S87041 |
HC-067047 |
源叶(MedMol) | 98% |
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- 产品描述: HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively
- 靶点: IC50: 48 nM (human TRPV4), 133 nM (rat TRPV4), 17 nM (mouse TRPV4);TRP/TRPVChannel
- 体内研究:
HC-067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4−/− mice, and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis. HC-067047 do not affect bladder function in Trpv4−/− mice. Animal Model: Cyclophosphamide-treated WT and Trpv4−/− mice, and naive WT mice[1] Dosage: 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg Administration: Intraperitoneal injection; for 30 minutes Result: Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4−/− mice.
- 参考文献:
1. Everaerts W et al. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.Proc Natl Acad Sci U S A. 2010 Nov 2;107(44):19084-9. 2. Xing Y, et al. Decreased Expression of TRPV4 Channels in HEI-OC1 Cells Induced by High Glucose Is Associated with Hearing Impairment. Yonsei Med J. 2018 Nov;59(9):1131-1137.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.119 ml 10.593 ml 21.186 ml 5 mM 0.424 ml 2.119 ml 4.237 ml 10 mM 0.212 ml 1.059 ml 2.119 ml 50 mM 0.042 ml 0.212 ml 0.424 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)