2304549-73-1
2304549-73-1 structure
- Name: GFB-8438
- Chemical Name: GFB-8438
- CAS Number: 2304549-73-1
- Molecular Formula: C16H14ClF3N4O2
- Molecular Weight: 386.76
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2020-04-24 23:20:51
- Modify Date: 2024-01-09 16:59:17
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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].
| Name | GFB-8438 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
hTRPC5:0.18 μM (IC50) hTRPC4:0.29 μM (IC50) rTRPC5:0.18 μM (IC50) |
| In Vitro | 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[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. |
| References |
| Density | 1.52±0.1 g/cm3(Predicted) |
|---|---|
| Molecular Formula | C16H14ClF3N4O2 |
| Molecular Weight | 386.76 |
| Storage condition | -20°C |
| Hazard Codes | Xn |
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