864082-47-3
864082-47-3 structure
- Name: GSK429286A
- Chemical Name: N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide
- CAS Number: 864082-47-3
- Molecular Formula: C21H16F4N4O2
- Molecular Weight: 432.371
- Catalog: Biochemical Inhibitor Cell Cycle ROCK inhibitor
- Create Date: 2018-12-24 12:07:34
- Modify Date: 2024-01-02 11:36:25
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GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
| Name | N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide |
|---|---|
| Synonyms |
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydropyridine-3-carboxamide
cc-634 N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide dihydropyridone indazole amide 15 3-Pyridinecarboxamide, N-(6-fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]- S1474_Selleck GSK429286A |
| Description | GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM. |
|---|---|
| Related Catalog | |
| Target |
ROCK1:14 nM (IC50) RSK:780 nM (IC50) p70S6K:1940 nM (IC50) |
| In Vitro | GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM[2]. |
| In Vivo | GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg[1]. |
| Animal Admin | Rats: Spontaneously hypertensive rats (SHRs) are treated with GSK429286A to establish its effect on mean arterial pressure. Compound is administered by single dose oral gavage (3, 10, 30 mg/kg)[1]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 688.4±55.0 °C at 760 mmHg |
| Molecular Formula | C21H16F4N4O2 |
| Molecular Weight | 432.371 |
| Flash Point | 370.2±31.5 °C |
| Exact Mass | 432.120941 |
| PSA | 90.37000 |
| LogP | 3.97 |
| Appearance | white to beige |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.627 |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: ≥10mg/mL |
