GSK2193874
GSK2193874
CAS: 1336960-13-4
Molecular Formula: C37H38BrF3N4O
GSK2193874 - Names and Identifiers
| Name | GSK2193874 |
| Synonyms | GSK2193874 GSK 2193874 GSK2193874 TRPV4 antagonist GS2193874 3-([1,4′-Bipiperidin]-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide 4-Quinolinecarboxamide, 3-([1,4'-bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]- |
| CAS | 1336960-13-4 |
GSK2193874 - Physico-chemical Properties
| Molecular Formula | C37H38BrF3N4O |
| Molar Mass | 691.62 |
| Density | 1.43±0.1 g/cm3(Predicted) |
| Boling Point | 737.8±60.0 °C(Predicted) |
| Solubility | DMSO: ≥ 100 mg/mL |
| Appearance | powder |
| Color | white to beige |
| pKa | 12.82±0.20(Predicted) |
| Storage Condition | room temp |
| In vitro study | GSK2193874 antagonizes TRP channels and is more selective for target inhibition than for TRPV1, TRPA1, TRPC3, TRPC6, and TRPM8. Treatment of human umbilical vein endothelial cells (HUVECs) with GSK2193874 concentration-dependently prevented cell contraction and inhibited cell detachment caused by TRPV4 activation by GSK1016790. |
| In vivo study | The pharmacokinetics of GSK2193874 were tested in rats and dogs and it was found that GSK2193874 has a half-life and other properties suitable for the oral route in chronic animal models. (In rats: iv CL = 7.3 mL/min/kg, po t1/2=10 h, %F = 31; In dogs: iv CL = 6.9 mL/min/kg, po t1/2=31 h, %F = 53). In addition, in rats, GSK2193874 had no effect on blood pressure or heart rate when the concentration was as high as 30 mg/kg. In some models of heart failure, GSK2193874 improved lung function. Pretreatment with GSK2193874 inhibits the formation of pulmonary edema and enhances arterial oxygenation in acute and chronic heart failure models. GSK2193874 can maintain endothelial cell integrity, inhibit endothelial TRPV4 current, and protect the lung from pulmonary edema formation in ex vivo lung and heart failure models. |
GSK2193874 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
GSK2193874 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.446 ml | 7.229 ml | 14.459 ml |
| 5 mM | 0.289 ml | 1.446 ml | 2.892 ml |
| 10 mM | 0.145 ml | 0.723 ml | 1.446 ml |
| 5 mM | 0.029 ml | 0.145 ml | 0.289 ml |
Last Update：2024-01-02 23:10:35
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Product Name: GSK2193874 Visit Supplier Webpage Request for quotationCAS: 1336960-13-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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