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首页-小分子抑制剂&激动剂-GPCR-mGluR-VU6024578
VU6024578

Chemical Structure : VU6024578

CAS No.:

VU6024578 (BI02982816)

货号: PC-23777Not For Human Use, Lab Use Only.

VU6024578 (BI02982816) is a selective and CNS penetrant metabotropic glutamate receptor subtype 1 (mGlu1) positive allosteric modulator (PAM) with EC50 of 54 nM and 46 nM for human and rat mGlu1 respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

VU6024578 (BI02982816) is a selective and CNS penetrant metabotropic glutamate receptor subtype 1 (mGlu1) positive allosteric modulator (PAM) with EC50 of 54 nM and 46 nM for human and rat mGlu1 respectively.
VU6024578 also maintains across species, with mouse (EC50 = 27 nM (89% Glumax) [n = 5] (pEC50 = 7.59 ± 0.07)) and dog (EC50 = 87 nM (129% Glumax) [n = 3] (pEC50 = 7.07 ± 0.07)) being in-line with human and rat mGlu1 PAM activity.
VU6024578 displays no agonism up to 30 μM for mGlu5, also is inactive at 5-HT2B, but a functional antagonist at the peripheral BZD (IC50 = 207 nM).
VU6024578 is active in both amphetamine-induced hyperlocomotion (minimum effective dose (MED) = 3 mg/kg, p.o.) and MK-801 induced disruptions of novel object recognition (minimum effective dose = 10 mg/kg p.o.).
VU6024578 is a best-in-class in vivo rodent tool compound to study selective mGlu1 activation.

物理化学性质&存储条件

分子量 395.85
分子式 C20H18ClN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-chloro-N-((1,2'-dimethyl-1H,2'H-[3,3'-bipyrazol]-5-yl)methyl)-5-(furan-2-yl)benzamide

参考文献

1. Reed CW, et al. J Med Chem. 2024 Dec 26;67(24):22291-22312.

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