY-N7109
-
|
|
PI3K
Endogenous Metabolite
|
Neurological Disease
|
|
Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia
.
|
-
- HY-P10782
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
Pt(IV)-M13 is a BBB-penatrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .
|
-
- HY-161029
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (Ki=22 nM, IC50=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .
|
-
- HY-N7109B
-
|
|
PI3K
Endogenous Metabolite
|
Neurological Disease
|
|
Erucic acid sodium, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid sodium can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid sodium can improve cognitive impairment and be effective against dementia .
|
-
- HY-169116
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D5R agonist 1 (Compound 5j) is a selective, orally active and BBB penetrable D5R partial agonist (EC50: 269.7 nM). D5R agonist 1 enhances the cognition in the Scopolamine (HY-N0296)-induced amnesia model .
|
-
- HY-173157
-
|
|
iGluR
|
Neurological Disease
Inflammation/Immunology
|
|
Analgesic/antidepressant agent-1 (Compound k1) is an orally active and BBB-penatrable N-acetamide ketamine derivative. Analgesic/antidepressant agent-1 has a strong binding affinity for the NMDA receptor, possesses analgesic, anti-inflammatory, and antidepressant activities, and has low psychomimetic activity .
|
-
- HY-163369
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-35 (compound C4 (ZINC000077541942)) is a potent and BBB-penetrated HDAC6 inhibitor with the IC50 of 4.7 μM. HDAC6-IN-35 shows cell toxicity against MDA-MB-231 with EC50 of 40.6 μM .
|
-
- HY-144610
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD) .
|
-
- HY-159578S
-
|
|
mAChR
|
Neurological Disease
|
|
VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
|
-
- HY-76772
-
|
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
Cancer
|
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
|
-
- HY-111187
-
|
KX-02
|
Src
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell .
|
-
- HY-116820
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
OS-3-106 is a potent, BBB-penetrated and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research .
|
-
- HY-70020B
-
|
AF102B hydrochloride
|
mAChR
|
Neurological Disease
Cancer
|
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
|
-
- HY-17383R
-
|
|
Antifolate
|
Neurological Disease
|
|
Levomefolate (calcium) (Standard) is the analytical standard of Levomefolate (calcium). This product is intended for research and analytical applications. Levomefolate (calcium) is an orally active, BBB-penatrable and active form of folic acid. Levomefolate (calcium) can be used as a food supplement for folic acid and in the research of neural tube defect diseases .
|
-
- HY-164512
-
|
|
Drug Intermediate
|
Neurological Disease
|
|
NRMA-I is the amide produrg of the small molecule nuclear receptor modulator. NRMA-I exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-I can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .
|
-
- HY-B1410R
-
|
|
Biochemical Assay Reagents
|
Others
Cancer
|
|
Ioversol (Standard) is the analytical standard of Ioversol. This product is intended for research and analytical applications. Ioversol (MP-328) is a nonionic iodinated contrast medium (CM) that is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal [4].
|
-
- HY-147953
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC50 value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease .
|
-
- HY-105327
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease .
|
-
- HY-14759
-
|
PAZ-417
|
PAI-1
Amyloid-β
|
Neurological Disease
|
|
Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research .
|
-
- HY-170945
-
|
|
iGluR
Serotonin Transporter
|
Neurological Disease
|
|
Antidepressant agent 9 (Compound 24) is an orally active and BBB-penatrable NMDAR and SERT inhibitor with IC50 values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test .
|
-
- HY-144446
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD). BuChE-IN-1 shows low cytotoxicity and high blood brain barrier (BBB) permeability. BuChE-IN-1 is a promising BuChE inhibitor for the research of AD .
|
-
- HY-114320
-
|
TM-10
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease .
|
-
- HY-P10822
-
|
|
Caspase
|
Neurological Disease
|
|
ED11 is a potent and selective caspase-6 inhibitor with an IC50 of 12.12 nM. ED11 competes with Htt for the caspase-6 active site, and thus reduce Htt cleavage. ED11 can cross the blood-brain barrier (BBB). ED11 has the potential for the study of Huntington's disease (HD) .
|
-
- HY-P3223
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-19838
-
|
|
GPR139
|
Neurological Disease
|
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB) .
|
-
- HY-P99694
-
|
JR-171
|
Transferrin Receptor
|
Neurological Disease
|
|
Lepunafusp alfa (JR-171) is a BBB-penetrable fusion protein consisting of J-Brain Cargo and IDUA (a lysosomal enzyme, α-L-iduronidase). Lepunafusp alfa can reduce concentration of heparan sulfate (HS) and dermatan sulfate (DS). Lepunafusp alfa can be used for research of mucopolysaccharidosis type I .
|
-
- HY-13289A
-
|
SYN-117 hydrochloride; RS-25560-197 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB) .
|
-
- HY-134189
-
|
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
|
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
|
-
- HY-P2343
-
|
|
Apoptosis
|
Cancer
|
|
BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian .
|
-
- HY-70020
-
|
AF102B
|
mAChR
|
Neurological Disease
Cancer
|
|
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline can cross the blood-brain barrier (BBB) .
|
-
- HY-156432
-
|
|
Anaplastic lymphoma kinase (ALK)
mTOR
PARP
Caspase
|
Cancer
|
|
ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies .
|
-
- HY-P10861
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 is an orally active and a BBB-penatrable Tau aggregation peptide inhibitor. RI-AG03 inhibits Tau aggregation and improves associated neurodegeneration and behavioral phenotypes in both in vivo and in vitro models. RI-AG03 can be used in the study of tauopathies such as Alzheimer's disease .
|
-
- HY-147684
-
|
|
FGFR
|
Neurological Disease
|
|
FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research .
|
-
- HY-139464
-
|
|
Nuclear Factor of activated T Cells (NFAT)
|
Neurological Disease
|
|
Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer's disease (AD) and aging-related disorders research .
|
-
- HY-128868D
-
|
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 40000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 40000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 40000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption .
|
-
- HY-138967
-
|
|
Nuclear Hormone Receptor 4A/NR4A
RAR/RXR
|
Neurological Disease
|
|
BRF110 is the selective, orally active rexinoid for Nurr1-RXRα, that selectively activates the Nurr1-RXRα heterodimer with an EC50 of 0.9 μM in SH-SY5Y. BRF110 upregulates the expression of BDNF, exhibits neuroprotective activity against MPP+ induced toxicity. BRF110 can cross blood-brain barrier .
|
-
- HY-B2150S
-
|
4-Hydroxyphenazone-d3; NSC 174055-d3
|
Drug Metabolite
Isotope-Labeled Compounds
|
Others
|
|
4-Hydroxyantipyrine-d3 is the deuterium labeled 4-Hydroxyantipyrine. 4-Hydroxyantipyrine is the major metabolite of Antipyrine, can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Antipyrine in the brain[1][2][3].
|
-
- HY-153831
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-17 is a potent c-Met kinase inhibitor with an IC50 of 0.031 μM. c-Met-IN-17 can be used in anticancer research. . c-Met-IN-17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-13788
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent .
|
-
- HY-128868
-
|
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 10000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 10000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 10000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption .
|
-
- HY-118152
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively .Org-12962 displays antiaversive effects in a rat model of panic-like anxiety .
|
-
- HY-128868A
-
|
|
Fluorescent Dye
|
Others
|
|
FITC-Dextran (MW 4000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 4000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 4000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption .
|
-
- HY-13788B
-
|
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent .
|
-
- HY-21994
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model .
|
-
- HY-108801A
-
|
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease .
|
-
- HY-D1672
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
TMR Biocytin is a polar tracer used in the research of cell-cell and cell-liposome fusions, as well as membrane permeability and cellular uptake during pinocytosis. TMR Biocytin can be detected using streptavidin, and is an effective neuronal tracer in live tissue (Ex=544 nm, Em=571 nm) .
