| Identification | Back Directory | [Name]
GFB-8438 | [CAS]
2304549-73-1 | [Synonyms]
GFB-8438
4-Chloro-5-[3-oxo-4-(2-trifluoromethyl-benzyl)-piperazin-1-yl]-2H-pyridazin-3-one
4-chloro-5-(3-oxo-4-(2-(trifluoromethyl)benzyl)piperazin-1-yl)pyridazin-3(2H)-one
3(2H)-Pyridazinone, 4-chloro-5-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]-1-piperazinyl]- | [Molecular Formula]
C16H14ClF3N4O2 | [MDL Number]
MFCD32671553 | [MOL File]
2304549-73-1.mol | [Molecular Weight]
386.76 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
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[1].
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[1]. | Animal Model: | Sprague Dawley rats (DOCA-salt rat model of FSGS)[1] | | 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[1] | | 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. |
| [IC 50]
hTRPC5: 0.18 μM (IC50); hTRPC4: 0.29 μM (IC50); rTRPC5: 0.18 μM (IC50) | [References]
[1] Yu M, et al.Discovery?of a?Potent?and?Selective?TRPC5?Inhibitor,?Efficacious?in a?Focal?Segmental?Glomerulosclerosis?Model.ACS Med Chem Lett.?2019 Oct 22;10(11):1579-1585. DOI:10.1021/acsmedchemlett.9b00430 |
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cjbscvictory
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13348960310 13348960310 |
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https://www.weikeqi-biotech.com/ |
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