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
- 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.
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.
- 更新日期：2024/11/08
- 产品编号：HY-100208
- 产品名称：883031-03-6 HC-067047
- CAS编号：883031-03-6
- 包装：5mg
- 价格：660元
- 更新日期：2024/11/08
- 产品编号：HY-100208
- 产品名称：883031-03-6 HC-067047
- CAS编号：883031-03-6
- 包装：10mM * 1mLin DMSO
- 价格：685元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
