A potent and selective EP4 receptor antagonist (Kis = 11.7

BGC 20-1531 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1962928-26-2
Storage:
-20
UN-No:
Non-Hazardous - /

BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively.{17141} It is selective for EP4, exhibiting 2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance with an ID50 value of 5 mg/kg in dogs.  

 

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SKU: 19742 - Category:

Description

A potent and selective EP4 receptor antagonist (Kis = 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively); selective for EP4, exhibiting 2-induced cAMP accumulation in HEK293 EBNA cells that stably express human EP4 receptors; reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle meningeal arterial rings; prevents PGE2-induced increases in carotid blood flow and decreases in carotid resistance in dogs (ID50 = 5 mg/kg)

Formal name: 4-[[4-(5-methoxy-2-pyridinyl)phenoxy]methyl]-5-methyl-N-[(2-methylphenyl)sulfonyl]-2-furancarboxamide, monohydrochloride

Synonyms:  PGN 1531

Molecular weight: 529

CAS: 1962928-26-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Vasculature|Vasoconstriction

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