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CNS penetration

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46

Inhibitors & Agonists

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101281
    VU 6008667

    		mAChR Neurological Disease
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .
    VU 6008667
  • HY-116016
    Etilevodopa

    L-DOPA ethyl ester; Levodopa ethyl ester

    		 Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester), an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .
    Etilevodopa
  • HY-116016A
    Etilevodopa hydrochloride

    L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride

    		 Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .
    Etilevodopa hydrochloride
  • HY-108460
    A-784168

    		TRP Channel Neurological Disease
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .
    A-784168
  • HY-101281A
    (Rac)-VU 6008667

    		mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration .
    (Rac)-VU 6008667
  • HY-125692
    L-740093

    		Cholecystokinin Receptor Metabolic Disease
    L-740093 is a potent cholecystokinin-B receptor antagonist. L-740093 has excellent central nervous system (CNS) penetration .
    L-740093
  • HY-144696
    Dyrk1A/α-synuclein-IN-2

    		DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .
    Dyrk1A/α-synuclein-IN-2
  • HY-144695
    Dyrk1A/α-synuclein-IN-1

    		DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .
    Dyrk1A/α-synuclein-IN-1
  • HY-123934
    VU6007477

    		P-glycoprotein Neurological Disease
    VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
    VU6007477
  • HY-147999
    GlcN-6-P Synthase-IN-1

    		Bacterial Fungal Cytochrome P450 Infection
    GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .
    GlcN-6-P Synthase-IN-1
  • HY-120184
    VU0467485

    AZ13713945

    		 mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
    VU0467485
  • HY-130121
    MK-8719

    		OGA Neurological Disease
    MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (Ki=7.9 nM for hOGA) with excellent CNS penetration .
    MK-8719
  • HY-108463
    A-967079
    5+ Cited Publications

    		 TRP Channel Inflammation/Immunology
    A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
    A-967079
  • HY-16617
    Auglurant

    VU0424238

    		 mGluR Neurological Disease
    Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration .
    Auglurant
  • HY-111258
    GSK345931A

    		Prostaglandin Receptor Neurological Disease Inflammation/Immunology
    GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain .
    GSK345931A
  • HY-101789
    Nav1.7-IN-3

    		Sodium Channel Neurological Disease
    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration .
    Nav1.7-IN-3
  • HY-B0250A
    Lamivudine salicylate

    BCH-189 salicylate

    		 HIV Reverse Transcriptase HBV Infection
    Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine salicylate can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
    Lamivudine salicylate
  • HY-147405
    Tinlorafenib

    PF-07284890; ARRY-461

    		 Raf Cancer
    Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAF V600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies .
    Tinlorafenib
  • HY-13011S
    Alectinib-d8

    CH5424802-d8; RO5424802-d8; AF802-d8

    		 Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
    Alectinib-d8
  • HY-13011S1
    Alectinib-d6

    CH5424802-d6; RO5424802-d6; AF802-d6

    		 Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
    Alectinib-d6
  • HY-17595
    Mebendazole
    3 Publications Verification

    		 Parasite Apoptosis Microtubule/Tubulin Infection Cancer
    Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
    Mebendazole
  • HY-146101
    NMDA receptor antagonist 5

    		iGluR Neurological Disease
    NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research .
    NMDA receptor antagonist 5
  • HY-163131
    Glucosylceramide synthase-IN-4

    		Glucosylceramide Synthase (GCS) Neurological Disease
    Glucosylceramide synthase-IN-4 (compound 12) is a potent glucosylceramide synthase (GCS) inhibitor, with an IC50 of 6.8 nM. Glucosylceramide synthase-IN-4 shows excellent PK properties and stability in human hepatocytes. Glucosylceramide synthase-IN-4 has good CNS penetration and acceptable PXR selectivity .
    Glucosylceramide synthase-IN-4
  • HY-145086
    R-PSOP

    		Others Metabolic Disease
    R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .
    R-PSOP
  • HY-109189
    Rezivertinib
    1 Publications Verification

    BPI-7711

    		 EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
    Rezivertinib
  • HY-17595R
    Mebendazole (Standard)

