Search Result
Results for "
Blood-brain barrier permeability
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-128868
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Fluorescent Dye
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Others
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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 .
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- HY-128868A
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Fluorescent Dye
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Others
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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 .
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- HY-128868D
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Fluorescent Dye
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Others
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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 .
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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-14160
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- HY-161899
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MCHR1 (GPR24)
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Others
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MCHR1 antagonist 4 (Compound 2m) is a blood-brain barrier permeable MCHR1 antagonist with Ki values of 0.74 nM and 0.76 nM for hMCHR1 and rMCHR1, respectively. MCHR1 antagonist 4 is also an effective anti-obesity agent .
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- HY-157466
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Parasite
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Infection
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Antiparasitic agent-21 (compound 28) has selectively antiparasitic activity against Naegleria fowleri with an EC50 of 0.92 μM. Antiparasitic agent-21 has excellent blood-brain barrier permeability .
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- HY-155939
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TGF-β Receptor
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Cancer
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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) .
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- HY-155733
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iGluR
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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AChE/Aβ-IN-1 (compound 32) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 86 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 3.876 μM. AChE/Aβ-IN-1 also inhibits Aβ aggregation and shows good blood-brain barrier permeability and neuroprotection. AChE/Aβ-IN-1 improves cognitive and spatial memory impairment in rats model .
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- HY-155735
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iGluR
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model .
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- HY-12354
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MMP
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Cancer
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SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity .
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- HY-18738
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Ammonium pyrrolidinedithiocarbamate; PDTC ammonium; APDC
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NF-κB
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Inflammation/Immunology
Cancer
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Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate) is a selective and blood-brain barrier (BBB) permeable NF-κB inhibitor.
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- HY-11054
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meso-GS 164
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Others
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Neurological Disease
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TH-237A(meso-GS 164) is a neuroprotective agent with good blood-brain barrier permeability.
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- HY-N6685
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Others
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Cardiovascular Disease
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3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative , is a blood-brain barrier (BBB) permeable mycotoxin .
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- HY-126899
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Microtubule/Tubulin
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Cancer
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TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain .
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- HY-162117
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mGluR
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Neurological Disease
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LBG30300 is a subtype-selective mGlu2 receptor agonist EC50 0.6 nM. LBG30300 is blood-brain barrier permeable .
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- HY-N2332A
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MLA
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nAChR
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Neurological Disease
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Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR) with blood-brain barrier permeability.
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- HY-154959
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Ras
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Cancer
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AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS G12C inhibitor. AZD4747 has the potential to study cancer .
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- HY-120332
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KH176 hydrochloride
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Reactive Oxygen Species
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Metabolic Disease
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Sonlicromanol (KH176) hydrochloride, a chemical entity derivative of Trolox, is a blood-brain barrier permeable ROS-redox modulator. Sonlicromanol (KH176) hydrochloride is used in the study for mitochondrial disorders .
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- HY-158765
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Others
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Neurological Disease
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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) .
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- HY-P4989
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Biochemical Assay Reagents
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Infection
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Type A Allatostatin III (allatostatin 3) is a blood-brain barrier permeable and reversible neuropeptide that inhibits hormone synthesis in juvenile female cockroaches. Type A Allatostatin III can be used in pesticide research .
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- HY-158693
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Sigma Receptor
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Neurological Disease
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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 .
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- HY-128868B
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Biochemical Assay Reagents
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Others
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FITC-Dextran (MW 3000-5000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 3000-5000) 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 3000-5000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption . Storage: protect from light.
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- HY-111653
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CycLuc1
2 Publications Verification
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Reactive Oxygen Species
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Others
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CycLuc1 is a blood-brain barrier permeable luciferase substrate that displays near-infrared (NIR) emission with a peak luminescence wavelength of 599 nm. CycLuc1 can be used for in vivo bioluminescence imaging .
