L-798,106

Prostaglandin E2 (Item No. 14010) exerts its effects through four separate G-protein coupled receptors (EP1, EP2, EP3, and EP4).1 L-798,106 is a highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively.2 At 0.2 µM, it blocks the EP3 agonist activity of sulprostone (Item No. 14765) on guinea pig vas deferens and trachea.3WARNING This product is not for human or veterinary use.

A selective EP3 receptor antagonist

536.4

≥95%

Biochemicals/Receptor Pharmacology/Antagonists

Formal_Name:(2E)-N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-2-propenamide;Synonyms:CM 9 GW 671021

O=C(NS(C1=C(OC)C=CC(Br)=C1)(=O)=O)/C=C/C2=CC=CC=C2CC3=CC4=C(C=C3)C=CC=C4

C27H22BrNO4S

244101-02-8

≥ 4 years

Acetonitrile: 1 mg/ml DMF: 20 mg/ml DMSO: 10 mg/ml

1.Coleman, R.A.,Smith, W.L. and Narumiya, S. Classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacological Reviews 46, 205-229 (1994).
2.Juteau, H.,Gareau, Y.,Labelle, M., et al. Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP₃ prostanoid receptor. Bioorganic & Medicinal Chemistry 9, 1977-1984 (2001).
3.Jones, R.L.,Giembycz, M.A. and Woodward, D.F. Prostanoid receptor antagonists: Development strategies and therapeutic applications. British Journal of Pharmacology 158(1), 104-145 (2009).