|
-
- HY-141660
-
-
- HY-108801
-
|
VEGF Trap; VEGF-TRAPR1R2; VEGF-trapR1
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease .
|
-
- HY-N4134
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory .
|
-
- HY-157400
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-7 (compound 11n) is a potent and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B), with the IC50 value of 0.79±0.05 μM. hMAO-B-IN-7 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
|
-
- HY-P1335
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-122559
-
|
|
mGluR
|
Neurological Disease
|
|
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
|
-
- HY-163415
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-IN-5 (Compound ZINC000016952895) is a monoamine oxidase (MAO) inhibitor. According to the prediction of Swiss ADME, MAO-IN-5 can inhibit the CYP enzyme family, has blood-brain barrier (BBB) permeability, and has a high gastrointestinal absorption rate. MAO-IN-5 can be used in the study of neurological diseases .
|
-
- HY-162750
-
|
|
DYRK
Tau Protein
|
Neurological Disease
|
|
ZJCK-6-46 (32) is a potential and orally activeDYRK1A inhibitor (IC50 = 0.68 nM) with high BBB permeability (CNS+). ZJCK-6-46 (32) reduces tau phosphorylation. ZJCK-6-46 (32) ameliorates cognitive dysfunction by obviously reducing the expression of phosphorylated tau and neuronal loss in vivo .
|
-
- HY-B1715
-
|
ISF2522
|
GABA Receptor
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
Oxiracetam (ISF2522) is an orally active and a BBB-penatrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases .
|
-
- HY-171033
-
|
|
Phospholipase
|
Neurological Disease
|
|
ASM-IN-3 (Compound 21b) is a selective and BBB-penetrating acid sphingomyelinase (ASM) inhibitor (IC50: 3.37 μM for pure human ASM). ASM-IN-3 improves depression-like behaviors by inhibiting ASM activity and increasing neurogenesis in hippocampus in Reserpine (HY-N0480)-induced depressed rats .
|
-
- HY-134189A
-
|
|
Sigma Receptor
Opioid Receptor
|
Neurological Disease
|
|
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
|
-
- HY-161842
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-67 (compound 8n) is a potent AChE inhibitor, with an IC50 of 0.033 μM. AChE-IN-67 exhibits activity similar to Donepezil (HY-14566). AChE-IN-67 exhibits high blood-brain barrier (BBB) permeability. AChE-IN-67 can be used for Alzheimer's disease research .
|
-
- HY-124160
-
|
|
iGluR
|
Neurological Disease
|
|
JNJ-56022486 is an orally active and potent negative AMPA receptor modulator (Ki=19 nM) selective for?TARP-γ8. JNJ-56022486 is also a TARP-γ8 receptor antagonist, with blood?brain?barrier (BBB) permeability. JNJ-56022486 can be used for research of Epilepsy .
|
-
- HY-107663
-
|
Pro-Leu-Gly-NH2; Melanostatin
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-147748
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC50 of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase .
|
-
- HY-13289
-
|
SYN117; RS-25560-197
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB) .
|
-
- HY-15771
-
|
ONO-4059; GS-4059
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies .
|
-
- HY-170905S
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-22 (Compound 29-1) is a BBB-penatrable and orally active MAT2A inhibitor with an IC50 of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects .
|
-
- HY-124813
-
|
113B7
|
FAK
EGFR
MMP
|
Cancer
|
|
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion .
|
-
- HY-164311
-
|
|
Transmembrane Glycoprotein
|
Neurological Disease
|
|
GPR17 modulator-1 (Compound 2-046) is a modulator for G protein-coupled receptor 17 GPR17, with an IC50<10 nM for hGPR17 in CHO. GPR17 modulator-1 exhibits moderate pharmacokinetic characteristics in mice. GPR17 modulator-1 ix blood-brain barrier (BBB) permeable .
|
-
- HY-107529
-
|
|
GSK-3
|
Neurological Disease
Metabolic Disease
|
|
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases .
|
-
- HY-15771A
-
|
ONO-4059 hydrochloride; GS-4059 hydrochloride
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies .
|
-
- HY-12678
-
|
NMS-E628; RXDX-101
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-148250
-
|
|
iGluR
|
Neurological Disease
|
|
TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission .
|
-
- HY-D2268
-
|
|
Fluorescent Dye
Amyloid-β
|
Neurological Disease
|
|
QM-FN-SO3 is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 can be used for in vivo detection of Aβ plaques. QM-FN-SO3 has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
|
-
- HY-B0602
-
|
O-Desmethylvenlafaxine
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-N7109R
-
|
|
PI3K
Endogenous Metabolite
|
Neurological Disease
|
|
Erucic acid (Standard) is the analytical standard of Erucic acid. This product is intended for research and analytical applications. Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia .
|
-
- HY-W004425
-
|
3,7-Dimethyl-1-propargylxanthine
|
Adenosine Receptor
|
Neurological Disease
|
|
DMPX (3,7-Dimethyl-1-propargylxanthine) is a BBB-penatrable caffeine analogue. DMPX is A2 selective adenosine receptor (AR) antagonist that strongly and selectively blocks hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists such as NECA (HY-103173). DMPX can be used in the study of Parkinson's disease and other diseases .
|
-
- HY-170907
-
|
|
HDAC
DNA/RNA Synthesis
RAD51
|
Cancer
|
|
HDAC-IN-85 (Compound 1) is a BBB-permeable HDAC inhibitor. HDAC-IN-85 has an inhibitory effect on brain tumor cell lines. HDAC-IN-85 can induce acetylation, leading to DNA double-strand breaks, and induce the ubiquitination of RAD51, disrupting the DNA repair process. HDAC-IN-85 can be used in the research of glioblastoma .
|
-
- HY-N8852
-
|
6-MeOF
|
GABA Receptor
|
Neurological Disease
|
|
6-Methoxyflavanone (6-MeOF) is an orally active flavonoid compound. 6-Methoxyflavanone has anxiolytic properties. 6-Methoxyflavanone targets unique sites on GABA-A receptors, different from traditional benzodiazepines. 6-Methoxyflavanone can be used to study anxiety disorders. 6-Methoxyflavanone readily crosses the blood brain barrier (BBB) .
|
-
- HY-161663
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
|
-
- HY-147697
-
|
|
Histone Demethylase
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC50 of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity .
|
-
- HY-P1335A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-150791
-
|
|
Reactive Oxygen Species
DNA/RNA Synthesis
|
Cancer
|
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells .
|
-
- HY-146315
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE-IN-6 (compound 22) is a potent dual AChE/BChE inhibitor with IC50 values of 0.809 µM, 2.248 µM and > 100 µM for hBChE, hAChE and hMAO-B, respectively. AChE/BChE-IN-6 penetrates the blood-brain barrier (BBB). AChE/BChE-IN-6 can be used for Alzheimer’s disease (AD) research .
|
-
- HY-146312
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity .
|
-
- HY-149014
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
|
-
- HY-161331
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
S16–1029 is a selective and orally active butyrylcholinesterase (BChE) inhibitor with IC50s of 11.35 nM and 48.1 nM for eqBChE and hBChE, respectively. S16–1029 could cross the blood-brain barrier (BBB) and reach the central nervous system (CNS). S16–1029 can be used for Alzheimer's disease (AD) research .
|
-
- HY-143413
-
|
|
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
|
BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu 2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease .
|
-
- HY-A0031
-
|
TSE-424
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-137262
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Protein deglycase DJ-1 against-1, a DJ-1-binding compound, dependently targets DJ1. Protein deglycase DJ-1 against-1 penetrates through the blood brain barrier (BBB). Protein deglycase DJ-1 against-1 is used as a neuroprotective agent and has the potential for Parkinson's disease research .
