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Description: Selective β3 antagonist
Chemical Name: N-[[3-[(2S)-2-Hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for L-748,337

L-748,337 is a competitive β3-adrenoceptor antagonist that displays selectivity over β1 and β2 receptors (Ki values are 4.0, 204 and 390 nM for β3-, β2- and β1-adrenoceptors respectively). Inhibits cAMP accumulation in response to Isoproterenol (IC50 = 6 nM). Reduces iNOS expression, attenuates nitric oxide-induced cell proliferation and induces apoptosis in a melanoma cell line.

Compound Libraries for L-748,337

L-748,337 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for L-748,337

M. Wt 497.61
Formula C26H31N3O5S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 244192-94-7
PubChem ID 10028830
Smiles O[C@H](COC2=CC=CC(CNC(C)=O)=C2)CNCCC1=CC=C(NS(=O)(C3=CC=CC=C3)=O)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for L-748,337

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 49.76 100
ethanol 4.98 10

Preparing Stock Solutions for L-748,337

The following data is based on the product molecular weight 497.61. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.01 mL 10.05 mL 20.1 mL
5 mM 0.4 mL 2.01 mL 4.02 mL
10 mM 0.2 mL 1 mL 2.01 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets for L-748,337

Certificate of Analysis / Product Datasheet
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References for L-748,337

References are publications that support the biological activity of the product.

Candelore et al (1999) Potent and selective human β3-adrenergic receptor antagonist. J.Pharmacol.Exp.Ther. 290 649 PMID: 10411574

Neidhold et al (2007) The function of α- and β-adrenoceptors of the saphenous artery in caveolin-1 knockout and wild-type mice. Br.J.Pharmacol. 150 261 PMID: 17179950

Dal Monte et al (2014) β3-adrenergic receptor activity modulates melanoma cell proliferation and survival through nitric oxide signaling. Naunyn Schmiedebergs Arch.Pharmacol. 387 533 PMID: 24599317

If you know of a relevant reference for L-748,337, please let us know.

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Citations for L-748,337

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Literature in this Area

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Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.