| CAS NO: | 942206-85-1 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 942206-85-1 |
| 化学名 | N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]-benzo[b]thiophene-2-carboxamide |
| Canonical SMILES | ClC1=CC=C(S(N[C@H](C(N2CCN(C([C@@H](NC(C3=CC4=C(C=CC=C4)S3)=O)CC(C)C)=O)CC2)=O)CO)(=O)=O)C(Cl)=C1 |
| 分子式 | C28H32Cl2N4O6S2 |
| 分子量 | 655.6 |
| 溶解度 | ≤10mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | GSK1016790A is a small molecule TRPV4 channel activator [1]. TRPV4 is a Ca2+-permeable, nonselective cation channel that has been involved in multiple physiologic functions, such as the regulation of systemic osmotic pressure, vascular function, skin barrier function, airway- and lung function, and in pain. The channel is activated by osmotic, mechanical, chemical cues and thermal changes. Channel activation can be sensitized by inflammation and injury. Mutations of TRPV4 may lead to premature osteoarthritis, skeletal dysplasias, and neurological motor function disorders [2]. In mouse and human TRPV4-expressing human embryonic kidney (HEK) cells, GSK1016790A elicited Ca2+ influx with the EC50 values of 18 and 2.1 nM, respectively. GSK1016790A dose-dependently evoked the activation of TRPV4 whole-cell currents at concentrations above 1 nM [1]. TRPV4 activation with GSK1016790A contracted TRPV4+/+ mouse bladders in vitro. Infusion of GSK1016790A into the bladders of TRPV4+/+ mice induced bladder overactivity with no effect in TRPV4-/- mice [1]. References: |
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