|
-
- HY-15008
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor .
|
-
- HY-N1501
-
|
|
α-synuclein
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Beta-asarone is an orally active and BBB-penatrable anti-inflammatory agent and neuroprotective agent, which is the major ingredient of Acorus tatarinowii Schott. Beta-asarone can protect nerve cells from apoptosis and autophagy, inhibit expression of α-synuclein, as well as myocardial protection. Beta-asarone can be used in the study of neurological and cardiovascular diseases .
|
-
- HY-172461
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
MAO-IN-6 (Compound 3f) is a BBB permeable and reversible MAO-B inhibitor with an IC50 of 0.09 μM. MAO-IN-6 also exhibits certain inhibitory activities against AChE and BChE, with IC50 values of 4.48 μM and 17.03 μM, respectively. MAO-IN-6 has low cytotoxicity and can be used in the research of Alzheimer's disease .
|
-
- HY-146347
-
|
|
Monoamine Oxidase
Amyloid-β
|
Neurological Disease
|
|
MAO-B-IN-10 (compound 4f) is a potent, selective, BBB-penetrated MAO-B (monoamine oxidase-B) inhibitor, with IC50 of 5.3 μM. MAO-B-IN-10 can inhibit (58.2%) and disaggregate (43.3%) self-mediated Aβ (amyloid β) aggregation. MAO-B-IN-10 can be use for Alzheimer’s disease research .
|
-
- HY-B0602A
-
|
O-Desmethylvenlafaxine succinate hydrate; Desvenlafaxine succinate monohydrate
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-117727S
-
|
MIN-102-d4; Hydroxypioglitazone-d4
|
Isotope-Labeled Compounds
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penatrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
|
-
- HY-121156
-
|
LF 16-0687; XY-2405
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
|
-
- HY-121156A
-
|
LF 16-0687 hydrochloride; XY-2405 hydrochloride
|
Bradykinin Receptor
|
Neurological Disease
|
|
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
|
-
- HY-147027
-
|
|
PARP
Caspase
Apoptosis
|
Cancer
|
|
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
|
-
- HY-106004
-
|
BIA 5-1058
|
Dopamine β-hydroxylase
P-glycoprotein
BCRP
|
Cardiovascular Disease
Cancer
|
|
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8?μM and 17.0?μM, respectively . Zamicastat reduces high blood pressure .
|
-
- HY-107531
-
|
|
GSK-3
|
Neurological Disease
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain. A 1070722 decreases spontaneous locomotion .
|
-
- HY-168494
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2A Allosteric modulator 1 (Compound 11) is an orally active, BBB-penatrable and highly selective GluN2A negative allosteric modulator. GluN2A Allosteric modulator 1 has IC50 values of 0.042 μM and 13 μM for GluN2A and GluN2B, respectively. GluN2A Allosteric modulator 1 can be used for the research of nervous system diseases .
|
-
- HY-16170
-
|
O-Desmethylvenlafaxine succinate; Wy-45233 succinate
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
|
Desvenlafaxine succinate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate (DVS) shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-107663A
-
|
Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-W010936
-
|
NBMPR
|
Adenosine Receptor
|
Neurological Disease
|
|
Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier .
|
-
- HY-17366
-
|
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
|
-
- HY-110278
-
|
|
mGluR
|
Neurological Disease
|
|
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity .
|
-
- HY-17366R
-
-
- HY-B2150
-
|
4-Hydroxyphenazone; NSC 174055
|
Drug Metabolite
|
Others
|
|
4-Hydroxyantipyrine (4-Hydroxyphenazone; NSC 174055) is the major metabolite of Antipyrine (HY-B0171), can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Citicoline and Antipyrine in the brain .
|
-
- HY-170499
-
|
BI02982816
|
mGluR
|
Neurological Disease
|
|
VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
|
-
- HY-168096
-
|
|
NO Synthase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
iNOs-IN-5 (Compound BN-4) is an inhibitor for iNOS with an IC50 of 0.1707 μM, and reduces NO levels in LPS (HT-D1056)-induced RAW264.7 cells. iNOs-IN-5 reduces the hypoxic injury stimulated ROS and lactate dehydrogenase expression, and exhibits anti-necrosis and anti-apoptosis efficacy. iNOs-IN-5 exhibits anti-cerebral ischemia and neuroprotective activities in SD rat models. iNOs-IN-5 is blood-brain barrier penetrable .
|
-
- HY-111136
-
|
|
GABA Receptor
5-HT Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
|
|
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
|
-
- HY-171317
-
|
|
Bacterial
|
Infection
|
|
SMARt751 targets the transcriptional regulatory factor VirS, inhibits its DNA binding ability, upregulates the mymA operon expression, thereby activating Ethionamide (HY-B0276), enhancing the antimicrobial activity of Ethionamide. SMARt751 enhances the antibacterial activity of Ethionamide against M. tuberculosis, reverses the Ethionamide resistance. SMARt751 improves the antibacterial effect of Ethionamide and reduces its effective dose in mouse models. SMARt751 can cross blood brain barrier .
|
-
- HY-N4190
-
|
1,6-O,O-Diacetylbritannilactone; Di-O-acetylbritannilactone
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC50 value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property .
|
-
- HY-B1715R
-
|
|
GABA Receptor
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
Oxiracetam (Standard) is the analytical standard of Oxiracetam. This product is intended for research and analytical applications. Oxiracetam (ISF2522) is an orally active and a BBB-penatrable cyclic derivative of γ-aminobutyric acid (GABA). Oxiracetam reaches the hippocampus and cerebral cortex in high concentrations. Oxiracetam can promote cognitive function and regulate inflammatory response, with powerful neuroprotective effects. Oxiracetam can be used in the study of central nervous system diseases .
|
-
- HY-13289B
-
|
(R)-SYN117 hydrochloride; (R)-RS-25560-197 hydrochloride; RS-25560-198 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
(R)-Nepicastat hydrochloride is the isomer of Nepicastat (HY-13289). Nepicastat (SYN117) is a selective，potent，and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB) .
|
-
- HY-137466
-
|
|
Topoisomerase
|
Cancer
|
|
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .
|
-
- HY-19939S
-
VX-984
4 Publications Verification
M9831
|
DNA-PK
|
Cancer
|
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
- HY-144272
-
-
- HY-A0031A
-
|
TSE-424 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .
|
-
- HY-N0408
-
-
- HY-D2268A
-
|
|
Amyloid-β
Fluorescent Dye
|
Neurological Disease
|
|
QM-FN-SO3 ammonium is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 ammonium can be used for in vivo detection of Aβ plaques. QM-FN-SO3 ammonium has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
|
-
- HY-149984
-
|
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-21 is an excellent MAO-B inhibitor with antioxidant activity and anti-Aβ aggregation activity. MAO-B-IN-21 also exhibits metal-ion chelating ability, anti-neuroinflammation (NO, TNF-α), neuroprotective activity and BBB permeability. MAO-B-IN-21 significantly improves the memory and cognitive impairment in Aβ1-42 induced Alzheimer's disease mice model .
|
-
- HY-B0410A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
|
-
- HY-170976
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-16 (Compound 6a) is an orally active, BBB-permeable, and selective BuChE inhibitor with an IC50 of 0.33 μM. BuChE-IN-16 has anti-inflammatory and neuroprotective effects. BuChE-IN-16 can improve the cognitive function of zebrafish with Alzheimer's disease (AD) and alleviate memory impairment in mice induced by Scopolamine (HY-N0296). BuChE-IN-16 can be used for the research of AD .
|
-
- HY-151886
-
|
|
PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
|
Neurological Disease
Cancer
|
|
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB) .
