L-748,337
Names
Biological Activity
[Description]:
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[1]. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6[2]. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases[1][2][3].
[Related Catalog]:
[Target]
Beta-3 adrenergic receptor:4 nM (Ki)
Beta-2 adrenergic receptor:204 nM (Ki)
Beta-1 adrenergic receptor:390 nM (Ki)
[In Vitro]
L748337 (1 μM) inhibits iNOS expression in B16F10 cells[1].
[In Vivo]
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[1]. Animal Model: Fifty male C57BL/6 J mice (8 weeks of age) bearing syngeneic B16F10 cell[1] Dosage: 5 mg/kg Administration: Beginning 10 days until D18 Result: Exhibited anti-cancer effects.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C26H31N3O5S
[ Molecular Weight ]:
497.60600
[ Exact Mass ]:
497.19800
[ PSA ]:
125.14000
[ LogP ]:
4.63110