HC-067047

• CAT Number: I005306
• CAS Number: 883031-03-6
• Molecular Formula: C26H28F3N3O2
• Molecular Weight: 471.51
• Purity: ≥95%
• Synonyms: 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
• InChI: InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33)
• InChIKey: NCZYSQOTAYFTNM-UHFFFAOYSA-N
• SMILES: CC1=C(C=C(N1CCCN2CCOCC2)C3=CC=CC=C3)C(=O)NC4=CC=CC(=C4)C(F)(F)F

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].

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.
 [Content Brief]

[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.
 [Content Brief]