|4-氯-5-(3-氧代-4-(2-(三氟甲基)苄基)哌嗪-1-基)哒嗪-3(2H)-酮|CsnPharm

CAS No.: 2304549-73-1

GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively.

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400-920-2911

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描述The nonselective Ca²⁺-permeable transient receptor potential (TRP) channels play important roles in diverse cellular processes, including actin remodeling and cell migration. TRP channel subfamily C, member 5 (TRPC5) helps regulate a tight balance of cytoskeletal dynamics in podocytes and is involved in the pathogenesis of proteinuric kidney diseases, such as focal segmental glomerulosclerosis (FSGS). GFB-8438 is a potent and selective inhibitor of TRPC5 with IC₅₀s of 0.18, 0.29 and 0.18 μM for hTRPC5, hTRPC4 and rTRPC5, respectively. In vitro, pretreatment of mouse podocyte with GFB-8438 (1 μM for 30 min), followed by incubation with PS (protamine sulfate), effectively blocked synaptopodin loss and cytoskeletal remodeling. In an in vivo deoxycorticosterone acetate (DOCA)-rat model of FSGS, GFB-8438 (30 mg/kg; s.c.; daily for 3 weeks) caused significant reductions in urine protein concentrations when compared to the DOCA control group. This trend was even more robust when analyzing the urine albumin concentrations, which were significantly lower at both two- and three-week time points and similar to the eplerenone control group^[1].
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技术信息

CAS号

2304549-73-1

储存条件

分子式

C16H14ClF3N4O2

运输

蓝冰

分子量

386.76

别名

溶解度

动物实验配方

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