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highly brain penetrable

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101188
    INCB38579

    		Histamine Receptor Infection
    INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities .
    INCB38579
  • HY-128351
    SHR1653

    		Oxytocin Receptor Neurological Disease Endocrinology
    SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR .
    SHR1653
  • HY-13909
    RGFP966
    Maximum Cited Publications
    37 Publications Verification

    		 HDAC Cancer
    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
    RGFP966
  • HY-14136
    Rimonabant
    5+ Cited Publications

    SR141716

    		 Cannabinoid Receptor Bacterial Infection Metabolic Disease Cancer
    Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
    Rimonabant
  • HY-104044
    Pamiparib
    2 Publications Verification

    BGB-290

    		 PARP Cancer
    Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
    Pamiparib
  • HY-107691
    GR 159897

    		Neurokinin Receptor Neurological Disease Endocrinology Cancer
    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .
    GR 159897
  • HY-128349
    MT-3014

    		Phosphodiesterase (PDE) Neurological Disease
    MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively .
    MT-3014
  • HY-14136S
    Rimonabant-d10

    SR141716-d10

    		 Isotope-Labeled Compounds Cannabinoid Receptor Bacterial Infection Metabolic Disease Cancer
    Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
    Rimonabant-d10
  • HY-104044R
    Pamiparib (Standard)

    		PARP Cancer
    Pamiparib (Standard) is the analytical standard of Pamiparib. This product is intended for research and analytical applications. Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
    Pamiparib (Standard)
  • HY-104044A
    Pamiparib maleate

    BGB-290 maleate

    		 Apoptosis Neurological Disease
    Pamiparib maleate (BGB-290 maleate) is a highly potent and selective PARP inhibitor with neurotoxicity-inducing activity. Pamiparib maleate can effectively penetrate the blood-brain barrier and cause cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos exposed. Pamiparib maleate exposure downregulates the activities of acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase) and leads to upregulation of oxidative stress, which triggers apoptosis and interferes with the expression of neurodevelopment-related genes. The use of pamiparib maleate is also accompanied by downregulation of the Notch signaling pathway, while activation of the Notch signaling pathway can partially rescue neurodevelopmental toxicity. Therefore, pamiparib maleate provides a reference for evaluating its potential neurotoxicity during embryonic development .
    Pamiparib maleate
  • HY-13488
    HG-10-102-01
    1 Publications Verification

    		 LRRK2 MNK Neurological Disease
    HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research .
    HG-10-102-01
  • HY-120144
    SR-8993

    		Opioid Receptor Neurological Disease
    SR-8993 is a highly selective nociceptin receptor agonist that can penetrate the blood-brain barrier and has the activity of reducing alcohol intake and relieving withdrawal anxiety. SR-8993 has shown mild anxiolytic effects in animal models and can effectively reverse anxiety caused by acute alcohol withdrawal. SR-8993 further reduces restricted drinking, operant responses for alcohol, and increased drinking induced by long-term intermittent exposure to alcohol. SR-8993 also reduces stress- and cue-related alcohol-seeking relapse .
    SR-8993

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