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brain-permeable

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57

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100614
    AS1517499
    Maximum Cited Publications
    24 Publications Verification

    STAT Inflammation/Immunology Cancer
    AS1517499 is a potent and brain-permeable STAT6 phosphorylation inhibitor with an IC50 of 21 nM.
    AS1517499
  • HY-16691
    AK-7
    1 Publications Verification

    Sirtuin Neurological Disease
    AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
    AK-7
  • HY-137440

    TAK-994 free base

    Orexin Receptor (OX Receptor) Neurological Disease
    Firazorexton (TAK-994 free base) is an orally active, brain-permeable orexin type 2 receptor (OX2R) agonist. Firazorexton has the potential to improve narcolepsy like symptoms .
    Firazorexton
  • HY-149966

    HDAC Inflammation/Immunology
    PB131 is a selective and brain-permeable HDAC6 inhibitor with high binding affinity (IC50: 1.8 nM). PB131 has potent anti-inflammatory activity. PB131 can be used for research of inflammation, especially neuroinflammation .
    PB131
  • HY-136094

    Sirtuin Neurological Disease
    SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect .
    SRT3657
  • HY-15262
    SRT 2104
    10+ Cited Publications

    Sirtuin Neurological Disease Metabolic Disease Cancer
    SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD + dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease .
    SRT 2104
  • HY-131036

    Monoamine Oxidase Neurological Disease
    MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease . MAO-IN-M30 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MAO-IN-M30 dihydrochloride
  • HY-149202

    PGE synthase Inflammation/Immunology
    UT-11 is a potent and brain-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50s of 0.10 μM and 2.00 μM for inhibiting PGE2 production in human (SK-N-AS) and murine (BV2) cells, respectively .
    UT-11
  • HY-14552
    Talnetant
    3 Publications Verification

    SB 223412

    Neurokinin Receptor Neurological Disease Endocrinology
    Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies .
    Talnetant
  • HY-14552A

    SB 223412 hydrochloride; SB 223412-A

    Neurokinin Receptor Neurological Disease Endocrinology
    Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies .
    Talnetant hydrochloride
  • HY-W686216

    Ferroptosis Neurological Disease
    VK-28, a brain-permeable iron chelator, inhibits both basal and Fe/ascorbate-induced mitochondrial membrane lipid peroxidation, with an IC50 of 12.7 μM. VK-28 exhibits significant neuroprotective effects on ICV-6-OHDA. VK-28 can be used for the research of Parkinson’s disease and other neurodegenerative diseases .
    VK-28
  • HY-18679

    mGluR Neurological Disease
    TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo .
    TC-N 22A
  • HY-133011

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease .
    nAChR agonist 1
  • HY-158115

    Molecular Glues Raf MEK Cancer
    NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .
    NST-628
  • HY-13438
    AZD3839 free base
    1 Publications Verification

    Beta-secretase Cancer
    AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
    AZD3839 free base
  • HY-16936

    JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome .
    JH-II-127
  • HY-155088

    mGluR Metabolic Disease
    MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
    MK-8768
  • HY-133555

    mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
    mGluR2 antagonist 1
  • HY-U00046

    COX Inflammation/Immunology
    Apyramide is an anti-inflammatory agent (NSAID) and behaves as a proagent of indomethacin (HY-14397). Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2.
    Apyramide
  • HY-108920

    4-Cl-KYN; AV-101

    Others Neurological Disease
    4-Chlorokynurenine is a prodrug of a NMDA receptor antagonist. 4-Chlorokynurenine has orally active and blood-brain permeability that can be used for the research of depression .
    4-Chlorokynurenine
  • HY-107409

    iGluR Neurological Disease
    GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
    GNE 5729
  • HY-10547
    OSU-03012
    4 Publications Verification

    AR-12; PDK1 inhibitor AR-12

    PDK-1 Autophagy Cancer
    OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM .
    OSU-03012
  • HY-146101

    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-108337

    iGluR Neurological Disease
    GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively .
    GNE-0723
  • HY-B0762
    Acetyl-L-carnitine hydrochloride
    2 Publications Verification

    O-Acetyl-L-carnitine hydrochloride; ALCAR hydrochloride

    Endogenous Metabolite Neurological Disease
    Acetyl-L-carnitine (O-Acetyl-L-carnitine) hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders .
    Acetyl-L-carnitine hydrochloride
  • HY-155079

