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GSK-269984A Catalog No.GC30307

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1mg
$1,174.00
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5mg
$1,878.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Animal experiment:

Rats are used in this study. GSK-269984A is progressed to the rat CFA model of inflammatory pain. GSK-269984A is dosed orally at doses of 1, 3 and 10 mg/kg, 23 h after intraplantar administration of the adjuvant. Analgesia is assessed 1 h post-dose of GSK-269984A[1].

References:

[1]. Hall A, et al. Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain. Bioorg Med Chem Lett. 2009 May 1;19(9):2599-603.

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Chemical Properties

Cas No. 892664-04-9 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES ClC1=CC(F)=C(COC2=CC=C(Cl)C=C2CC3=CC=CC(C(O)=O)=N3)C=C1.[Na]
Formula C20H14Cl2FNNaO3 M.Wt 429.22
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9.

Results from [3H]-PGE2 binding assay in CHO cells overexpressing the human EP1 receptor demonstrate that GSK-269984A is an antagonist of EP1 receptor with a pIC50 of 7.9. GSK-269984A is found to cause a concentration-dependent rightward shift of the PGE2 dose-response curve and Schild analysis shows that GSK-269984A is a competitive antagonist with pA2 8.1±0.3 and slope 1.0[1].

GSK-269984A demonstrates an ED50 of 2.6 mg/kg (po), with the 10 mg/kg dose showing equivalent reversal of hypersensitivity to the standard. GSK-269984A displays moderate blood clearance in the ratand dog and high clearance in the monkey which is reflected in the half-life for each species[1].

[1]. Hall A, et al. Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain. Bioorg Med Chem Lett. 2009 May 1;19(9):2599-603.