GFB-8438

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GFB-8438 是一种有效的 TRPC5 亚型选择性抑制剂（hTRPC5 和 hTRPC4 的 IC50 值分别为 0.18 和 0.29 μM）。

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively). GFB-8438 is a novel TRPC5 inhibitor.?GFB-8438 protects mouse podocytes from injury induced by protamine sulfate (PS) in vitro.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.

Pretreatment of mouse podocyte with GFB-8438 (1 μM for 30 min), followed by incubation with protamine sulfate, effectively blocked synaptopodin loss and cytoskeletal remodeling.

GFB-8438 (30 mg/kg; s.c.; daily for 3 weeks) is efficacious in a hypertensive deoxycorticosterone acetate (DOCA)-salt rat model of focal segmental glomerulosclerosis (FSGS), significantly reducing both total protein and albumin concentrations in urine.GFB-8438 (1 mg/kg; i.v.) treatment shows the?Cl,?VSS,?and ?t1/2?were?31?mL/min/kg,?1.17?L/kg,?and?0.5 hours, respectively. Animal Model:Sprague Dawley rats (DOCA-salt rat model of FSGS)Dosage:30 mg/kg Administration:s.c.; daily for 3 weeks Result:Significant reduction in urine protein concentrations.Animal Model:6-8 weeks old male SD rats Dosage:1 mg/kg Administration:i.v. (Pharmacokinetic?Analysis)Result:The?Cl,?Vss,??and t1/2?were?31?mL/min/kg,?1.17?L/kg,?and?0.5 hours, respectively.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPC5

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2304549-73-1

386.75

C16H14ClF3N4O2

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (215.46 mM)

FC(F)(F)C1=CC=CC=C1CN1CCN(CC1=O)C1=C(Cl)C(=O)NN=C1

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(-20℃)

With Ice Pack

≥ 2 years