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- HY-155086
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Cholinesterase (ChE)
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Neurological Disease
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hAChE-IN-4 (Compd 5d) is a potent, blood-brain barrier-permeable hAChE inhibitor with IC50 of 0.25 μM. hAChE-IN-4 can be used in Alzheimer's disease research .
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- HY-12936
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DNA/RNA Synthesis
Parasite
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Infection
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DDD100097 is a potent acyltransferase (TbNMT) inhibitor with an IC50 value of 2 nM. DDD100097 can significantly improve blood-brain barrier permeability. DDD100097 can be used in the study of African trypanosomiasis .
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- HY-112906
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STING
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Inflammation/Immunology
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C-176 is a selective and blood-brain barrier permeable STING inhibitor. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING .
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- HY-161307
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HDAC
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Neurological Disease
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T-518 is an orally active, selective, and blood-brain barrier permeable HDAC6 inhibitor with an IC50 value of 36 nM for human HDAC6. T-581 can be used in research on tauopathy .
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- HY-161163
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AMPK
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Neurological Disease
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IND 1316 is an orally active, blood-brain barrier permeable AMPK activator with neuroprotective effects in animal models of Huntington's disease. IND 1316 can be used for research on neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease .
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- HY-160791
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Others
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Infection
Cancer
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Claramine is a steroid polyamine with blood-brain barrier permeability. Claramine can regulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and biological protein-based toxins .
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- HY-161683
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JAK
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Neurological Disease
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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 .
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- HY-162920
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Aminopeptidase
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Cardiovascular Disease
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QGC583 is an effective selective Aminopeptidase A (APA) inhibitor with oral activity and blood-brain barrier permeability, boasting an IC50 value of 4 nM. QGC583 can inhibit APA activity in the brain, kidneys, and heart of rats .
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- HY-109061
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YH25448; GNS-1480
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EGFR
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Cancer
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Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer .
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- HY-157430
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Epigenetic Reader Domain
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Neurological Disease
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BET-IN-21 (compound 16) is a blood-brain barrier-permeable extra terminal domain (BET) inhibitor with the Ki of 230 nM. BET-IN-21 inhibits microglia activation and has ameliorative effects on experimental autoimmune encephalomyelitis mice .
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- HY-162821
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Others
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Neurological Disease
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IP6K-IN-2 (compound 29c) is an orally bioavailable and blood-brain barrier permeable IP6K inhibitor (IC50: 15.8 nM) that can be used in the study of central nervous system diseases .
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- HY-N6685R
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Others
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Cardiovascular Disease
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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 .
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- HY-125017
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PLB-1001; CBT-101; Vebreltinib
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c-Met/HGFR
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Cancer
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Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily .
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- HY-18236
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Calpain Inhibitor III
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Proteasome
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Neurological Disease
Inflammation/Immunology
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MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration . MDL-28170 also block γ-secretase .
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- HY-N6685S1
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Isotope-Labeled Compounds
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Cardiovascular Disease
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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 .
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- HY-152141
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Carbonic Anhydrase
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Others
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hCAII-IN-9 is a potent carbonic anhydrase inhibitor with IC50s of 1.18 μM (hCA II), 0.17 μM (hCA IX), and 2.99 μM (hCA XII), respectively. hCAII-IN-9 has no blood-brain barrier permeability .
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- HY-149212
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Cholinesterase (ChE)
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Neurological Disease
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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 .
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- HY-153715
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Mitochondria modulator-1
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Biochemical Assay Reagents
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Metabolic Disease
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Mitochondria modulator-1 is a mitochondrial regulator that stimulates mitochondrial ATP production. Mitochondria modulator-1 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. Mitochondria modulator-1 has the potential to study mitochondrial diseases .
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- HY-160168
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- HY-161380
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Fungal
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Infection
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Antifungal agent 96 (Compound WZ-2) is an antifungal agent with good blood-brain barrier permeability and brain penetration. Antifungal agent 96 inhibits the growth of C. neoformans H99 and C. albicans 0304103 with MIC values of 0.016 and 32 μg/mL, respectively .
