A selective EP3 antagonist (Ki = 0.8 nM); binds to the EP4 receptor (Ki = 715 nM) but does not bind to EP1 or EP2 receptors up to a concentration of 5

L-826,266 – 5 mg

Brand:
Cayman
CAS:
244101-03-9
Storage:
-20
UN-No:
Non-Hazardous - /

L-826,266 is a potent and selective competitive antagonist of the prostaglandin E2 receptor subtype EP3 (Ki = 0.8 nM).{9826} It also binds to the EP4 receptor (Ki = 715 nM) but does not bind to EP1 or EP2 receptors up to a concentration of 5,000 nM. L-826,266 inhibits vasoconstriction induced by the EP3 agonist sulprostone (Item No. 14765) in a concentration-dependent manner (EC50s = 0.45-24.5 µM in isolated human pulmonary arteries).{40626} It also inhibits sulprostone-induced norepinephrine and serotonin release in rat cortex and norepinephrine release in rat vas deferens (pA2s = 7.56, 7.67, and 7.87, respectively).{40635}  

 

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Description

A selective EP3 antagonist (Ki = 0.8 nM); binds to the EP4 receptor (Ki = 715 nM) but does not bind to EP1 or EP2 receptors up to a concentration of 5,000 nM; inhibits vasoconstriction induced by the EP3 agonist sulprostone (EC50s = 0.45-24.5 µM)

Formal name: (2E)-N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[5-chloro-2-(2-naphthalenylmethyl)phenyl]-2-propenamide

Synonyms: 

Molecular weight: 570.9

CAS: 244101-03-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area

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