244192-94-7

244192-94-7 structure

Name: L-748,337
Chemical Name: L-748,337,N-[[3-[(2S)-2-Hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide
CAS Number: 244192-94-7
Molecular Formula: C₂₆H₃₁N₃O₅S
Molecular Weight: 497.60600
Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
Create Date: 2016-10-14 03:33:18
Modify Date: 2024-01-17 15:32:59
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].

Name	L-748,337,N-[[3-[(2S)-2-Hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide
Synonyms	L 748,337 6-Chloromelatonin

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	Research Areas >> Cancer Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Metabolic Disease
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.

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

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