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- HY-162693
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-68 (compound 2l) is a potent and selective AChE inhibitor, with an IC50 value of 0.040 μM. AChE-IN-68 has high blood-brain barrier permeability. AChE-IN-68 can be used for the research of neurodegenerative disorders, particularly Alzheimer’s disease .
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- HY-154959A
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Others
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Cancer
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(9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRAS G12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer .
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- HY-167702
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Others
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Neurological Disease
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(Rac)-Acetoxyvalerenic acid is a derivative of valerenic acid that acts as a GABA (A) receptor modulator, potentially providing sedative and sleep-enhancing effects. (Rac)-Acetoxyvalerenic acid exhibits slower permeability across the blood-brain barrier compared to diazepam, indicating that its transport may rely on an unidentified pathway rather than transcellular passive diffusion.
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- HY-14197
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M&B 9302
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Monoamine Oxidase
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Neurological Disease
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Clorgyline (M&B 9302) is an orally active, blood-brain barrier permeable and selective monoamine oxidase A (MAO-A) inhibitor. Clorgyline's selective inhibition of MAO-A leads to reduced metabolism of neurotransmitters such as serotonin (5-hydroxytryptamine), which accumulates in the brain. Clorgyline can be used in the study of depression and neurodegenerative diseases .
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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-161666
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- HY-120741
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Phosphodiesterase (PDE)
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Neurological Disease
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PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC50 values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease .
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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-146762
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- HY-156432
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Anaplastic lymphoma kinase (ALK)
mTOR
PARP
Caspase
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Cancer
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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 .
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- HY-159480
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Src
ATM/ATR
Apoptosis
mTOR
AMPK
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Cancer
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AD1058 is an orally active, selective, and blood-brain barrier permeable inhibitor of ATR. AD1058 exhibits in vivo anticancer activity, inhibiting cell proliferation, disrupting the cell cycle, and inducing Apoptosis. AD1058 can be utilized in research on brain and central nervous system metastases stemming from advanced solid tumors .
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- HY-112226
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Caspase
Drug Metabolite
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Inflammation/Immunology
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VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively .
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- HY-12768B
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BLZ945 dihydrochloride
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c-Fms
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Neurological Disease
Cancer
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Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
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- HY-163415
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Monoamine Oxidase
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Neurological Disease
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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 .
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- HY-161842
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Cholinesterase (ChE)
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Neurological Disease
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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 .
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- HY-14503
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DWK-1339
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Amyloid-β
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Neurological Disease
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MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
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- HY-13340
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VU152100
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mAChR
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Neurological Disease
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VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
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- HY-10232
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THIP
1 Publications Verification
Gaboxadol
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GABA Receptor
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Neurological Disease
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THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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- HY-103268
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Potassium Channel
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Neurological Disease
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(Rac)-AZD3839 is an orally active beta-amyloid precursor protein cleaving enzyme (BACE1) inhibitor that is blood-brain barrier-permeable. (Rac)-AZD3839 has an affinity for the human ether-a-go-go related gene (hERG) ion channel. (Rac)-AZD3839 can be used in the research of Alzheimer's disease .
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- HY-157555
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NOD-like Receptor (NLR)
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Neurological Disease
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NLRP3-IN-29(Compound 5M) is an inhibitor of NLR family pyrin domain containing 3 (NLRP3). NLRP3-IN-29 has the potential for blood-brain barrier permeability and inflammation inhibition both in vivo and in vitro. NLRP3-IN-29 can be used for research on Alzheimer's disease .
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- HY-164311
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Others
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Neurological Disease
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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 .
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- HY-111544
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Histone Methyltransferase
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Cancer
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EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated .
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- HY-161303
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Others
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Cancer
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ZNF207-IN-1 (compound C16) is a potent inhibitor of Zinc Finger Protein 207 (ZNF207)， with IC50 values ranging from 0.5–2.5 μM for inhibiting sphere formation and 0.5–15 μM for cytotoxicity. ZNF207-IN-1 exhibites efficient permeability across the blood–brain barrier .
