HTL14242 | mGlu5 NAM | Probechem Biochemicals

Chemical Structure : HTL14242

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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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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.

HTL14242 (HTL0014242)

生物&药学活性

物理化学性质&存储条件

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HTL14242 (HTL0014242)

生物&药学活性

物理化学性质&存储条件

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