L-798106

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-798106 是强效且高度选择性的前列腺素类 EP3 受体拮抗剂 (Ki=0.3 nM)，它在 EP4，EP1 和 EP2 受体上也具有微摩尔活性，Ki 值分别为 916 nM，>5000 nM 和 >5000 nM。

L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has ?micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of916 nM, >5000 nM and >5000 nM, respectively.

L-798106 (200 nM) inhibits electrical field stimulation-induced contractile responses.L-798106 (10 μM) inhibits electrical field stimulation-evoked ACh release.Cell Viability Assay Cell Line:Guinea-pig vas deferens Concentration:200 nM Incubation Time:Result:Showed an apparent pA2 of 7.48±0.25.Cell Viability Assay Cell Line:Guinea-pig tracheal smooth muscle Concentration:10 μM Incubation Time:Result:Attenuated significantly the inhibitory effect of all agents tested (in % inhibition of EFS-induced release: 8-iso-PGE1 from 56.9 to 8.6; 8-iso-PGE2 from 51.6 to 9.2; PGE2 from 61.2 to 2.9; sulprostone from 55.9 to 18.8).

L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice.Animal Model:Male db/db mice Dosage:50 and 100 μg/kg Administration:Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks Result:Suppressed the increased fasting blood glucose levels in the db/db mice.Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of the db/db mice.

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GPCR/G Protein

Prostaglandin Receptor

Prostaglandin Receptor

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244101-02-8

536.44

C27H22BrNO4S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 10 mg/mL (18.64 mM; 超声助溶 )

COc1ccc(Br)cc1S(=O)(=O)NC(=O)\C=C\c1ccccc1Cc1ccc2ccccc2c1

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(-20℃)

With Ice Pack

≥ 2 years