L748337 is a potent β3-adrenergic receptor blocker (antagonist) with selectivity for β1 and β2 receptors. The Kis of L748337 for β3-, β2-, and β1-adrenergic receptors are 4.0 nM, 204 nM, and 390 nM, respectively. L748337 mainly binds to Gi to activate MAPK signaling and increase the phosphorylation of Erk1/2, with pEC50 of 11.6. L748337 may be utilized in study/research of cancer, non-alcoholic fatty liver disease (NAFLD) and cardiovascular-related diseases.

Physicochemical Properties

Molecular Formula	C26H31N3O5S
Molecular Weight	497.61
Exact Mass	497.198
CAS #	244192-94-7
PubChem CID	10028830
Appearance	White to off-white solid powder
LogP	4.631
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	13
Heavy Atom Count	35
Complexity	715
Defined Atom Stereocenter Count	1
SMILES	CC(=O)NCC1=CC(=CC=C1)OC[C@H](CNCCC2=CC=C(C=C2)NS(=O)(=O)C3=CC=CC=C3)O
InChi Key	AWIONHVPTYTSHZ-DEOSSOPVSA-N
InChi Code	InChI=1S/C26H31N3O5S/c1-20(30)28-17-22-6-5-7-25(16-22)34-19-24(31)18-27-15-14-21-10-12-23(13-11-21)29-35(32,33)26-8-3-2-4-9-26/h2-13,16,24,27,29,31H,14-15,17-19H2,1H3,(H,28,30)/t24-/m0/s1
Chemical Name	N-[[3-[(2S)-3-[2-[4-(benzenesulfonamido)phenyl]ethylamino]-2-hydroxypropoxy]phenyl]methyl]acetamide
Synonyms	L748337; L 748337; L-748337
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In B16F10 cells, L748337 (1 μM) suppresses iNOS expression [1].
ln Vivo	L-748337 (ip; 5 mg/kg; 10 days until D18) decreases tumor vasculature in mice and inhibits the growth of melanoma caused by B16F10 cell inoculation [1].
Animal Protocol	Animal/Disease Models: 50 male C57BL/6 J mice (8 weeks old), carrying syngeneic B16F10 cells [1] Doses: 5 mg/kg Route of Administration: starting from day 10 until D18 Experimental Results: demonstrated anti-cancer effect.
References	[1]. 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]. 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]. 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.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~200.96 mM) Ethanol : ~30 mg/mL (~60.29 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (5.02 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0096 mL	10.0480 mL	20.0961 mL
	5 mM	0.4019 mL	2.0096 mL	4.0192 mL
	10 mM	0.2010 mL	1.0048 mL	2.0096 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.