    EGFR Cancer
    DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
    DZD1516
  • HY-157132

    FAAH Neurological Disease
    FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity .
    FAAH-IN-8
  • HY-148246

    TGF-β Receptor Cancer
    MU1700 is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability .
    MU1700
  • HY-133898

    TAK-925

    Orexin Receptor (OX Receptor) Others
    Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms .
    Danavorexton
  • HY-110176

    GlyT Neurological Disease
    ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease .
    ASP2535
  • HY-161377

    TGF-β Receptor Cancer
    M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6 .
    M4K2306
  • HY-161116

    Others Cancer
    AD-5584 is an ACSS2 inhibitor with blood-brain permeability. AD-5584 can significantly reduce lipid storage, reduce colony formation, and increase cell death. AD-5584 has antitumor activity .
    AD-5584
  • HY-129545
    DS-1001b
    1 Publications Verification

    Isocitrate Dehydrogenase (IDH) Cancer
    DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity .
    DS-1001b
  • HY-162235

    Orexin Receptor (OX Receptor)
    CVN766 is an orally active inhibitor of orexin 1 receptor antagonist with blood-brain permeability with the IC50 values of 8 nM and >10 μM for OX1R and OX2R, respectively. CVN766 can be used for study schizophrenia .
    CVN766
  • HY-161376

    TGF-β Receptor Cancer
    M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h .
    M4K2281
  • HY-B0762S

    O-Acetyl-L-carnitine-d3 (hydrochloride)

    Endogenous Metabolite Neurological Disease
    Acetyl-L-carnitine-d3 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
    Acetyl-L-carnitine-d3 hydrochloride
  • HY-B0762S1

    O-Acetyl-L-carnitine-d3-1 (hydrochloride)

    Endogenous Metabolite Neurological Disease
    Acetyl-L-carnitine-d3-1 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
    Acetyl-L-carnitine-d3-1 hydrochloride
  • HY-B0762R

    O-Acetyl-L-carnitine hydrochloride (Standard); ALCAR hydrochloride (Standard)

    Endogenous Metabolite Neurological Disease Cancer
    Acetyl-L-carnitine (hydrochloride) (Standard) is the analytical standard of Acetyl-L-carnitine (hydrochloride). This product is intended for research and analytical applications. Acetyl-L-carnitine (O-Acetyl-L-carnitine) hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders .
    Acetyl-L-carnitine hydrochloride (Standard)
  • HY-111274

    Indometacin farnesil

    COX Autophagy Inflammation/Immunology
    Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes .
    Indomethacin farnesil
  • HY-14397S

    Indometacin-d4

    Isotope-Labeled Compounds COX Autophagy Inflammation/Immunology Cancer
    Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
    Indomethacin-d4
  • HY-149143

    TRP Channel Inflammation/Immunology
    JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia .
    JNJ-28583113
  • HY-156168

    Caspase Cancer
    M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability .
    M190S
  • HY-14397S1

    COX Autophagy Inflammation/Immunology Cancer
    Indomethacin-d4 Methyl Ester is the deuterium labeled Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
    Indomethacin-d4 Methyl Ester
  • HY-143330

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
    MAO-B-IN-4
  • HY-105670A

    nAChR Neurological Disease
    PHA-543613 hydrochloride is an oral or active α7 nAChR agonist with brain permeability, For α3β4, α1β1γδ, α4β2 and 5-HT3 receptors selective. PHA-543613 hydrochloride affects sensory gating and memory in an in vivo model of schizophrenia .
    PHA-543613 hydrochloride
  • HY-14405A

    GW679769B

    Neurokinin Receptor Cytochrome P450 Neurological Disease Cancer
    Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
    Casopitant mesylate
  • HY-155534

    Endogenous Metabolite Others
    17β-HSD10-IN-1 (compound 9) is an orally active inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) with blood-brain permeability. 17β-HSD10-IN-1 doesn't result additional effects for mitochondrial off-targets and cytotoxic or neurotoxic effects .
    17β-HSD10-IN-1
  • HY-118858

    EAAT Neurological Disease Cancer
    UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder .
    UCPH-102
  • HY-W018643

    Methyl ferulate

    p38 MAPK Autophagy Neurological Disease Inflammation/Immunology Cancer
    Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties . Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders . Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages .
    Ferulic acid methyl ester
  • HY-119190

    Phosphodiesterase (PDE) Neurological Disease
    PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study .
    PF-06445974

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