GSK2239633A

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

GSK2239633A
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Size Price Stock
50mg$750Check With Us
100mg$1250Check With Us
200mg$1875Check With Us

Cat #: V3603 CAS #: 1240516-71-5 Purity ≥ 98%

Description: GSK2239633A (GSK-2239633A), a 4-aminoindazole sulfonamide, is a novel and potent antagonist of human CC-chemokine receptor 4 (CCR4) with anti-inflammatory activity.

References: Cahn A, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study. BMC Pharmacol Toxicol. 2013 Feb 28;14:14.

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Molecular Weight (MW)549.06
Molecular FormulaC24H25ClN4O5S2
CAS No.1240516-71-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
ProtocolIn VitroThe GSK2239633A is an allosteric antagonist of human CCR4. GSK2239633A inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96±0.11 and also inhibits thymus- and activation-regulated chemokine-induced (TARC)-induced increases in the F-actin content of isolated human CD4+ CCR4+ T-cells with a pA2 of 7.11±0.29[1]. The effect of GSK2239633A (Compound 3) on CCL17-induced increases in the F-actin content of human CD4+ CCR4+ T cells is measured. The pEC50 value is 8.79±0.22
In VivoFollowing intravenous dosing, plasma GSK2239633A displays rapid, bi-phasic distribution and slow terminal elimination (t1/2: 13.5 hours), suggesting that GSK2239633A is a low to moderate clearance drug. Following oral dosing, blood levels of GSK2239633A reach Cmax rapidly (median tmax: 1.0-1.5 hours). Estimated GSK2239633A bioavailability is low with a maximum value determined of only 16%
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
1mM1.8213 mL9.1065 mL18.2129 mL36.4259 mL
5mM0.3643 mL1.8213 mL3.6426 mL7.2852 mL
10mM0.1821 mL0.9106 mL1.8213 mL3.6426 mL
20mM0.0911 mL0.4553 mL0.9106 mL1.8213 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Concentration
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Volume
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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
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Volume(start)
V1
=
Concentration(final)
C2
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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.