Benzo[b]thiophene-2-carboxamide, N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]-
GSK1016790A
CAS: 942206-85-1
Molecular Formula: C28H32Cl2N4O6S2
Benzo[b]thiophene-2-carboxamide, N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]- - Names and Identifiers
Benzo[b]thiophene-2-carboxamide, N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]- - Physico-chemical Properties
| Molecular Formula | C28H32Cl2N4O6S2 |
| Molar Mass | 655.61 |
| Density | 1.426±0.06 g/cm3(Predicted) |
| Melting Point | >119°C (dec.) |
| Solubility | DMSO: ≥ 33 mg/mL |
| Appearance | white solid |
| Color | White to Off-White |
| pKa | 8.29±0.50(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| In vitro study | At concentrations above 1 nM, GSK1016790A induces calcium ion (Ca2) influx in HEK cells expressing murine and human TRPV4 (EC50=18 and 2.1 nM, respectively), results in a dose-dependent activation of TRPV4 whole-cell current. It can stimulate and activate TRPV4 in a variety of cell types, including endothelial cells, urinary tract smooth muscle cells, urothelial cells, and HEK293 cells overexpressing TRPV4. GSK1016790A specifically activates TRPV4, which triggers down-regulation of the expression of this channel on the plasma membrane and rapid partial desensitization. |
| In vivo study | GSK1016790A in the case of high pulmonary vascular tension, the systemic vascular resistance and pulmonary vascular resistance decreased sharply. GSK1016780A activates TRP4, causing vasodilation, leakage, and tissue bleeding. |
Benzo[b]thiophene-2-carboxamide, N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]- - Risk and Safety
| WGK Germany | 1 |
Benzo[b]thiophene-2-carboxamide, N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.525 ml | 7.626 ml | 15.253 ml |
| 5 mM | 0.305 ml | 1.525 ml | 3.051 ml |
| 10 mM | 0.153 ml | 0.763 ml | 1.525 ml |
| 5 mM | 0.031 ml | 0.153 ml | 0.305 ml |
Last Update：2024-01-02 23:10:35
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Spot supply
Product Name: GSK1016790A Visit Supplier Webpage Request for quotationCAS: 942206-85-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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