883031-03-6
| 中文名称 | 883031-03-6 |
|---|---|
| 中文同义词 | 化合物HC-067047;HC 067047,可逆TRPV4拮抗剂 |
| 英文名称 | 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide |
| 英文同义词 | 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide;HC 067047;2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-N-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide;HC-067047;HC 067047;HC067047;1221277-90-2;1H-Pyrrole-3-carboxamide, 2-methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-;HC-067047 >=98% (HPLC);Transient receptor potential channels,HC-067047,Inhibitor,HC 067047,TRP Channel,inhibit |
| CAS号 | 883031-03-6 |
| 分子式 | C26H28F3N3O2 |
| 分子量 | 471.51 |
| EINECS号 | |
| 相关类别 | Potent and selective TRPV4 antagonist. |
| Mol文件 | 883031-03-6.mol |
| 结构式 |  |
883031-03-6 性质
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | 在DMSO中的溶解度≥15mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色至棕褐色 |
| 稳定性 | 从购买之日起 2 年内保持稳定。 DMSO 或乙醇溶液可在 -20℃ 下保存长达 3 个月。 |
| Target | Value |
|
mTRPV4
(Cell-free assay) | 17 nM |
|
hTRPV4
(Cell-free assay) | 48 nM |
|
rTRPV4
(Cell-free assay) | 133 nM |
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. |
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 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-100208 | 883031-03-6 HC-067047 | 883031-03-6 | 5mg | 660元 |
| 2024/04/30 | HY-100208 | 883031-03-6 HC-067047 | 883031-03-6 | 10mM * 1mLin DMSO | 685元 |