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首页-小分子抑制剂&激动剂-GPCR-mGluR-HTL14242
HTL14242

Chemical Structure : HTL14242

CAS No.: 1644645-32-8

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HTL14242 (HTL0014242)

货号: PC-49746Not For Human Use, Lab Use Only.

HTL14242 (HTL0014242) a potent, selective mGlu5 negative allosteric modulator (NAM) with pKi of 9.3 and pIC50 of 9.2, shows high selectivity within the metabotropic family of GPCRs.

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10 mg ￥2380 In stock
25 mg ￥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HTL14242 (HTL0014242) a potent, selective mGlu5 negative allosteric modulator (NAM) with pKi of 9.3 and pIC50 of 9.2, shows high selectivity within the metabotropic family of GPCRs.
HTL14242 displays 10-100 fold lower affinities and potencies than mavoglurant (pKi 8.0, pIC50 8.0) and dipraglurant (pKi 6.9, pIC50 6.9).
HTL0014242 (oral dose of 3 mg/kg) demonstrated 80% mGlu5 target receptor occupancy and in rats.

物理化学性质&存储条件

分子量 310.72
分子式 C16H8ClFN4
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

3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile

参考文献

1. Bennett KA, et al. Adv Pharmacol. 2020;88:35-58.

2. Bennett KA, et al. J Pharmacol Exp Ther. 2021 Apr;377(1):157-168.

3. Christopher JA, et al. J Med Chem 58:6653–6664.

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