产品
编 号：F284281
分子式：C16H14ClF3N4O2
分子量：386.76
分子式：C16H14ClF3N4O2
分子量：386.76
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 2304549-73-1
产品详情
生物活性：
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
体内研究：
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.
体外研究：
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 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
体内研究：
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.
体外研究：
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.
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