N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide
GSK429286A
CAS: 864082-47-3
Molecular Formula: C21H16F4N4O2
N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide - Names and Identifiers
N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide - Physico-chemical Properties
| Molecular Formula | C21H16F4N4O2 |
| Molar Mass | 432.37 |
| Density | 1.468 |
| Boling Point | 688.4±55.0 °C(Predicted) |
| Solubility | DMSO: ≥10mg/mL |
| Appearance | powder |
| Color | white to beige |
| pKa | 12.10±0.40(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| In vitro study | GSK429286A slightly inhibited RSK and p70S6K,IC50 were 0.78 and 1.94 μm, respectively. GSK429286A significantly inhibited the expansion of rat aortic rings with an IC50 of 190 nM. GSK429286A reduced ROCK2 activity by 20-fold at a concentration of 1 μm. Under this condition, only MSK1 was significantly inhibited by other kinases tested, and its activity was reduced by ~ 5-fold. The specific kinase panel evaluation showed that GSK429286A is a more selective ROCK2 inhibitor than the widely used ROCK Inhibitor Y-27632, while LRRK2 was not significantly inhibited (IC50 500-fold higher than ROCK2 inhibition) even at a dose as high as 30 μm. Like GSK269962A, unlike sunitinib,10 μm GSK429286A treatment eliminated the phosphorylation of MYPT on Thr850 in HEK-293 cells induced by basal or G14V-Rho mutants, with a similar degree of action as H-1152 and Y-27632, consistent with ROCK-mediated phosphorylation, GSK429286A did not inhibit ERM protein phosphorylation whether G14V-Rho was present or not. |
| In vivo study | GSK429286A has an oral bioavailability of 61% in male Sprague-Dawley rats. Single oral administration of GSK429286A at 3-30 mg/kg significantly reduced mean arterial pressure in spontaneously hypertensive rats (SHRs) in a dose-dependent manner, approximately 2 hours after treatment at a dose of 30 mg/kg, maximum reduction 50 mmHg. |
N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - 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 |
N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.313 ml | 11.564 ml | 23.128 ml |
| 5 mM | 0.463 ml | 2.313 ml | 4.626 ml |
| 10 mM | 0.231 ml | 1.156 ml | 2.313 ml |
| 5 mM | 0.046 ml | 0.231 ml | 0.463 ml |
Last Update：2024-01-02 23:10:35
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View History
N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide
[4-(6-Chloro-4-trifluoromethyl-pyridin-2-yl)-benzyl]-diethyl-amine
伊利司莫
Phenol,2,2'-thiobis[4-chloro-6-[[(1,1-dimethylethyl)amino]methyl]-
(1,1-2H2)-1,1a-Dihydrobenzo[b]cyclopropa[e]pyran-7(7aH)-one
4878-36-8
3463-92-1
9-(2,4-Dichlorophenyl)-9H-purin-6-amine
Gly-Gly-Gly-Gly-Gly-OH
(2E,4E,6E,8E)-N-(4-Hydroxyphenyl)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenamide
[4-(6-Chloro-4-trifluoromethyl-pyridin-2-yl)-benzyl]-diethyl-amine
伊利司莫
Phenol,2,2'-thiobis[4-chloro-6-[[(1,1-dimethylethyl)amino]methyl]-
(1,1-2H2)-1,1a-Dihydrobenzo[b]cyclopropa[e]pyran-7(7aH)-one
4878-36-8
3463-92-1
9-(2,4-Dichlorophenyl)-9H-purin-6-amine
Gly-Gly-Gly-Gly-Gly-OH
(2E,4E,6E,8E)-N-(4-Hydroxyphenyl)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenamide