| 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 |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |