Description
GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9.
Product information
CAS Number: 892664-04-9
Molecular Weight: 429.22
Formula: C20H14Cl2FNNaO3
Chemical Name: 6-({5-chloro-2-[(4-chloro-2-fluorophenyl)methoxy]phenyl}methyl)pyridine-2-carboxylic acid sodium
Smiles: [Na].OC(=O)C1C=CC=C(CC2=CC(Cl)=CC=C2OCC2C=CC(Cl)=CC=2F)N=1 |^1:0|
InChiKey: JZFSUUQDZSQOHD-UHFFFAOYSA-N
InChi: InChI=1S/C20H14Cl2FNO3.Na/c21-14-6-7-19(27-11-12-4-5-15(22)10-17(12)23)13(8-14)9-16-2-1-3-18(24-16)20(25)26;/h1-8,10H,9,11H2,(H,25,26);
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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 ratand dog and high clearance in the monkey which is reflected in the half-life for each species.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.