| Description | L-798106 (CM9) is a selective and potent prostaglandin-like EP3 receptor antagonist that inhibits EP4, EP1, and EP2 receptors, suppresses levels of pro-inflammatory cytokines in atherosclerosis, and attenuates PGE2-induced cough. |
| In vitro | 在豚鼠输精管中，L-798106（200 nM）显示出表观 pA2 为 7.48±0.25[2]。 |
| In vivo | 在雄性 db/db 小鼠中，L-798106（ 50 和 100 μg/kg；口服灌胃；每日一次；8 周）能够抑制 db/db 小鼠中增加的空腹血糖水平，并抑制从 db/db 小鼠附睾脂肪组织分离的脂肪细胞中增加的促炎基因表达[3]。 |
| Target activity | EP1/2 receptor:> 5000 nM(ki), EP3 receptor: 0.3 nM(ki), EP4 receptor:916 nM(ki), EP3 receptor:0.3 nM(Ki), EP4 receptor:916 nM(Ki), EP1/2 receptor:> 5000 nM(Ki) |
| Synonyms | L 798106, CM9, GW-671021, CM-9, GW671021 |
| molecular weight | 536.44 |
| Molecular formula | C27H22BrNO4S |
| CAS | 244101-02-8 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5 mg/mL (9.32 mM), Sonication is recommended. |
| References | 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. 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. 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. |