L748337

Research use only, not for human use.

L748337 is a competitive and potent β3-adrenoceptor antagonist that inhibits the action of β3-, β2-, and β1-adrenoceptors, activates MAPK signaling, promotes phosphorylation of Erk1/2, and inhibits the protective effects of CL316243, and is used in the study of disorders caused by abnormalities of the β3-adrenoceptors.

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.

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GPCR/G Protein

Adrenergic Receptor

Adrenergic Receptor

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244192-94-7

497.61

C26H31N3O5S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (200.96 mM; Ultrasonic )Ethanol : 30 mg/mL (60.29 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years