L-748,337

Modify Date: 2024-01-17 15:32:59

L-748,337 Structure
L-748,337 structure
Common Name L-748,337
CAS Number 244192-94-7 Molecular Weight 497.60600
Density N/A Boiling Point N/A
Molecular Formula C26H31N3O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of L-748,337


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].

 Names

Name L-748,337,N-[[3-[(2S)-2-Hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide
Synonym More Synonyms

 L-748,337 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

[1]. S Neidhold, et al. The function of alpha- and beta-adrenoceptors of the saphenous artery in caveolin-1 knockout and wild-type mice. Br J Pharmacol. 2007 Feb;150(3):261-70.

[2]. Masaaki Sato, et al. The beta3-adrenoceptor agonist 4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-phenyl]-benzenesulfonamide (L755507) and antagonist (S)-N-[4-[2-[[3-[3-(acetamidomethyl)phenoxy]-2-hydroxypropyl]amino]-ethyl]phenyl]benzenesulfonamide (L748337) activate different signaling pathways in Chinese hamster ovary-K1 cells stably expressing the human beta3-adrenoceptor. Mol Pharmacol. 2008 Nov;74(5):1417-28.

[3]. Ziwen Wang, et al. The protective effects of the β3 adrenergic receptor agonist BRL37344 against liver steatosis and inflammation in a rat model of high-fat diet-induced nonalcoholic fatty liver disease (NAFLD). Mol Med. 2020 Jun 5;26(1):54.

 Chemical & Physical Properties

Molecular Formula C26H31N3O5S
Molecular Weight 497.60600
Exact Mass 497.19800
PSA 125.14000
LogP 4.63110

 Synonyms

L 748,337
6-Chloromelatonin
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