产品说明书
GFB-8438
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同义名 : | - |
| CAS号 : | 2304549-73-1 | |
| 货号 : | A1226349 | |
| 分子式 : | C16H14ClF3N4O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 386.756 | |
| MDL号 : | MFCD32671553 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 85 mg/mL(219.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.59mL 0.52mL 0.26mL |
12.93mL 2.59mL 1.29mL |
25.86mL 5.17mL 2.59mL |
| 参考文献 |
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