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- HY-132242
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SFN-NAC
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HDAC
Apoptosis
Drug Metabolite
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Cancer
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DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC) is an orally active HDAC inhibitor and metabolite of sulforaphane (HY-13755) with longer half-life and better blood-brain barrier permeability. DL-Sulforaphane N-acetyl-L-cysteine activates autophagy-mediated downregulation of α-tubulin expression through the ERK pathway and can be used in cancer research .
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- HY-162402
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Reactive Oxygen Species
Cholinesterase (ChE)
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Cancer
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NLRP3-IN-33 (Compound 12o) is a blood-brain barrier permeable inhibitor of AChE and BChE, with IC50 values of 1.02 μM and 7.03 μM against hAChE and hBChE respectively. NLRP3-IN-33 possesses antioxidant, anti-inflammatory, and metal chelating activities, making it a potential candidate for research in Alzheimer's disease (AD) .
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- HY-158160
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Sodium Channel
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Metabolic Disease
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LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable .
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- HY-P10698
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LDLR
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Neurological Disease
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VH-N412 is a vectorized neuropeptide (NT) with good blood-brain barrier permeability. VH-N412 binds to the low-density lipoprotein receptor (LDLR) and neuropeptide receptor 1 (NTSR-1), and acts as a pharmacological-induced hypothermia (PIH) inducer. VH-N412 exhibits anticonvulsant and neuroprotective effects, and can be used in the study of neurological diseases such as epilepsy.
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-
- HY-A0168R
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
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-155532
-
|
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Apoptosis
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
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-
- 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 .
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-
- HY-107758
-
|
|
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) .
|
-
- HY-157382
-
|
|
Cholinesterase (ChE)
Amyloid-β
MMP
|
Neurological Disease
|
|
AChE-IN-51 (compound 8C) is an orally active, non-competitive inhibitor of AChE and BChE (IC50: 84 nM, 97 nM). It also inhibits MMP-2 and amyloid Aβ1-42 aggregates (IC50: 724 nM, 302 nM). AChE-IN-51 has low cytotoxicity and in silico predicted blood-brain barrier permeability. Can be used for research on diseases such as Alzheimer's disease (AD) .
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-
- HY-16969
-
Dihexa
5 Publications Verification
PNB-0408; N-hexanoic-Try-Ile-(6)-amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2
|
c-Met/HGFR
|
Neurological Disease
|
|
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
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-
- HY-152142
-
|
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
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-
- HY-158365
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability .
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-
- HY-N0108
-
|
Parietin; Rheochrysidin
|
Bacterial
Toll-like Receptor (TLR)
NF-κB
Apoptosis
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells .
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-
- 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.
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-
- HY-160831
-
|
PQQ-TME
|
Others
|
Neurological Disease
|
|
PQQ-trimethylester (PQQ-TME) is a synthetic compound that is a trimethylester derivative of pyrroloquinoline quinone (PQQ). PQQ-trimethylester has twice the blood-brain barrier permeability of PQQ (HY-100196) in vitro. In addition, PQQ-trimethylester shows strong inhibitory activity against α-synuclein, amyloid β1-42 (Aβ1-42) and prion protein fibrillation. PQQ-trimethylester can be used in the study of neurodegenerative diseases .
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-
- HY-10232S
-
|
Gaboxadol-d4
|
Isotope-Labeled Compounds
GABA Receptor
|
Neurological Disease
|
|
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
|
-
- 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-110155
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
|
-
- HY-161466
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
AChE-IN-62 (Compound 1) is an effective mixed and selective acetylcholinesterase (AChE) inhibitor with an IC50 value of 0.421 μM. AChE-IN-62 exhibits excellent blood-brain barrier permeability and neuroprotective effects. Additionally, AChE-IN-62 can inhibit the aggregation of Aβ1-42 with an IC50 value of 44.64 μM. AChE-IN-62 is also an effective multi-target-directed ligand (MTDL) that can be utilized in the research of Alzheimer's disease .
