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) 抑制电场刺激引起的收缩反应^[2]。
L-798106 (10 μM) 抑制电场刺激引起的 ACh 释放^[2]。

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

L-798106 (口服灌胃；50 和 100 μg/kg；每天一次；8 周) 抑制 db/db 小鼠 的全身胰岛素抵抗和 AT 炎症^[3]。

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

536.44

C₂₇H₂₂BrNO₄S

244101-02-8

固体

White to off-white

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]