GFB-8438 是有效的TRPC5选择性抑制剂,对 hTRPC5 和 hTRPC4 的IC50分别为 0.18 和 0.29 μM。它对 TRPC6、其他 TRP 家族成员、NaV1.5 具有良好的选择性,对 HERG 通道的活性也有限。它对小鼠足细胞的保护作用。
产品描述
GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).
体外活性
GFB-8438 is a novel TRPC5 inhibitor.?GFB-8438 protects mouse podocytes from injury induced by protamine sulfate (PS) in vitro.
体内活性
GFB-8438?is also efficacious in a hypertensive deoxycorticosterone acetate (DOCA)-salt rat model of FSGS, significantly reducing both total protein and albumin concentrations in urine
动物实验
Sprague Dawley rats (DOCA-salt rat model of FSGS);30 mg/kg; Administration:s.c.; daily for 3 weeks
Cas No.
2304549-73-1
分子式
C16H14ClF3N4O2
分子量
386.76
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years