L-161982

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

L-161982 是 EP4 受体的选择性拮抗剂。

L-161982 is a selective antagonist of the EP4 receptor.(In Vitro):In squamous carcinoma Tca8113 cells, L-161982 induces apoptosis and cell cycle arrest, and inhibits prostaglandin E2-induced proliferation . L-161982 (10 μM) blocks PGE2-stimulated cell proliferation of HCA-7 cells and ERK phosphorylation.(In Vivo):In collagen-induced arthritis (CIA) mice model, L-161982 (5 mg/kg; i.p.) reduces arthritis lesions and lesion progression. L-161982 shows less joint swelling and lower arthritis score after 35 days post immunization.

L-161982 (10 μM; 2 hours) blocks PGE2-stimulated cell proliferation of HCA-7 cells.L-161982 (10 μM; 1 hour) blocks PGE2-stimulated ERK phosphorylation in HCA-7 cells.L-161982 induces apoptosis, cell cycle arrest, and inhibits prostaglandin E2-induced proliferation in oral squamous carcinoma Tca8113 cells. Cell Proliferation Assay Cell Line:HCA-7 cells Concentration:10 μM Incubation Time:2 hours Result:Blocked PGE2-induced cell proliferation.

L-161982 (5?mg/kg; i.p.; once per day for 2 weeks) reduces arthritis lesions and lesion progression in CIA mice. Animal Model:Female DBA/1 mice of 6 to 8?weeks old (collagen-induced arthritis (CIA) mice model)Dosage:5?mg/kg Administration:i.p.; once per day for 2 weeks Result:Showed less joint swelling and lower arthritis score after 35?days post immunization.

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GPCR/G Protein

Prostaglandin Receptor

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147776-06-5

654.72

C32H29F3N4O4S2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (152.74 mM)

CCCCc1nn(-c2ccccc2C(F)(F)F)c(=O)n1Cc1ccc(cc1)-c1ccccc1S(=O)(=O)NC(=O)c1sccc1C

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(-20℃)

With Ice Pack

≥ 2 years