|
-
- HY-12153
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
JNJ-1930942 is a selective and blood-brain barrier (BBB) penetrant α(7) nAChR positive allosteric modulator.JNJ-1930942 enhances the Choline (HY-B0282)-evoked rise in intracellular Ca 2+ levels and neurotransmission at hippocampal dentate gyrus synapses. JNJ-1930942 reverses the naturally occurring sensory gating deficit in DBA/2 mice .
|
-
- HY-B0410
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
|
-
- HY-17355
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
|
-
- HY-B1102
-
|
Direct Blue 53; T-1824; C.I. 23860
|
EAAT
iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .
|
-
- HY-16785
-
|
INXN-1001; RG-115932
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys .
|
-
- HY-12678R
-
|
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-144607
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
|
-
- HY-B0602S3
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
|
-
- HY-B0602S2
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
|
-
- HY-160761
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
|
-
- HY-144825
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function .
|
-
- HY-13240A
-
|
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
|
-
- HY-160959
-
|
|
nAChR
|
Neurological Disease
|
|
AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
|
-
- HY-17573R
-
|
|
Oxytocin Receptor
|
Neurological Disease
Endocrinology
|
|
Carbetocin (Standard) is the analytical standard of Carbetocin. This product is intended for research and analytical applications. Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
|
-
- HY-17366A
-
|
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
|
-
- HY-17573A
-
|
|
Oxytocin Receptor
|
Neurological Disease
Endocrinology
|
|
Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
|
-
- HY-13821
-
|
BU-4061T
|
Proteasome
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity .
|
-
- HY-17573
-
|
|
Oxytocin Receptor
|
Neurological Disease
Endocrinology
|
|
Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
|
-
- HY-103493
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment .
|
-
- HY-116480
-
|
|
mAChR
|
Neurological Disease
|
|
LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC50 of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research .
|
-
- HY-17366AR
-
-
- HY-15978
-
|
|
Others
|
Neurological Disease
|
|
P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment .
|
-
- HY-102050
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .
|
-
- HY-13240
-
|
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
|
-
- HY-120511
-
KNT-127
1 Publications Verification
|
Opioid Receptor
|
Neurological Disease
|
|
KNT-127 is a potent δ-opioid receptor agonist that crosses the blood-brain barrier (BBB). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 has analgesic, antidepressant and antianxiety activities .
|
-
- HY-152671
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
|
-
- HY-17368S1
-
|
(Rac)-ENA 713-d6 free base; (Rac)-SDZ-ENA 713-d6 free base
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
|
Neurological Disease
|
|
(Rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
|
-
- HY-A0031R
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-152026
-
|
|
NADPH Oxidase
|
Neurological Disease
|
|
NADPH oxidase-IN-1 is an orally active NADPH oxidase (Nox) inhibitor, related with neuronal inflammation. NADPH oxidase-IN-1 can cross the blood-brain barrier (BBB), inhibits Nox2 and Nox4 with IC50s of 1.9 μM and 2.47 μM, respectively. NADPH oxidase-IN-1 suppresses pro-inflammatory cytokines production and LPS-mediated microglial migration, also has in vivo efficacy .
|
-
- HY-169731
-
-
- HY-146678
-
|
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity .
|
-
- HY-144828
-
|
|
RIP kinase
Mixed Lineage Kinase
Necroptosis
|
Cancer
|
|
RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability .
|
-
- HY-B0602R
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine (Standard) is the analytical standard of Desvenlafaxine. This product is intended for research and analytical applications. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-W654336
-
|
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
|
Neurological Disease
|
|
(S)-Rivastigmine-d4 is deuterium labeled Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
- HY-A0031S
-
|
TSE-424-d4
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
|
-
- HY-N2426R
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
Desvenlafaxine (Standard) is the analytical standard of Desvenlafaxine. This product is intended for research and analytical applications. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-149247
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability .
|
-
- HY-P5754
-
|
|
Apoptosis
|
Neurological Disease
|
|
TAT-NEP1-40 is a BBB-penatrable peptide. TAT-NEP1-40 protects PC12 cells against oxygen and glucose deprivation (OGD), and promotes neurite outgrowth. TAT-NEP1-40 also improves ischemia-induced neurologic outcomes by inhibiting cell apoptosis in ischemic brains. TAT-NEP1-40 can be used for research of CNS injuries, such as axonal regeneration and functional recovery after stroke .
|
-
- HY-147851
-
|
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent .
|
-
- HY-A0031S2
-
|
TSE-424-d4 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
|
-
- HY-146679
-
|
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity .
|
-
- HY-150702
-
|
|
MAGL
|
Neurological Disease
Inflammation/Immunology
|
|
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
|
-
- HY-B0410AR
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole (dihydrochloride hydrate) (Standard) is the analytical standard of Pramipexole (dihydrochloride hydrate). This product is intended for research and analytical applications. Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
|
-
- HY-17355S
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d7 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
- HY-B0410S1
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
|
-
- HY-P5754A
-
|
|
Apoptosis
|
Neurological Disease
|
|
TAT-NEP1-40 TFA is a BBB-penatrable peptide. TAT-NEP1-40 TFA protects PC12 cells against oxygen and glucose deprivation (OGD), and promotes neurite outgrowth. TAT-NEP1-40 TFA also improves ischemia-induced neurologic outcomes by inhibiting cell apoptosis in ischemic brains. TAT-NEP1-40 TFA can be used for research of CNS injuries, such as axonal regeneration and functional recovery after stroke .
|
-
- HY-15113
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
Y-29794 is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 penetrates the brain-blood barrier (BBB) .
|
-
- HY-162596
-
|
BA-1049
|
ROCK
|
Neurological Disease
|
|
NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice .
|
-
- HY-170417
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
hAChE/hBuChE/GSK-3β-IN-1 (Compound 6c) is a BBB-penatrable and multi-target anti-Alzheimer's disease compound. hAChE/hBuChE/GSK-3β-IN-1 is the inhibitors of hAChE (IC50: 28.88 nM), hBuChE (IC50: 131.90 nM) and GSK-3β (IC50: 51.42 nM). hAChE/hBuChE/GSK-3β-IN-1 is the tau and Aβ protein aggregation inhibitors .
|
-
- HY-15113A
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
|
Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB) .
|
-
- HY-N1501R
-
|
|
α-synuclein
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Beta-asarone (Standard) is the analytical standard of Beta-asarone. This product is intended for research and analytical applications. Beta-asarone is an orally active and BBB-penatrable anti-inflammatory agent and neuroprotective agent, which is the major ingredient of Acorus tatarinowii Schott. Beta-asarone can protect nerve cells from apoptosis and autophagy, inhibit expression of α-synuclein, as well as myocardial protection. Beta-asarone can be used in the study of neurological and cardiovascular diseases .
|
-
- HY-17412A
-
-
- HY-P5762A
-
|
PNX-14 TFA
|
GnRH Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Phoenixin-14 (PNX-14) TFA, a BBB-penatrable neuropeptide, has anxiolytic, cardioprotective and neuroprotective effect. Phoenixin-14 TFA can regulate pituitary gonadotrophin secretion by upregulating the GnRH receptor mRNA. Phoenixin-14 TFA stimulates insulin secretion. Phoenixin-14 TFA also protects mice from ischemia/reperfusion (IR) injury. PNX-14 TFA prevents oxidative stress by reducing ROS and increasing GSH .
