GSK429286A

This product is for research use only, not for human use. We do not sell to patients.

GSK429286A
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Size Price Stock
100mg$550Check With Us
250mg$1050Check With Us
500mg$1575Check With Us

Cat #: V1345 CAS #: 864082-47-3 Purity ≥ 98%

Description: GSK429286A (also known as RHO15; GSK 429286A; RHO-15; GSK-429286A) is a potent, orally bioactive, and selective inhibitor of ROCK1/2 with antihypertensive effects.

References: Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60.

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Molecular Weight (MW)432.37
Molecular FormulaC21H16F4N4O2
CAS No.864082-47-3
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 87 mg/mL (201.2 mM)r
Water:<1 mg/mLr
Ethanol: 4 mg/mL (9.23mM)
Solubility In Vivo15% Captisol+citrate vehicle: 15 mg/mL
SynonymsRHO-15; GSK429286A; RHO15; GSK 429286A; RHO 15; GSK-429286A; GSK429286 A; GSK 429286-A; GSK-429286-A
ProtocolIn 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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.3128 mL11.5642 mL23.1283 mL46.2567 mL
5mM0.4626 mL2.3128 mL4.6257 mL9.2513 mL
10mM0.2313 mL1.1564 mL2.3128 mL4.6257 mL
20mM0.1156 mL0.5782 mL1.1564 mL2.3128 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.