HC 067047 |
カタログ番号GC12260 |
HC 067047 は、強力かつ選択的な TRPV4 アンタゴニストであり、それぞれ 48 nM、133 nM、および 17 nM の IC50 値で、ヒト、ラット、およびマウスの TRPV4 オルソログを流れる電流を可逆的に阻害します。
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Cas No.: 883031-03-6
Sample solution is provided at 25 µL, 10mM.
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[1].
HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells[2].HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein[2].HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation[2].HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis[2].
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[1].
References:
[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.
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