1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. GSK-269984A

GSK-269984A 

Cat. No.: HY-14467
Handling Instructions

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

For research use only. We do not sell to patients.

GSK-269984A Chemical Structure

GSK-269984A Chemical Structure

CAS No. : 892664-04-9

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Description

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

IC50 & Target[1]

EP1 Receptor

7.9 (pIC50)

In Vitro

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].

In Vivo

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 rat and dog and high clearance in the monkey which is reflected in the half-life for each species[1].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

429.22

Formula

C₂₀H₁₄Cl₂FNNaO₃

CAS No.

892664-04-9

SMILES

ClC1=CC(F)=C(COC2=CC=C(Cl)C=C2CC3=CC=CC(C(O)=O)=N3)C=C1.[Na]

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Product Name:
GSK-269984A
Cat. No.:
HY-14467
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GSK-269984A

Cat. No.: HY-14467