| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
L-748337 targets the β3-adrenergic receptor (β3-AR), a G protein-coupled receptor involved in the regulation of lipolysis, thermogenesis, and cardiovascular function. It is a selective and competitive antagonist with Ki values of 4 nM for β3, 390 nM for β1, and 204 nM for β2. By blocking β3-AR, it inhibits the receptor's signaling pathways and modulates the effects of β3-AR agonists.
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| ln Vitro |
In B16F10 cells, L748337 (1 μM) suppresses iNOS expression [1].
L-748337 is a potent β3-adrenergic receptor antagonist with a Ki of 4 nM for β3. It displays selectivity over β1 and β2 receptors. It activates MAPK signaling and promotes Erk1/2 phosphorylation. It inhibits the protective effects of CL316243. Its activity has been confirmed in various receptor binding and functional assays. |
| 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].
L-748337 is used in research on cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular-related diseases. Its ability to antagonize β3-AR and modulate signaling pathways makes it a valuable tool for studying the role of β3-AR in these conditions. However, specific in vivo efficacy data in animal models is limited. |
| Enzyme Assay |
The primary in vitro assay for L-748337 is a radioligand binding assay using membrane preparations from cells expressing β3, β1, or β2 adrenergic receptors. The compound's ability to displace a labeled ligand from these receptors is measured to determine its Ki values. Functional assays measure its ability to antagonize receptor-mediated signaling, such as the inhibition of cAMP accumulation.
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| