Darigabat (PF-06372865, CVL-865) | GABAA α2/α3 PAM | Probechem Biochemicals

Chemical Structure : Darigabat

CAS No.: 1614245-70-3

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Darigabat (PF-06372865, PF06372865, CVL-865, CVL865)

货号: PC-62089Not For Human Use, Lab Use Only.

Darigabat (PF-06372865, CVL-865) is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator with Ki of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively.

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5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
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100 mg		Get quote

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生物&药学活性

Darigabat (PF-06372865, CVL-865) is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator with Ki of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively.
PF-06372865 (Darigabat) exhibits functional selectivity for receptors containing α2/3/5 subunits, with significant positive allosteric modulation (90-140%) but negligible activity (<20%) at GABAA receptors containing α1 subunits.
PF-06372865 (Darigabat) demonstrates a robust increase in saccadic peak velocity, increases in beta frequency qEEG and a slight saturating increase in body sway in clinical trials.

物理化学性质&存储条件

分子量	440.493
分子式	C22H21FN4O3S
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	7-ethyl-4-(4'-(ethylsulfonyl)-6-fluoro-2'-methoxybiphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine

参考文献

1. Nickolls SA, et al. Br J Pharmacol. 2018 Feb;175(4):708-725.

Darigabat (PF-06372865, PF06372865, CVL-865, CVL865)

生物&药学活性

物理化学性质&存储条件

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Darigabat (PF-06372865, PF06372865, CVL-865, CVL865)

生物&药学活性

物理化学性质&存储条件

参考文献

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