L-798106  (Synonyms: CM9; GW671021)

L-798106 is potent and highly selective prostanoid EP₃ receptor antagonist (K_i=0.3 nM), it also has micromolar activities at the EP₄, EP₁ and EP₂ receptors with K_i values of 916 nM, >5000 nM and >5000 nM, respectively^[1].

L-798106 (200 nM) inhibits electrical field stimulation-induced contractile responses^[2].
L-798106 (10 μM) inhibits electrical field stimulation-evoked ACh release^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

536.44

C₂₇H₂₂BrNO₄S

244101-02-8

Solid

White to off-white

O=C(NS(=O)(C1=CC(Br)=CC=C1OC)=O)/C=C/C2=CC=CC=C2CC3=CC=C4C=CC=CC4=C3

Room temperature in continental US; may vary elsewhere.

• [1]. Juteau H, et al. Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor. Bioorg Med Chem. 2001 Aug;9(8):1977-84.  [Content Brief]

  [2]. Deborah L Clarke, et al. E-ring 8-isoprostanes inhibit ACh release from parasympathetic nerves innervating guinea-pig trachea through agonism of prostanoid receptors of the EP3-subtype. Br J Pharmacol. 2004 Feb;141(4):600-9.  [Content Brief]

  [3]. Pei-Chi Chan, et al. Importance of adipocyte cyclooxygenase-2 and prostaglandin E2-prostaglandin E receptor 3 signaling in the development of obesity-induced adipose tissue inflammation and insulin resistance. FASEB J. 2016 Jun;30(6):2282-97.  [Content Brief]