L748337

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

L748337 是一种有效的 β3-肾上腺素能受体 (β3-adrenergic receptor) 拮抗剂，对 β1 和 β2 受体具有选择性。L748337 对 β3-、β2- 和 β1-肾上腺素受体的 Ki 值分别为 4.0 nM、204 nM 和 390 nM。L748337 主要与 Gi 结合激活 MAPK 信号并增加 Erk1/2 的磷酸化，其 pEC50 值为 11.6。L748337 可用于癌症、非酒精性脂肪性肝病 (NAFLD) 及心血管相关等疾病的研究。

L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over?β1?and?β2?receptors. The Ki values of L748337 for β3-,?β2- and?β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for theresearch of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.

L748337 (1 μM) inhibits iNOS expression in B16F10 cells.

L-748337 (intraperitoneal?injection; 5 mg/kg; beginning 10 days until D18) decreases the growth of melanoma induced by B16F10 cell inoculation and decreases tumor vasculature in mice.Animal Model:Fifty male C57BL/6 J mice (8 weeks of age) bearing syngeneic B16F10 cell Dosage:5 mg/kg Administration:Beginning 10 days until D18 Result:Exhibited anti-cancer effects.

——

GPCR/G Protein

Adrenergic Receptor

Adrenergic Receptor

——

——

244192-94-7

497.61

C26H31N3O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (200.96 mM; 超声助溶 ) Ethanol 中的溶解度 : 30 mg/mL (60.29 mM; 超声加热助溶)

CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)c1

——

(-20℃)

With Ice Pack

≥ 2 years