|
-
- HY-117088
-
|
|
Neurokinin Receptor
|
Neurological Disease
|
|
LM11A-31, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
|
-
- HY-155085
-
|
|
Monoamine Oxidase
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
hAChE-IN-3 (compounds 5c) is a potent and blood-brain barrier permeable AChE, BuChE， MAO-B-IN-1 and BACE-1 inhibitor, with IC50 values of 0.44, 0.08, 5.15 and 0.38 μM, respectively. hAChE-IN-3 has antioxidant activity and metal chelating ability. In addition, hAChE-IN-3 can bind to peripheral anion sites, and affect β amyloid and reduce Alzheimer's-associated neurodegeneration. hAChE-IN-3 has the potential for the research of Alzheimer's disease .
|
-
- 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 .
|
-
- HY-161461
-
|
|
Amylases
|
Neurological Disease
|
|
E234G HYPE-IN-1 (Compound I2.10) is an inhibitor of AMPylation directed by the Huntingtin-interacting protein E (HYPE), possessing low micromolar bioactivity, low cytotoxicity, and blood-brain barrier permeability. E234G HYPE-IN-1 can inhibit the AMPylation of B-cell immunoglobulin-binding protein (BiP), the primary substrate of HYPE. E234G HYPE-IN-1 is suitable for development as a HYPE-specific therapeutic agent for clinical conditions such as neurodegenerative diseases and diabetes .
|
-
- 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 .
|
-
- HY-164495
-
|
|
FAAH
Thyroid Hormone Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Sob-AM2 is a potent substrate (Km=1.3 μM) targeting fatty acid amide hydrolase (FAAH) expressed in the brain and has blood-brain barrier permeability. Sob-AM2 delivers high concentrations of Sobetirome (HY-14823) to the central nervous system with minimal peripheral systemic dose, thereby stimulating central thyroid hormone receptor β (TRβ). In addition, Sob-AM2 can prevent myelin and axon degeneration in experimental autoimmune encephalomyelitis (EAE) mice .
|
-
- HY-103234A
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
|
-
- HY-103234
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research .
|
-
- HY-103234B
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research .
|
-
- HY-10895
-
|
SB 334867A
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
|
-
- HY-B0250S1
-
|
BCH-189-13C,15N2,d2
|
Isotope-Labeled Compounds
HBV
Reverse Transcriptase
HIV
|
Infection
|
|
Lamivudine-13C,15N2,d2 (BCH-189-13C,15N2,d2) is a 13C, 15N, and deuterium labeled Lamivudine (HY-B0250). Lamivudine is an orally active and blood-brain barrier permeable nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine inhibits HIV reverse transcriptase 1 and 2 and hepatitis B virus (HBV) reverse transcriptase .
|
-
- HY-16731
-
|
EVT 302; RG1577; RO4602522
|
Monoamine Oxidase
Reactive Oxygen Species
|
Neurological Disease
|
|
Sembragiline (EVT 302) is a potent, selective and reversible monoamine oxidase B (MAO-B) inhibitor. Sembragiline reduces the metabolism of dopamine and other amine neurotransmitters by inhibiting the activity of the MAO-B enzyme, thereby potentially increasing the concentration of these neurotransmitters in the brain. Inhibition of the MAO-B enzyme also reduces the formation of toxic reactive oxygen species (ROS) that play a role in the pathological process of AD. Sembragiline has good oral activity and blood-brain barrier permeability. Sembragiline can be used in studies of AD, especially in patients with AD who show increased MAO-B activity .
|
-
- HY-163746
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease .
|
-
- 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-162812
-
|
|
Apoptosis
Cholinesterase (ChE)
Tau Protein
Ferroptosis
Histamine Receptor
|
Neurological Disease
|
|
H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
|
-
- HY-16531
-
YF-2
2 Publications Verification
|
Histone Acetyltransferase
|
Neurological Disease
Cancer
|
|
YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease .
