GW 848687X

Confirm delete?

GW 848687X

Zoom

Cat No: 10010410

Biochemicals - Receptor Pharmacology

Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric pro...

This product can only be bought through Cayman Chemical. Please contact us.

Product Overview
Data
Downloads
About Cayman

Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

6-[2-[5-chloro-2-[(2,4-digluorophenyl)methoxy]phenyl]-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid

Correlated keywords:

Receptors EP1 PGE2 vasoconstriction bronchoconstriction hyperalgesia allodynia gastric protection relief hyperthermia sleep antagonists thromboxanes TP inflammation arthritis pain inflammatory GW848687X GW-848687X

Product Overview:
Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.{14997} Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.{14997} In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.{14997}

Size	500 µg
Shipping	dry ice
CAS Number	612831-24-0
Molecular Formula	C₂₄H₁₈ClF₂NO₃
SMILES	FC1=CC=C(COC2=C(C3=C(C4=CC=CC(C(O)=O)=N4)CCC3)C=C(Cl)C=C2)C(F)=C1
Molecular Weight	441,9
Formulation	A solution in methyl acetate
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

Technical File

MSDS

Click here to ask for your quote and get 15% off Cayman's products.

Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.