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首页-小分子抑制剂&激动剂-GPCR-mGluR-VU0424238
VU0424238

Chemical Structure : VU0424238

CAS No.: 1396337-04-4

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VU0424238 (VU 0424238, Auglurant)

货号: PC-63197Not For Human Use, Lab Use Only.

Auglurant (VU0424238) is a potent, selective, orally active mGlu5 negative allosteric modulator with Ki of 4.4 nM, displays >900-fold selectivity for mGlu5 versus the other mGlu receptors.

规格 价格 库存 数量
5 mg ￥3780 In stock
10 mg ￥5780 In stock
25 mg ￥8980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Auglurant (VU0424238) is a potent, selective, orally active mGlu5 negative allosteric modulator with Ki of 4.4 nM, displays >900-fold selectivity for mGlu5 versus the other mGlu receptors.
Auglurant (VU0424238) demonstrates 50% receptor occupancy at an oral dose of 0.8 mg/kg in rats and an intravenous dose of 0.06 mg/kg in baboons.

物理化学性质&存储条件

分子量 325.303
分子式 C16H12FN5O2
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

N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide

参考文献

1. Felts AS, et al. J Med Chem. 2017 Jun 22;60(12):5072-5085.

2. Crouch RD, et al. Drug Metab Dispos. 2017 Dec;45(12):1245-1259.

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