Cart
sales@molnova.com
GSK429286A
CAS No. 864082-47-3
GSK429286A( GSK429286A | GSK 429286A )
Catalog No. M17626 CAS No. 864082-47-3
GSK429286A is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 32 | In Stock |
|
| 5MG | 50 | In Stock |
|
| 10MG | 77 | In Stock |
|
| 25MG | 125 | In Stock |
|
| 50MG | 194 | In Stock |
|
| 100MG | 332 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NameGSK429286A
-
NoteResearch use only, not for human use.
-
Brief DescriptionGSK429286A is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
-
DescriptionGSK429286A is a selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.
-
In VitroGSK429286A 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.
-
In VivoGSK429286A 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.
-
SynonymsGSK429286A | GSK 429286A
-
PathwayOthers
-
TargetOther Targets
-
RecptorROCK1| ROCK2
-
Research AreaCancer
-
Indication——
Chemical Information
-
CAS Number864082-47-3
-
Formula Weight432.37
-
Molecular FormulaC21H16F4N4O2
-
Purity>98% (HPLC)
-
SolubilityDMSO : ≥ 51 mg/mL; 117.95 mM
-
SMILESCC1=C(C(CC(=O)N1)c1ccc(cc1)C(F)(F)F)C(=O)Nc1c(cc2c(c1)cn[nH]2)F
-
Chemical NameN-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Goodman KB, et al. J Med Chem, 2007, 50(1), 6-9.
molnova catalog
related products
-
Z-VRPR-FMK (TFA)
Z-VRPR-FMK (TFA) (VRPR) is a tetrapeptide and a selective and irreversible inhibitor of lymphoma translocation protein 1 (MALT1) in mucosa-associated lymphoid tissue.
-
MIF098
MIF098, a macrophage migration inhibitory factor (MIF) antagonist, inhibits pulmonary hypertension associated with SLE and the proliferation and migration of pulmonary arterial smooth muscle cells (PASMC).
-
Calcitonin (8-32), s...
Calcitonin (8-32), salmon is a highly selective amylin receptor antagonist.Calcitonin is a hormone known to participate in calcium and phosphorus metabolism. In mammals, the major source of calcitonin is from the parafollicular or C cells in the thyroid gland. Calcitonin is a 32 amino acid peptide cleaved from a larger prohormone.