    		Parasite Apoptosis Microtubule/Tubulin Infection Cancer
    Mebendazole (Standard) is the analytical standard of Mebendazole. This product is intended for research and analytical applications. Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
    Mebendazole (Standard)
  • HY-133166
    A-889425

    		TRP Channel Neurological Disease
    A-889425 is an oral active selective TRPV1 receptor antagonist with the with an IC50 of 335 nM (rat) and 34 nM (human). A-889425 has good penetration into the CNS and reduces mechanical allodynia and spinal neuron responses to mechanical stimulation of Complete Freund's adjuvant (HY-153808)-inflamed rat hind paws .
    A-889425
  • 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) .
    TAK-285
  • HY-145695
    Dual AChE-MAO B-IN-1

    		Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability .
    Dual AChE-MAO B-IN-1
  • HY-13011
    Alectinib
    Maximum Cited Publications
    32 Publications Verification

    CH5424802; RO5424802; RG7853

    		 Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib
  • HY-114331
    DLK-IN-1

    		MAP3K Neurological Disease
    DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
    DLK-IN-1
  • HY-13011A
    Alectinib Hydrochloride
    Maximum Cited Publications
    32 Publications Verification

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    		 Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib Hydrochloride
  • HY-144372
    TRPV1 antagonist 3

    		TRP Channel Neurological Disease
    TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .
    TRPV1 antagonist 3
  • HY-110191
    VU0469650

    		mGluR Neurological Disease Cancer
    VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM .
    VU0469650
  • HY-13011R
    Alectinib (Standard)

    		Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib (Standard) is the analytical standard of Alectinib. This product is intended for research and analytical applications. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib (Standard)
  • HY-19978
    RO-3

    		P2X Receptor Neurological Disease
    RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7) .
    RO-3
  • HY-B0250
    Lamivudine
    5+ Cited Publications

    BCH-189

    		 HIV Reverse Transcriptase HBV Infection Cancer
    Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
    Lamivudine
  • HY-130795
    GSK-3β inhibitor 2
    1 Publications Verification

    		 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 .
    GSK-3β inhibitor 2
  • HY-150503
    KH-259

    		HDAC Neurological Disease
    KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research .
    KH-259
  • HY-B0250S1
    Lamivudine-13C,15N2,d2

    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 .
    Lamivudine-13C,15N2,d2
  • HY-B0250S
    Lamivudine-15N,d2

    BCH-189-15N,d2

    		 HBV HIV Reverse Transcriptase Isotope-Labeled Compounds Infection Cancer
    Lamivudine- 15N,d2 is 15N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
    Lamivudine-15N,d2
  • HY-105685
    SRX246

    		Vasopressin Receptor Neurological Disease
    SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders .
    SRX246
  • HY-13637
    Ganciclovir
    15+ Cited Publications

    BW 759; 2'-Nor-2'-deoxyguanosine

    		 CMV HSV Antibiotic Nucleoside Antimetabolite/Analog Infection Cancer
    Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain .
    Ganciclovir
  • HY-13637A
    Ganciclovir sodium
    15+ Cited Publications

    BW 759 sodium; 2'-Nor-2'-deoxyguanosine sodium

    		 CMV HSV Antibiotic Nucleoside Antimetabolite/Analog Infection Cancer
    Ganciclovir (BW 759) sodium, a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir sodium also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir sodium inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir sodium has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain .
    Ganciclovir sodium
  • HY-13637B
    Ganciclovir hydrate

    BW-759 hydrate; 2'-Nor-2'-deoxyguanosine hydrate

    		 CMV HSV Antibiotic Nucleoside Antimetabolite/Analog Infection Cancer
    Ganciclovir (BW 759) hydrate, a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir hydrate also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir hydrate inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir hydrate has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain .
    Ganciclovir hydrate
  • HY-13637R
    Ganciclovir (Standard)

    		CMV HSV Antibiotic Nucleoside Antimetabolite/Analog Infection Cancer
    Ganciclovir (Standard) is the analytical standard of Ganciclovir. This product is intended for research and analytical applications. Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain .
    Ganciclovir (Standard)

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