Bioactivity | HC-067047 hydrochloride 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]. |
Invitro | HC-067047 hydrochloride(1 μM;24 小时;HEI-OC1 细胞)处理显着降低高糖培养的 HEI-OC1 细胞中的 mRNA 表达[2]。HC-067047 hydrochloride(1 μM;24 小时;HEI-OC1 细胞)处理显着降低 TRPV4 蛋白的表达[2]。HC-067047 hydrochloride(1 μM;48 小时;HEI-OC1 细胞)处理可抑制细胞增殖[2]。HC-067047 hydrochloride(1 μM;48 小时;HEI-OC1 细胞)处理可促进细胞凋亡[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HC-067047 hydrochloride 相关抗体: |
In Vivo | HC-067047 hydrochloride (0-50 mg/kg;腹腔注射;持续 30 分钟;环磷酰胺治疗的 WT 和 Trpv4-/- 小鼠,以及幼稚 WT 小鼠) 治疗可增加功能性膀胱容量并降低排尿频率 在患有膀胱炎的WT小鼠中。HC-067047 hydrochloride 不影响 Trpv4-/- 小鼠的膀胱功能[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 1481646-76-7 |
Formula | C26H29ClF3N3O2 |
Molar Mass | 507.98 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |