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centrally penetrant

" in MedChemExpress (MCE) Product Catalog:

39

Inhibitors & Agonists

1

Screening Libraries

3

Peptides

2

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-17001
    Flupirtine Maleate
    1 Publications Verification

    		 Potassium Channel iGluR Neurological Disease
    Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties .
    Flupirtine Maleate
  • HY-15722
    SB-222200
    4 Publications Verification

    		 Neurokinin Receptor Neurological Disease Endocrinology
    SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders .
    SB-222200
  • HY-132308
    DYRK1-IN-1
    3 Publications Verification

    		 DYRK Neurological Disease
    DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe .
    DYRK1-IN-1
  • HY-103530
    CGP35348
    1 Publications Verification

    		 GABA Receptor Neurological Disease
    CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM. CGP 35348 shows affinity for the GABAB receptor only . CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage .
    CGP35348
  • HY-19884B
    Relamorelin TFA

    RM-131 TFA; BIM-28131 TFA

    		 GHSR Metabolic Disease
    Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
    Relamorelin TFA
  • HY-101718
    Aticaprant
    Maximum Cited Publications
    7 Publications Verification

    CERC-501; LY-2456302

    		 Opioid Receptor Neurological Disease
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
    Aticaprant
  • HY-103530R
    CGP35348 (Standard)

    		Reference Standards GABA Receptor Neurological Disease
    CGP35348 (Standard) is the analytical standard of CGP35348. This product is intended for research and analytical applications. CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only . CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage .
    CGP35348 (Standard)
  • HY-19884
    Relamorelin

    RM-131; BIM-28131

    		 GHSR Metabolic Disease
    Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
    Relamorelin
  • HY-19884A
    Relamorelin acetate

    RM-131 acetate; BIM-28131 acetate

    		 GHSR Metabolic Disease
    Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research .
    Relamorelin acetate
  • HY-120862
    L 368935

    		Cholecystokinin Receptor Neurological Disease
    L 368935 is a cholecystokinin B receptor (CCKB receptor) antagonist. L 368935 is a brain-penetrant and centrally active compound .
    L 368935
  • HY-101022
    CXCR2-IN-1
    2 Publications Verification

    		 CXCR Inflammation/Immunology Endocrinology
    CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3.
    CXCR2-IN-1
  • HY-124382
    AS1928370

    		TRP Channel Neurological Disease
    AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain treatment research .
    AS1928370
  • HY-116524
    PF-04781340

    		5-HT Receptor Neurological Disease
    PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .
    PF-04781340
  • HY-10716A
    PF-03463275

    		GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
    PF-03463275
  • HY-10716
    PF-03463275 hydrochloride

    		GlyT Neurological Disease
    PF-03463275 hydrochloride is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 hydrochloride has the potential for Schizophrenia research .
    PF-03463275 hydrochloride
  • HY-164506
    NRMA-8

    		FAAH Neurological Disease Cancer
    NRMA-8 is a brain-penetrant small molecule nuclear receptor modulator. NRMA-8 is promising for research of central nervous system disorders, including Alzheimer's disease, Parkinson's disease, demylenation disorders and glioblastomas .
    NRMA-8
  • HY-116819A
    VU0453379 hydrochloride

    		GCGR Metabolic Disease
    VU0453379 hydrochloride is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
    VU0453379 hydrochloride
  • HY-116819
    VU0453379

    		GCGR Metabolic Disease
    VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
    VU0453379
  • HY-145778
    AGI-41998

    		Somatostatin Receptor Neurological Disease
    AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .
    AGI-41998
  • HY-101839
    ML381

    VU0488130

    		 mAChR Neurological Disease
    ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies .
    ML381
  • HY-145777
    AGI-43192

    		Somatostatin Receptor Neurological Disease Cancer
    AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease .
    AGI-43192
  • HY-17001R
    Flupirtine Maleate (Standard)

    		Reference Standards Potassium Channel iGluR Neurological Disease
    Flupirtine (Maleate) (Standard) is the analytical standard of Flupirtine (Maleate). This product is intended for research and analytical applications. Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties .
    Flupirtine Maleate (Standard)
  • HY-150640
    Rho-Kinase-IN-2

    		ROCK Neurological Disease
    Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research .
    Rho-Kinase-IN-2
  • HY-121313
    Embusartan

