| Identification | Back Directory | [Name]
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide | [CAS]
864082-47-3 | [Synonyms]
RHO-15
CS-557
GSK 429286 A
RHO-15(GSK429286A)
GSK 429286A;GSK-429286A;RHO-15
GSK429286A;GSK-429286A;GSK 429286A
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)-phenyl)-1,4,5,6-tetrahydrop
N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide
N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide
3-Pyridinecarboxamide, N-(6-fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide USP/EP/BP
GSK 429286 A
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide GSK 429286 A | [Molecular Formula]
C21H16F4N4O2 | [MDL Number]
MFCD16618404 | [MOL File]
864082-47-3.mol | [Molecular Weight]
432.37 |
| Chemical Properties | Back Directory | [Boiling point ]
688.4±55.0 °C(Predicted) | [density ]
1.468 | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥10mg/mL | [form ]
powder | [pka]
12.10±0.40(Predicted) | [color ]
white to beige | [InChIKey]
OLIIUAHHAZEXEX-UHFFFAOYSA-N | [SMILES]
C1(C)NC(=O)CC(C2=CC=C(C(F)(F)F)C=C2)C=1C(NC1C(F)=CC2=C(C=1)C=NN2)=O | [CAS DataBase Reference]
864082-47-3 |
| Hazard Information | Back Directory | [Uses]
GSK 429286 is a selective Rho-kinase (ROCK) inhibitor.It is orally available and has been shown to dramatically reduce mean arterial pressure in spontaneously hypertensive rats. | [Definition]
ChEBI: N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide is a member of (trifluoromethyl)benzenes. | [Biological Activity]
gsk429286a is a selective inhibitor of rock1 and rock2 with ic50 value of 14 nm and 63 nm, respectively [1].rho-kinase (rock) is a member of agc (protein kinase a, protein kinase g and protein kinase c) family and plays an important role in promoting actin-myosin-mediated contractile force generation [2].gsk429286a is a potent rock inhibitor and has a different activity with the reported rock inhibitor y27632. using gst method, it is shown that gsk429286a treatment (10 μm) increased mypt phosphrylation at thr850 via inhibiting rock which mediated this phosphorylation process [3].in male sprague-dawley rat model with spontaneously hypertensive, oral administration of gsk429286a (30 mg/kg) marks reduced mean arterial pressure and the maximum decreased was as 50 mmhg after nearly 2 h treatment [4]. | [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]. | [IC 50]
ROCK1: 14 nM (IC50); RSK: 780 nM (IC50); p70S6K: 1940 nM (IC50) | [storage]
Store at -20°C | [References]
[1]. nichols, r.j., et al., substrate specificity and inhibitors of lrrk2, a protein kinase mutated in parkinson's disease. biochem j, 2009. 424(1): p. 47-60.
[2]. shi, j., et al., distinct roles for rock1 and rock2 in the regulation of cell detachment. cell death dis, 2013. 4: p. e483.
[3]. davis, d.a., et al., increased therapeutic potential of an experimental anti-mitotic inhibitor sb715992 by genistein in pc-3 human prostate cancer cell line. bmc cancer, 2006. 6: p. 22.
[4]. goodman, k.b., et al., development of dihydropyridone indazole amides as selective rho-kinase inhibitors. j med chem, 2007. 50(1): p. 6-9. |
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