|
-
- HY-16531A
-
|
|
Histone Acetyltransferase
|
Neurological Disease
Cancer
|
|
YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease .
|
-
- HY-10895A
-
|
SB334867A free base
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
|
-
- HY-151929
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-4 is a potent inhibitor of JNK3 (IC50=1.0 nM) based on 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile. JNK3 inhibitor-4 shows excellent selectivity over other protein kinases including isoforms JNK1 (IC50=143.9 nM) and JNK2 (IC50=298.2 nM) . JNK3 inhibitor-4 has neuroprotective effect and predicated blood-brain barrier permeability .
|
-
- HY-126123
-
|
|
iGluR
Potassium Channel
|
Neurological Disease
|
|
NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier .
|
-
- HY-161953
-
|
|
OGA
|
Neurological Disease
|
|
O-GlcNAcase-IN-2 (compound 81) is an orally effective, blood-brain barrier-permeable OGA inhibitor (IC50=4.93 nM). O-GlcNAcase-IN-2 can increase the O-GlcNAcylation level of proteins and phosphorylation of tau (p-Ser199, p-Thr205 and p-Ser396) in the OA-damaged SH-SY5Y cell model. O-GlcNAcase-IN-2 can also improve cognitive impairment in APP/PS1 mice and has potential anti-Alzheimer's disease (AD) effects .
|
-
- 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-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-12678S1
-
|
NMS-E628-d8; RXDX-101-d8
|
Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
|
Cancer
|
|
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
|
-
- HY-163879
-
|
|
Monoamine Oxidase
Reactive Oxygen Species
Ferroptosis
|
Neurological Disease
|
|
hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
|
-
- HY-12098
-
|
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
|
-
- HY-151368
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research .
|
-
- HY-15292
-
S107
1 Publications Verification
|
Calcium Channel
Others
|
Cardiovascular Disease
|
|
S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca 2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold .
|
-
- HY-120464
-
|
SAM-760
|
5-HT Receptor
|
Neurological Disease
|
|
PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research .
|
-
- HY-158148
-
|
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
|
|
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 .
|
-
- HY-161512
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research .
|
-
- 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-107384
-
|
EMD-61753
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
|
-
- HY-107384A
-
|
EMD-61753 hydrochloride
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
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Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
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- HY-144765
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NF-κB
Apoptosis
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-152506
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Amyloid-β
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Neurological Disease
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Antioxidant agent-8 is an orally active inhibitor of Aβ1-42 deposition. Antioxidant agent-8 inhibits fibril aggregation (IC50=11.15 µM) and promotes fibril disaggregation (IC50=6.87 µM). Antioxidant agent-8 also inhibits Cu 2+-induced Aβ1-42 fibril aggregation (IC50=3.69 µM) and promotes Cu 2+-induced Aβ1-42 fibril disaggregation (IC50=3.35 µM). Antioxidant agent-8 has antioxidant activity, anti-inflammatory activity, biosafety, blood-brain barrier permeability and neuroprotective effect .
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- HY-103534
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GABA Receptor
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Neurological Disease
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CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities .
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- HY-123240
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GABA Receptor
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Neurological Disease
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CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities .
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- HY-12882
-
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RC 61-91; NP-120
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iGluR
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Neurological Disease
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Ifenprodil (RC 61-91) is a noncompetitive NMDA receptor antagonist with anti-excitotoxic activity. Ifenprodil significantly improves long-term sensorimotor and spatial learning deficits in mice after acute subarachnoid hemorrhage. Ifenprodil reduces neuronal cell death in the basal cortex and CA1 region of the hippocampus induced by experimental subarachnoid hemorrhage. Ifenprodil attenuates Ca2+ overload in basal cortical cells and mitochondria, as well as brain edema in blood-brain barrier damage and early brain injury. Ifenprodil reduces the intracellular Ca2+ increase and apoptosis of primary cortical neurons under conditions of high glutamate concentrations. Ifenprodil also reduces the increase in endothelial permeability caused by high glutamate concentrations in human brain microvascular endothelial cells. Ifenprodil also inhibits GIRK channels and interacts with α1-adrenergic, 5-HT, and σ receptors .
