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Results for "

mGluR5 inhibitor

" in MedChemExpress (MCE) Product Catalog:

9

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15445
    CTEP
    2 Publications Verification

    RO 4956371; mGluR5 inhibitor

    		 mGluR Neurological Disease
    CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CTEP
  • HY-119282
    AZD6538

    		mGluR Neurological Disease
    AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
    AZD6538
  • HY-122559
    BMS-984923

    		mGluR Neurological Disease
    BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
    BMS-984923
  • HY-11095
    NPS 2390

    		mGluR CaSR Cardiovascular Disease Neurological Disease
    NPS 2390 is a noncompetitive antagonist of mGluR1 and mGluR5 . NPS 2390 is also a potent CaSR (calcium-sensing receptor) inhibitor .
    NPS 2390
  • HY-100786
    DL-AP3

    		Endogenous Metabolite mGluR Phosphatase Neurological Disease Cancer
    DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect .
    DL-AP3
  • HY-101478
    Fenobam

    		mGluR Apoptosis Neurological Disease Cancer
    Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
    Fenobam
  • HY-129636
    CLH304a

    (E)-GABAB receptor antagonist 1

    		 GABA Receptor ERK Neurological Disease
    CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
    CLH304a
  • HY-125717
    VU0029251

    		mGluR Neurological Disease
    VU0029251 is a mGluR5 partial antagonist (Ki: 1.07 μM). VU0029251 inhibits glutamate induced calcium mobilization in HEK293 cell membranes expressing rat mGluR5 (IC50: 1.7 μM) .
    VU0029251
  • HY-101478A
    Fenobam hydrate

    		mGluR Apoptosis Neurological Disease Cancer
    Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .
    Fenobam hydrate

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