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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-GABA Receptor-PF-06372865
PF-06372865

Chemical Structure : PF-06372865

CAS No.: 1614245-70-3

PF-06372865 (Darigabat, PF06372865)

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

PF-06372865 (Darigabat) is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator.

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5 mg ¥1280 In stock
10 mg ¥1880 In stock
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50 mg ¥5580 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

PF-06372865 (Darigabat) is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator.
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.

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