    BAY 10-6734

    		 Angiotensin Receptor Neurological Disease Endocrinology
    Embusartan (BAY 10-6734) is a brain-penetrant and effective AT1 receptor blocker. Embusartan inhibits Ang II binding to brain AT1 receptors in the nuclei of central nervous system (CNS) inside due to high lipophilic character. Embusartan is promising for research of sympathetic hyperactivity and hypertension .
    Embusartan
  • HY-177085
    Fumiporexant

    		Orexin Receptor (OX Receptor) Neurological Disease
    Fumiporexant (Compound Example 93) is an orally active, brain-penetrant and selective Orexin receptor 2 (OX2R) antagonist. Fumiporexant regulates the sleep-wake cycle and emotion-related pathways in the central nervous system. Fumiporexant is promising for research of nervous system diseases such as insomnia and major depressive disorder .
    Fumiporexant
  • HY-W714513
    VU0469650 hydrochloride

    		mGluR Neurological Disease
    VU0469650 hydrochloride is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 1 (mGluR1). VU0469650 hydrochloride inhibits glutamate-induced calcium flux in cells expressing human mGluR1 (IC50= 99 nM). VU0469650 hydrochloride is promising for research of central nervous system diseases such as anxiety, addiction, and epilepsy .
    VU0469650 hydrochloride
  • HY-137055
    PF-3774076

    		Others Others
    PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
    PF-3774076
  • HY-122647
    Valiglurax

    VU0652957; VU2957

    		 mGluR Neurological Disease
    Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease .
    Valiglurax
  • HY-107727
    BMS-193885 L-Lactic acid

    		Neuropeptide Y Receptor Neurological Disease
    BMS-193885 (L-Lactic acid) is a potent, selective, and brain-penetrant neuropeptide Y1 receptor antagonist. BMS-193885 has a Ki value of 3.3 nM for the neuropeptide Y1 receptor, competitively acts on the neuropeptide Y binding site, and can reduce food intake and body weight through central Y1 inhibition .
    BMS-193885 L-Lactic acid
  • HY-109192
    Tolebrutinib
    5+ Cited Publications

    SAR442168; PRN2246

    		 Btk Neurological Disease
    Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS) .
    Tolebrutinib
  • HY-18750A
    Zorifertinib hydrochloride

    AZD3759 hydrochloride

    		 EGFR Apoptosis Cancer
    Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, EGFR inhibitor (IC50s: 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .
    Zorifertinib hydrochloride
  • HY-18750
    Zorifertinib
    5+ Cited Publications

    AZD3759

    		 EGFR Apoptosis Cancer
    Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .
    Zorifertinib
  • 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-149555
    DNL343

    		Eukaryotic Initiation Factor (eIF) Neurological Disease
    DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
    DNL343
  • HY-172182
    ONO-2920632

    VU6011887

    		 Potassium Channel Neurological Disease
    ONO-2920632 is an orally active and central nervous system (CNS)-penetrant TREK activator, with EC50 values of 0.3 µM and 2.8 μM for TREK-1 and TREK-2, respectively. ONO-2920632 exhibits selectivity for other K2P channels (>91-fold selective versus TASK1, TASK2, TASK3, TRAAK, and TWIK2; 31-fold selective versus TRESK). ONO-2920632 possesses analgesic effects and can be used in research on pain, migraine, and neurological disorders.
    ONO-2920632
  • HY-113357
    m-Coumaric acid

    		Endogenous Metabolite Neurological Disease Inflammation/Immunology
    m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .
    m-Coumaric acid
  • HY-113357R
    m-Coumaric acid (Standard)

    		Reference Standards Endogenous Metabolite Neurological Disease Inflammation/Immunology
    m-Coumaric acid (Standard) is the analytical standard of m-Coumaric acid. This product is intended for research and analytical applications. m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .
    m-Coumaric acid (Standard)
  • HY-W027553
    Ipidacrine

    NIK-247 free base

    		 Cholinesterase (ChE) Potassium Channel Sodium Channel Neurological Disease Metabolic Disease
    Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
    Ipidacrine
  • HY-W027553S1
    Ipidacrine-d9

    NIK-247-d10 free base

    		 Isotope-Labeled Compounds Cholinesterase (ChE) Potassium Channel Sodium Channel Metabolic Disease
    Ipidacrine-d9 (NIK-247-d9 (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
    Ipidacrine-d9

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