|
-
- HY-17355S1
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d5 (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
- HY-B0410R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole (Standard) is the analytical standard of Pramipexole. This product is intended for research and analytical applications. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
|
-
- HY-162573
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 5 (Compound 16d) is a selective and reversible inhibitor for monoamine oxidase B (hMAO-B) with an IC50 of 67.3 nM and a Ki of 82.5 nM. Monoamine Oxidase B inhibitor 5 exhibits good pharmacokinetic characters and weak toxicity in rats model. Monoamine Oxidase B inhibitor 5 alleviates MPTP-induced (HY-15608) motor impairment in Parkinson’s mouse model. Monoamine Oxidase B inhibitor 5 is blood-brain barrier (BBB) penetrate .
|
-
- HY-17412
-
-
- HY-124959
-
|
U-62066 mesylate
|
Opioid Receptor
|
Neurological Disease
|
|
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-P4073
-
|
GRN1005; Paclitaxel trevatide
|
Peptide-Drug Conjugates (PDCs)
LDLR
|
Cancer
|
|
ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .
|
-
- HY-130795
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease .
|
-
- HY-N3187
-
-
- HY-106756
-
|
U-62066
|
Opioid Receptor
|
Neurological Disease
|
|
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-150794
-
|
|
Others
|
Cancer
|
|
FLDP-8 is a curcuminoid analogues, has potent anti-cancer effects. FLDP-8 can induce cell death with an IC50 value of 4 μM in LN-18 cells .
|
-
- HY-130252
-
YQ128
1 Publications Verification
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
|
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 μM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity . YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-124582
-
NEO214
1 Publications Verification
|
Autophagy
mTOR
|
Cancer
|
|
NEO214 is an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram (HY-16900) and perillyl alcohol (HY-N7000). It has anti-cancer activity and blood-brain barrier (BBB) permeability. Over sex. NEO214 prevents autophagy-lysosome fusion, thereby blocking autophagic flux and triggering glioma cell death. The process involves mTOR activation, andTFEB(Transcription Factor EB) aggregation. NEO214 inhibitionMacroautophagy/autophagy in glioblastoma cells has the potential to overcome chemotherapy resistance in glioblastoma .
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-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
|
-
- HY-11017R
-
|
ENA 713 (Standard); SDZ-ENA 713 (Standard)
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine (tartrate) (Standard) is the analytical standard of Rivastigmine (tartrate). This product is intended for research and analytical applications. Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
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-
- HY-161643
-
|
|
Cholinesterase (ChE)
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
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-
- HY-17355S2
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Pramipexole-d7-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
|
-
- HY-W654335
-
|
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine-d4 (tartrate) is deuterium labeled Rivastigmine (tartrate). Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
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-
- HY-147859
-
|
|
Amyloid-β
|
Neurological Disease
|
|
BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research .
|
-
- HY-12678S
-
|
NMS-E628-d4; RXDX-101-d4
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
Isotope-Labeled Compounds
|
Cancer
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-168859
-
|
|
JNK
GSK-3
Amyloid-β
|
Neurological Disease
|
|
JNK3 inhibitor-9 (Compound 24a) is a potent, selective and BBB-permeable JNK3 inhibitor with an IC50 value of 12 nM. JNK3 inhibitor-9 also potently inhibits GSK3α/β (IC50s: 14 and 35 nM, respectively) involved in Tau phosphorylation. JNK3 inhibitor-9 reduces c-Jun and APP phosphorylation. JNK3 inhibitor-9 protects neurons from Aβ1-42 toxicity .
|
-
- HY-W654013
-
|
|
Isotope-Labeled Compounds
Apoptosis
Potassium Channel
Antibiotic
Bacterial
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
Calcium Channel
|
Infection
|
|
Minocycline-d7 is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
|
-
- HY-163288
-
|
|
Histone Methyltransferase
HSP
Apoptosis
|
Cancer
|
|
EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB) .
|
-
- HY-146691
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-138669
-
|
|
PROTACs
Tau Protein
|
Neurological Disease
|
|
C004019 is a BBB-penatrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases. (Pink: Ligand for target protein (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))
|
-
- HY-109968A
-
|
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-110291
-
|
|
LPL Receptor
|
Neurological Disease
|
|
A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC50s of .362, >10, 0.006 μM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis .
|
-
- HY-168241
-
|
|
Cholinesterase (ChE)
5-HT Receptor
|
Infection
|
|
Flucopride (Compound 4a) is an AChE inhibitor (IC50: 24 nM), and a partial 5-HT4R agonist (Ki: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT4R (EC50: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay) .
|
-
- HY-17412R
-
-
- HY-109968
-
|
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-P0299
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .
|
-
- HY-143264
-
|
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment .
|
-
- HY-P0299A
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .
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-
- HY-162373
-
|
|
Amylases
Glycosidase
P-glycoprotein
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-10 (compound 5d) is an α-amylase and α-glucosidase inhibitor (IC50: 30.39 μM and 65.1 μM) with potential diabetes inhibitory effects. α-Amylase/α-Glucosidase-IN-10 exhibits high gastrointestinal (GI) absorption in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) prediction. While α-Amylase/α-Glucosidase-IN-10 acts as a substrate for P-gp and does not cross the blood-brain barrier (BBB), there may be a risk of central nervous system side effects .
|
-
- HY-170994
-
|
|
Imidazoline Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
I2-IRs ligand-1 (Compound 12d) is an orally active and BBB-penatrable compound. I2-IRs ligand-1 has a high affinity for imidazoline I2 receptors (I2-IRs) (pKi: 9.98). I2-IRs ligand-1 can improve cognitive impairment in senescent mice and exhibits analgesic, anti-inflammatory, and neuroprotective activities. I2-IRs ligand-1 can be used for the research of Alzheimer's disease and related pain disorders .
|
-
- HY-149090
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BuChE/MAO-B-IN-2 (compound 4b) is a potent AChE/BuChE inhibitor and showed good blood brain barrier (BBB) permeability in vitro with an IC50 value of 5.3 μM, 12.4 μM, 1.9±0.08 μM, for AChE, BuChE, huMAO-B, respectively. AChE/BuChE/MAO-B-IN-2 (compound 4b) can inhibit excess AChE/BuChE in Alzheimer's disease (AD) brain. AChE/BuChE/MAO-B-IN-2 (compound 4b) can be used in anti-Alzheimer's research .
|
-
- HY-124475
-
|
|
CRFR
|
Neurological Disease
|
|
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier .
|
-
- HY-128463
-
|
|
COX
Reactive Oxygen Species
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier .
|
-
- HY-B0007S2
-
|
|
GABA Receptor
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Baclofen-d5 hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
|
-
- HY-B0007S
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen-d4 is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].
|
-
- HY-135749
-
|
|
IGF-1R
|
Neurological Disease
Inflammation/Immunology
|
|
BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects .
|
-
- HY-19918A
-
|
|
NF-κB
Amyloid-β
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
|
-
- HY-B0007
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
|
-
- HY-121618
-
|
|
GABA Receptor
Reactive Oxygen Species
Parasite
Apoptosis
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier .
|
-
- HY-170409
-
|
|
Trk Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable .
|
-
- HY-125469
-
|
PF-04895162
|
Potassium Channel
|
Neurological Disease
|
|
ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects .
|
-
- HY-B0007C
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research .
|
-
- HY-144790
-
|
|
Amyloid-β
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu 2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease .
|
-
- HY-161925
-
|
|
TGF-β Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
sTGFBR3 antagonist 1 (Compound p24) is an antagonist for soluble transforming growth factor beta receptor 3 (sTGFBR3), thus activates TGF-β signaling pathway, and inhibits IκBα/NF-κB signaling pathway. sTGFBR3 antagonist 1 inhibits NO-release in LPS (HY-D1056) -induced BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities with blood brain barrier (BBB) permeability. sTGFBR3 antagonist 1 can be used in Alzheimer’s Disease research .
|
-
- HY-A0168S
-
|
CVT-3146-d3
|
Adenosine Receptor
|
Cardiovascular Disease
Cancer
|
|
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
|
-
- HY-146314
-
|
|
Monoamine Oxidase
Amyloid-β
|
Neurological Disease
|
|
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-161783
-
|
|
HDAC
Keap1-Nrf2
Reactive Oxygen Species
Apoptosis
|
Neurological Disease
|
|
HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability .
|
-
- HY-139604
-
|
|
MARK
Apoptosis
|
Cancer
|
|
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability .
|
-
- HY-N0408R
-
|
|
NF-κB
Reactive Oxygen Species
Apoptosis
Influenza Virus
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Picroside II (Standard) is the analytical standard of Picroside II. This product is intended for research and analytical applications. Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities.
picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways .
Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities .
|
-
- HY-124832
-
|
|
Caspase
Amyloid-β
|
Neurological Disease
|
|
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
|
-
- HY-151389
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease .
|
-
- HY-155330
-
|
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
PZ-1922 (Compound 16) is a BBB-penetrable 5-HT6R/5-HT3R antagonist (Ki: 17 nM, 0.45 nM for 5-HT6R/5-HT3R respectively). PZ-1922 reversibly inhibits MAO-B (pIC50: 8.93). PZ-1922 reverses Scopolamine (SCOP) (HY-N0296) induced memory deficits in the novel object recognition (NOR) test in rats. PZ-1922 prevents Aβ-induced memory decline in the T-maze test .
|
-
- HY-155330A
-
|
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
PZ-1922 free base is a BBB-penetrable 5-HT6R/5-HT3R antagonist (Ki: 17 nM, 0.45 nM for 5-HT6R/5-HT3R respectively). PZ-1922 free base reversibly inhibits MAO-B (pIC50: 8.93). PZ-1922 free base reverses Scopolamine (SCOP) (HY-N0296) induced memory deficits in the novel object recognition (NOR) test in rats. PZ-1922 free base prevents Aβ-induced memory decline in the T-maze test .
|
-
- HY-P99530
-
|
AGT-181; HIRMAb-IDUA
|
Insulin Receptor
|
Metabolic Disease
|
|
Valanafusp alfa (AGT-181) is a chimeric monoclonal antibody that fuses human α-L-iduronidase (IDUA) and targets the human insulin receptor (HIR). Valanafusp alfa has brain penetrating properties, making it useful for research on mucopolysaccharidosis type I (MPS I) .
|
-
- HY-B1080R
-
|
|
HIF/HIF Prolyl-Hydroxylase
Influenza Virus
|
Infection
Neurological Disease
|
|
Tilorone (dihydrochloride) (Standard) is the analytical standard of Tilorone (dihydrochloride). This product is intended for research and analytical applications. Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV) .
|
-
- HY-B1080
-
|
|
HIF/HIF Prolyl-Hydroxylase
Influenza Virus
|
Infection
Neurological Disease
|
|
Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV) .
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-
- HY-131688R
-
|
|
PARP
Caspase
|
Inflammation/Immunology
|
|
Neomycin (sulfate) (Standard) is the analytical standard of Neomycin (sulfate). This product is intended for research and analytical applications. Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis .
|
-
- HY-153321
-
|
BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
|
-
- HY-150537
-
|
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
|
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-159941
-
|
|
α-synuclein
|
Neurological Disease
|
|
tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice .
|
-
- HY-13488
-
|
|
LRRK2
MNK
|
Neurological Disease
|
|
HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research .
|
-
- HY-D0186R
-
|
|
Endogenous Metabolite
Thymidylate Synthase
|
Infection
|
2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
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-
-
-
HY-L0123V
-
|
|
30,300 compounds
|
|
The incidence and significance of central nervous system diseases are increasing at an alarming rate all over the world. Although substantial research efforts have been applied to develop new CNS-active drugs, only a few CNS disorders are addressed satisfactorily, while the remaining ones pose significant clinical challenges. Blood-brain barrier (BBB) permeability is one of the most important limiting factors in the design and development of novel CNS-targeted pharmaceuticals for the treatment of neurological disorders.
Carefully selected from the HTS Compound Collection to meet the parameters optimized for high BBB-permeability, our CNS Focused Screening Library comprising over 30,300 structurally-diverse and potentially CNS-active screening compounds. This original Screening Compound Library is aimed at supporting CNS drug design projects and HTS efforts in search for novel neurotherapeutics.
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-
-
HY-L028
-
|
|
927 compounds
|
|
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.
MCE offers a unique collection of 927 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.
|
| Cat. No. |
Product Name |
Type |
-
- HY-128868G
-
|
|
Fluorescent Dyes/Probes
|
|
FITC-Dextran (MW 150000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=491 nm; Em=518 nm). FITC-Dextran (MW 150000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 150000) can be used in perfusion studies in animals or in fluorescence microlymphography, to study processes that affect the permeability of the blood brain barrier (BBB) . FITC-Dextran (MW 150000) can be used as fluorescent probe to study cell permeability .
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-
- HY-128868D
-
|
|
Fluorescent Dyes/Probes
|
|
FITC-Dextran (MW 40000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 40000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 40000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption .
|
-
- HY-128868
-
|
|
Fluorescent Dyes/Probes
|
|
FITC-Dextran (MW 10000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 10000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 10000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption .
|
-
- HY-128868A
-
|
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Fluorescent Dyes/Probes
|
|
FITC-Dextran (MW 4000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 4000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 4000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption .
|
-
- HY-D2343
-
|
|
Dyes
|
|
PB0822 can be used for in vivo PET imaging when labeled with [ 18F]fluoride. [ 18F]PB0822 is a PET radioligand. [ 18F]PB0822 has a cLogP value of 1.54, which is a good predictive index for BBB penetration. [ 18F]PB0822 can be used for Alzheimer’s Disease research .
|
-
- HY-151615
-
|
|
Fluorescent Dyes/Probes
|
|
DCI-Br-3 is a rapid, highly sensitive, and selective probe to monitor thiols in the epileptic brain. (λex=537 nm, λem=675 nm).DCI-Br-3 can effectively cross the blood-brain barrier (BBB) .
|
-
- HY-D1672
-
|
|
Fluorescent Dyes/Probes
|
|
TMR Biocytin is a polar tracer used in the research of cell-cell and cell-liposome fusions, as well as membrane permeability and cellular uptake during pinocytosis. TMR Biocytin can be detected using streptavidin, and is an effective neuronal tracer in live tissue (Ex=544 nm, Em=571 nm) .
|
-
- HY-D2268
-
|
|
Fluorescent Dyes/Probes
|
|
QM-FN-SO3 is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 can be used for in vivo detection of Aβ plaques. QM-FN-SO3 has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
|
-
- HY-D2268A
-
|
|
Fluorescent Dyes/Probes
|
|
QM-FN-SO3 ammonium is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 ammonium can be used for in vivo detection of Aβ plaques. QM-FN-SO3 ammonium has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
|
| Cat. No. |
Product Name |
Type |
-
- HY-137499
-
|
|
Drug Delivery
|
|
NT1-O12B, an endogenous chemical and a neurotransmitter-derived lipidoid (NT-lipidoid), is an effective carrier for enhanced brain delivery of several blood-brain barrier (BBB)-impermeable cargos. Doping NT1-O12B into BBB-impermeable lipid nanoparticles (LNPs) gives the LNPs the ability to cross the BBB. NT-lipidoids formulation not only facilitate cargo crossing of the BBB, but also delivery of the cargo into neuronal cells for functional gene silencing or gene recombination .