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- HY-N6962
-
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TRP Channel
COX
Bacterial
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Infection
Neurological Disease
Metabolic Disease
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α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( TRPV1), and it's also an inhibitor of COX-1 and COX-2, with IC50 values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice .
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- HY-163565
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Btk
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Neurological Disease
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BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. BIIB129 can be used in multiple sclerosis (MS) research .
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- HY-149090
-
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Cholinesterase (ChE)
Monoamine Oxidase
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Neurological Disease
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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 .
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- HY-161925
-
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Others
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-148030
-
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PROTACs
LRRK2
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Neurological Disease
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XL01126 is a potent LRRK2 PROTAC (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)) composed of the VHL ligand VH 101, thiol (HY-47851, blue part) and the LRRK2 inhibitor HG-10-102-01 (HY-13488, red part). XL01126 crosses the blood-brain barrier and is used as a degradation probe in Parkinson's disease research. XL01126 can be used to study the non-catalytic and framework functions of LRRK2 .
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- HY-136026
-
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BLU-5937
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P2X Receptor
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Inflammation/Immunology
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Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough .
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HY-L028
-
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877 compounds
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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 877 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.
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HY-L0123V
-
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30,300 compounds
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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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| Cat. No. |
Product Name |
Type |
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- HY-128868
-
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Fluorescent Dyes/Probes
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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 .
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- HY-128868A
-
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Fluorescent Dyes/Probes
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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 .
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- HY-128868D
-
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Fluorescent Dyes/Probes
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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 .
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- HY-128868G
-
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Fluorescent Dyes/Probes
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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-128868B
-
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Dyes
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FITC-Dextran (MW 3000-5000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). FITC-Dextran (MW 3000-5000) 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 3000-5000) can also be used for cell permeability studies, such as blood-brain barrier permeability and determination of the extent of blood-brain barrier disruption . Storage: protect from light.
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- HY-111653
-
CycLuc1
2 Publications Verification
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Chromogenic Substrates
|
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CycLuc1 is a blood-brain barrier permeable luciferase substrate that displays near-infrared (NIR) emission with a peak luminescence wavelength of 599 nm. CycLuc1 can be used for in vivo bioluminescence imaging .
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| Cat. No. |
Product Name |
Type |
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- HY-B1102
-
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Direct Blue 53; T-1824; C.I. 23860
|
Cell Assay Reagents
|
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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 .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P4989
-
|
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Biochemical Assay Reagents
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Infection
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Type A Allatostatin III (allatostatin 3) is a blood-brain barrier permeable and reversible neuropeptide that inhibits hormone synthesis in juvenile female cockroaches. Type A Allatostatin III can be used in pesticide research .
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- HY-P10502
-
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Peptides
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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-P10153
-
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Peptides
|
Others
|
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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 .
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- HY-P10698
-
|
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LDLR
|
Neurological Disease
|
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VH-N412 is a vectorized neuropeptide (NT) with good blood-brain barrier permeability. VH-N412 binds to the low-density lipoprotein receptor (LDLR) and neuropeptide receptor 1 (NTSR-1), and acts as a pharmacological-induced hypothermia (PIH) inducer. VH-N412 exhibits anticonvulsant and neuroprotective effects, and can be used in the study of neurological diseases such as epilepsy.
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-N6685S1
-
|
|
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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 .
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- HY-12678S1
-
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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- HY-10232S
-
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THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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- HY-B0250S1
-
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Lamivudine-13C,15N2,d2 (BCH-189-13C,15N2,d2) is a 13C, 15N, and deuterium labeled Lamivudine (HY-B0250). Lamivudine is an orally active and blood-brain barrier permeable nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine inhibits HIV reverse transcriptase 1 and 2 and hepatitis B virus (HBV) reverse transcriptase .
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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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