產品描述: | 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 |
靶點: |
IC50: 48 nM (human TRPV4), 133 nM (rat TRPV4), 17 nM (mouse TRPV4);TRP/TRPVChannel |
體內研究: |
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. |
參考文獻: |
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 |
保存條件: |
2-8℃ |
配置溶液濃度參考: |
|
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: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |