883031-03-6

生物活性靶点体外研究体内研究 883031-03-6 试剂级价格

883031-03-6

CAS号:883031-03-6
英文名:2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
中文名:883031-03-6
CBNumber:CB62518965
分子式:C26H28F3N3O2
分子量:471.51
MOL File:883031-03-6.mol

883031-03-6化学性质

储存条件 :2-8°C
溶解度 :DMSO: ≥15mg/mL
形态 :powder
颜色 :white to tan
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

安全信息

危险品标志 :T
危险类别码 :25-36
安全说明 :26-45
危险品运输编号 :UN 2811 6.1 / PGIII
WGK Germany :3

883031-03-6性质、用途与生产工艺

生物活性 HC-067047是一种选择性的TRPV4拮抗剂，对人TRPV4，大鼠TRPV4和小鼠TRPV4的IC50分别为48 nM，133 nM和17 nM。
靶点
Target Value
mTRPV4
(Cell-free assay) 17 nM
hTRPV4
(Cell-free assay) 48 nM
rTRPV4
(Cell-free assay) 133 nM

体外研究

HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells.
HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein.
HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation.
HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis.

RT-PCR

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	24 hours
Result:	The mRNA expression was significantly decreased.

Western Blot Analysis

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	24 hours
Result:	The expression of TRPV4 protein was significantly decreased.

Cell Proliferation Assay

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	48 hours
Result:	Inhibited cell proliferation.

Apoptosis Analysis

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	48 hours
Result:	Promoted cell apoptosis.

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
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.