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-
- HY-137500
-
|
|
Drug Delivery
|
|
NT1-014B is a potent NT1-lipidoid encapsulated AmB (amphotericin B). NT1-014B dopes the NT-lipidoids into BBB-impermeable lipid nanoparticles (LNPs) gave the LNPs the ability to cross the BBB. NT1-014B enhances brain delivery through intravenous injection .
|
-
- HY-B1102
-
|
Direct Blue 53; T-1824; C.I. 23860
|
Cell Assay Reagents
|
|
Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-105155
-
|
RMP 7
|
Bradykinin Receptor
|
Cancer
|
|
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
|
-
- HY-P10235
-
|
|
Amylin Receptor
|
Neurological Disease
|
|
Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
|
-
- HY-P2297
-
-
- HY-P2297A
-
-
- HY-P0285
-
|
|
RABV
|
Infection
|
|
Rabies Virus Glycoprotein is a 29-amino-acid cell penetrating peptide derived from a rabies virus glycoprotein that can cross the blood-brain barrier (BBB) and enter brain cells.
|
-
- HY-P1178A
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B TFA inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B TFA has analgesic and anxiolytic effects .
|
-
- HY-P10502
-
|
|
LDLR
|
Others
|
|
L57 exhibits high affinity to the low-density lipoprotein receptor-related protein 1 (LRP1) with Ki of 45 nM. L57 exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 can be utilized as the carrier for CNS drug delivery .
|
-
- HY-149941
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
|
-
- HY-P2342
-
-
- HY-P10777
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
ANG1009 is a BBB-penatrable anticancer agent. ANG1009 is cytotoxic to a variety of tumor cells and can induce cell cycle arrest. ANG1009 can be used in the study of brain cancer .
|
-
- HY-P0285A
-
|
|
RABV
|
Infection
|
|
Rabies Virus Glycoprotein (TFA) is a 29-amino-acid cell penetrating peptide derived from a rabies virus glycoprotein that can cross the blood-brain barrier (BBB) and enter brain cells .
|
-
- HY-P10911
-
|
|
LDLR
|
Others
|
|
IETP2 targets low-density lipoprotein receptor-related protein 1 (LRP1) with a KD of 738 nM and can be used for drug- and imaging agents delivery across the blood-labyrinth barrier (BLB) .
|
-
- HY-P1178
-
|
|
Trk Receptor
p38 MAPK
|
Neurological Disease
|
|
Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects .
|
-
- HY-P10310
-
|
|
HIV
|
Infection
|
|
F9170 is an amphipathic peptide with an activity of inactivate HIV-1 virions. F9170 targets the conserved cytoplasmic tail of HIV-1 env and disrupts the integrity of the viral membrane. F9170 is able to cross the blood-brain barrier (BBB) .
|
-
- HY-P10359
-
|
|
TGF-beta/Smad
MMP
|
Neurological Disease
|
|
TAT-QFNP12 is a peptide that blocks the NDRG2-PPM1A binding and reduces Smad2/3 phosphorylation, decreases astrocytic MMP-9 production and BBB disruption after subarachnoid hemorrhage (SAH) .
|
-
- HY-P3895
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
Substance P (3-11) is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) has contracting activities on guinea pig ileum. Substance P (3-11) also promotes human monocyte chemotaxis .
|
-
- HY-P10782
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
|
Pt(IV)-M13 is a BBB-penatrable Platinum (IV) prodrug-perfluoroaryl macrocyclic peptide conjugate. Pt(IV)-M13 is cytotoxic to glioma stem cells and increases uptake of platinum in the brain. Pt(IV)-M13 can be used in the study of glioblastoma .
|
-
- HY-P10822
-
|
|
Caspase
|
Neurological Disease
|
|
ED11 is a potent and selective caspase-6 inhibitor with an IC50 of 12.12 nM. ED11 competes with Htt for the caspase-6 active site, and thus reduce Htt cleavage. ED11 can cross the blood-brain barrier (BBB). ED11 has the potential for the study of Huntington's disease (HD) .
|
-
- HY-P3223
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-P2343
-
|
|
Apoptosis
|
Cancer
|
|
BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian .
|
-
- HY-P10861
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 is an orally active and a BBB-penatrable Tau aggregation peptide inhibitor. RI-AG03 inhibits Tau aggregation and improves associated neurodegeneration and behavioral phenotypes in both in vivo and in vitro models. RI-AG03 can be used in the study of tauopathies such as Alzheimer's disease .
|
-
- HY-P1335
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-107663
-
|
Pro-Leu-Gly-NH2; Melanostatin
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-P1335A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
|
-
- HY-P10153
-
|
|
Peptides
|
Others
|
|
gH625 is a cell-penetrating viral peptide which is a part of glycoprotein H of Herpes simplex virus type I. gH625 is able to cross the cell membrane and to transport many conjugated cargoes into the cytosol. gH625 is permeable to the blood-brain barrier (BBB) and can enter the rat brain in vivo without toxic effects. gH625 can be used for siRNA delivery research .
|
-
- HY-107663A
-
|
Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
|
Dopamine Receptor
|
Neurological Disease
|
|
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-17573R
-
|
|
Oxytocin Receptor
|
Neurological Disease
Endocrinology
|
|
Carbetocin (Standard) is the analytical standard of Carbetocin. This product is intended for research and analytical applications. Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
|
-
- HY-17573A
-
|
|
Oxytocin Receptor
|
Neurological Disease
Endocrinology
|
|
Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
|
-
- HY-17573
-
|
|
Oxytocin Receptor
|
Neurological Disease
Endocrinology
|
|
Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
|
-
- HY-P5754
-
|
|
Apoptosis
|
Neurological Disease
|
|
TAT-NEP1-40 is a BBB-penatrable peptide. TAT-NEP1-40 protects PC12 cells against oxygen and glucose deprivation (OGD), and promotes neurite outgrowth. TAT-NEP1-40 also improves ischemia-induced neurologic outcomes by inhibiting cell apoptosis in ischemic brains. TAT-NEP1-40 can be used for research of CNS injuries, such as axonal regeneration and functional recovery after stroke .
|
-
- HY-P5754A
-
|
|
Apoptosis
|
Neurological Disease
|
|
TAT-NEP1-40 TFA is a BBB-penatrable peptide. TAT-NEP1-40 TFA protects PC12 cells against oxygen and glucose deprivation (OGD), and promotes neurite outgrowth. TAT-NEP1-40 TFA also improves ischemia-induced neurologic outcomes by inhibiting cell apoptosis in ischemic brains. TAT-NEP1-40 TFA can be used for research of CNS injuries, such as axonal regeneration and functional recovery after stroke .
|
-
- HY-P5762A
-
|
PNX-14 TFA
|
GnRH Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Phoenixin-14 (PNX-14) TFA, a BBB-penatrable neuropeptide, has anxiolytic, cardioprotective and neuroprotective effect. Phoenixin-14 TFA can regulate pituitary gonadotrophin secretion by upregulating the GnRH receptor mRNA. Phoenixin-14 TFA stimulates insulin secretion. Phoenixin-14 TFA also protects mice from ischemia/reperfusion (IR) injury. PNX-14 TFA prevents oxidative stress by reducing ROS and increasing GSH .
|
-
- HY-P4073
-
|
GRN1005; Paclitaxel trevatide
|
Peptide-Drug Conjugates (PDCs)
LDLR
|
Cancer
|
|
ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .
|
-
- HY-P0299
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .
|
-
- HY-P0299A
-
|
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99403
-
|
GSK249320
|
Inhibitory Antibodies
|
Neurological Disease
|
|
Refanezumab (GSK249320) is an IgG1-type humanized monoclonal antibody directed against myelin-associated glycoprotein (MAG). Refanezumab binds to MAG and blocks MAG-mediated inhibition of axonal regeneration. Refanezumab can cross the blood-brain barrier (BBB) in animal stroke models. Refanezumab has the potential for the enhancement of recovery of function poststroke .
|
-
- HY-108801A
-
|
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease .
|
-
- HY-P99530
-
|
AGT-181; HIRMAb-IDUA
|
Insulin Receptor
|
Metabolic Disease
|
|
Valanafusp alfa (AGT-181) is a chimeric monoclonal antibody that fuses human α-L-iduronidase (IDUA) and targets the human insulin receptor (HIR). Valanafusp alfa has brain penetrating properties, making it useful for research on mucopolysaccharidosis type I (MPS I) .
|
-
- HY-P99694
-
|
JR-171
|
Transferrin Receptor
|
Neurological Disease
|
|
Lepunafusp alfa (JR-171) is a BBB-penetrable fusion protein consisting of J-Brain Cargo and IDUA (a lysosomal enzyme, α-L-iduronidase). Lepunafusp alfa can reduce concentration of heparan sulfate (HS) and dermatan sulfate (DS). Lepunafusp alfa can be used for research of mucopolysaccharidosis type I .
|
-
- HY-108801
-
|
VEGF Trap; VEGF-TRAPR1R2; VEGF-trapR1
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Aflibercept (VEGF Trap) is a soluble decoy VEGFR constructed by fusing the Ig domains of VEGFR1 and VEGFR2 with the Fc region of human IgG1. Aflibercept inhibits VEGF signaling by reducing VEGF-regulated processes. Aflibercept can be used for thr research of age-related macular degeneration (AMD) and cardiovascular disease .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-137499
-
-
-
- HY-N9343
-
-
-
- HY-B0303A
-
-
-
- HY-P0285
-
-
-
- HY-B0303
-
-
-
- HY-N9038
-
-
-
- HY-N6685
-
-
-
- HY-N12171
-
-
-
- HY-N6685R
-
-
-
- HY-B0303R
-
-
-
- HY-N7109
-
-
-
- HY-N7109B
-
-
-
- HY-N4134
-
-
-
- HY-N7109R
-
-
-
- HY-N1501
-
-
-
- HY-N0408
-
-
-
- HY-13821
-
-
-
- HY-N2426R
-
|
|
Clerodendrum trichotomum Thunb.
Structural Classification
Flavonoids
Verbenaceae
Plants
Isoflavones
|
Interleukin Related
|
|
Desvenlafaxine (Standard) is the analytical standard of Desvenlafaxine. This product is intended for research and analytical applications. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
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-
-
- HY-N1501R
-
-
-
- HY-N3187
-
-
-
- HY-121618
-
-
-
- HY-N0408R
-
|
|
Structural Classification
Iridoids
Terpenoids
Scrophulariaceae
Plants
Picrorhiza scrophulariiflora Pennell
|
NF-κB
Reactive Oxygen Species
Apoptosis
Influenza Virus
|
|
Picroside II (Standard) is the analytical standard of Picroside II. This product is intended for research and analytical applications. Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities.
picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways .
Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities .
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-
-
- HY-D0186R
-
|
|
Structural Classification
Natural Products
Immune System Disorder
Microorganisms
Source classification
Disease markers
Endogenous metabolite
|
Endogenous Metabolite
Thymidylate Synthase
|
2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
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-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0303AS1
-
|
|
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Diphenhydramine-d5 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].
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-
-
- HY-B0303AS
-
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|
Diphenhydramine-d6 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].
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-
-
- HY-N6685S1
-
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|
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3-Acetyldeoxynivalenol- 13C17 is the 13C labeled 3-Acetyldeoxynivalenol (HY-N6685) . 3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative , is a blood-brain barrier (BBB) permeable mycotoxin .
|
-
-
- HY-19939S
-
4 Publications Verification
|
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VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
-
- HY-109502S
-
|
|
|
10-OH-NBP-d4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research[1].
|
-
-
- HY-17368S2
-
|
|
|
Rivastigmine-d3 hydrochloride is deuterated labeled Rivastigmine (HY-17368). Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
-
- HY-159578S
-
|
|
|
VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
|
-
-
- HY-B2150S
-
|
|
|
4-Hydroxyantipyrine-d3 is the deuterium labeled 4-Hydroxyantipyrine. 4-Hydroxyantipyrine is the major metabolite of Antipyrine, can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Antipyrine in the brain[1][2][3].
|
-
-
- HY-170905S
-
|
|
|
MAT2A-IN-22 (Compound 29-1) is a BBB-penatrable and orally active MAT2A inhibitor with an IC50 of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects .
|
-
-
- HY-117727S
-
|
|
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penatrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
|
-
-
- HY-B0602S3
-
|
|
|
Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
|
-
-
- HY-B0602S2
-
|
|
|
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
|
-
-
- HY-17368S1
-
|
|
|
(Rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
|
-
-
- HY-W654336
-
|
|
|
(S)-Rivastigmine-d4 is deuterium labeled Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
-
- HY-A0031S
-
|
|
|
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
|
-
-
- HY-A0031S2
-
|
|
|
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
|
-
-
- HY-17355S
-
|
|
|
Pramipexole-d7 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
-
- HY-B0410S1
-
|
|
|
Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
|
-
-
- HY-17355S1
-
|
|
|
Pramipexole-d5 (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
|
-
-
- HY-17355S2
-
|
|
|
Pramipexole-d7-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
|
-
-
- HY-W654335
-
|
|
|
Rivastigmine-d4 (tartrate) is deuterium labeled Rivastigmine (tartrate). Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
|
-
-
- HY-12678S
-
|
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
-
- HY-W654013
-
|
|
|
Minocycline-d7 is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
|
-
-
- HY-B0007S2
-
|
|
|
Baclofen-d5 hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .
|
-
-
- HY-B0007S
-
|
|
|
Baclofen-d4 is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].
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-
-
- HY-A0168S
-
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|
|
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-151657
-
|
|
|
Azide
|
|
Spermine(N3BBB) is a click chemistry reagent containing an azide group and can be used for various biochemical studies . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
|
-
- HY-130252
-
YQ128
1 Publications Verification
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|
Alkynes
|
|
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 μM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity . YQ128 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146314
-
|
|
|
Alkynes
|
|
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-159578S
-
|
|
|
Azide
|
|
VU6036864 (compound 45) is an orally active, selective mAChR M5 antagonist with IC50=20 nM for human M5. VU6036864 is >500-fold selective for human M1-4, with BBB characteristic and high oral bioavailability (%F>100%) .
|
-
- HY-153831
-
|
|
|
Alkynes
|
|
c-Met-IN-17 is a potent c-Met kinase inhibitor with an IC50 of 0.031 μM. c-Met-IN-17 can be used in anticancer research. . c-Met-IN-17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146691
-
|
|
|
Alkynes
|
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-137501
-
|
|
|
Cationic Lipids
|
|
306-O12B-3 is a lipidoid that can efficiently deliver ASO both in vitro and in vivo. 306-O12B-3 is used to transport small molecule drugs across the blood-brain barrier (BBB) .
|
-
- HY-137499
-
|
|
|
Cationic Lipids
|
|
NT1-O12B, an endogenous chemical and a neurotransmitter-derived lipidoid (NT-lipidoid), is an effective carrier for enhanced brain delivery of several blood-brain barrier (BBB)-impermeable cargos. Doping NT1-O12B into BBB-impermeable lipid nanoparticles (LNPs) gives the LNPs the ability to cross the BBB. NT-lipidoids formulation not only facilitate cargo crossing of the BBB, but also delivery of the cargo into neuronal cells for functional gene silencing or gene recombination .
|
-
- HY-137500
-
|
|
|
Cationic Lipids
|
|
NT1-014B is a potent NT1-lipidoid encapsulated AmB (amphotericin B). NT1-014B dopes the NT-lipidoids into BBB-impermeable lipid nanoparticles (LNPs) gave the LNPs the ability to cross the BBB. NT1-014B enhances brain delivery through intravenous injection .
|
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