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VU6001376 Sale

目录号 : GC37931

VU6001376 是一种有效、选择性的变性谷氨酸受体 4 正变构调节剂 (mGlu4 PAM), 其 EC50 值为 50.1 nM。

VU6001376 Chemical Structure

Cas No.:1968546-34-0

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Sample solution is provided at 25 µL, 10mM.

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产品描述

VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM[1]. mGlu4|50.1 nM (EC50)

[1]. Bollinger SR, et al. Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4). J Med Chem. 2019 Jan 10;62(1):342-358.

Chemical Properties

Cas No. 1968546-34-0 SDF
Canonical SMILES O=C(NC1CC(F)(F)C1)C2=NSC3=CC(NC4=NNC5=C4N=CC=C5)=CC=C32
分子式 C18H14F2N6OS 分子量 400.41
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.4974 mL 12.4872 mL 24.9744 mL
5 mM 0.4995 mL 2.4974 mL 4.9949 mL
10 mM 0.2497 mL 1.2487 mL 2.4974 mL
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Research Update

Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4)

J Med Chem 2019 Jan 10;62(1):342-358.PMID:30247901DOI:10.1021/acs.jmedchem.8b00994

This work describes the discovery and characterization of novel 6-(1 H-pyrazolo[4,3- b]pyridin-3-yl)amino-benzo[ d]isothiazole-3-carboxamides as mGlu4 PAMs. This scaffold provides improved metabolic clearance and CYP1A2 profiles compared to previously discovered mGlu4 PAMs. From this work, 27o (VU6001376) was identified as a potent (EC50 = 50.1 nM, 50.5% GluMax) and selective mGlu4 PAM with an excellent rat DMPK profile ( in vivo rat CLp = 3.1 mL/min/kg, t1/2 = 445 min, CYP1A2 IC50 > 30 μM). Compound 27o was also active in reversing haloperidol induced catalepsy in a rodent preclinical model of Parkinson's disease.