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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-GFB-8438
GFB-8438

Chemical Structure : GFB-8438

CAS No.: 2304549-73-1

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GFB-8438 (GFB8438)

货号: PC-73245Not For Human Use, Lab Use Only.

GFB-8438 is a potent, selective TRPC5 inhibitor with IC50 of 0.18 uM (hTRPC5, Qpatch assay).

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 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

GFB-8438 is a potent, selective TRPC5 inhibitor with IC50 of 0.18 uM (hTRPC5, Qpatch assay).
GFB-8438 inhibited the whole cell current with an IC50 of 0.28 μM comparable to the IC50 in Qpatch assay.
GFB-8438 was equipotent against TRPC4 (IC50=0.29 uM) and TRPC5.
GFB-8438 showed excellent selectivity against TRPC6, other TRP family member (TRPC3/7, TRPA1, TRPV1/2/3/4/5, and TRPM2/3/4/8).
GFB-8438 protects mouse podocytes from injury induced by protamine sulfate (PS) in vitro.
GFB-8438 demonstrated robust efficacy in the hypertensive DOCA-salt rat model without affecting blood pressure.

物理化学性质&存储条件

分子量 386.76
分子式 C16H14ClF3N4O2
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

4-chloro-5-(3-oxo-4-(2-(trifluoromethyl)benzyl)piperazin-1-yl)pyridazin-3(2H)-one

参考文献

1. Maolin Yu, et al. ACS Med Chem Lett. 2019 Oct 22;10(11):1579-1585.

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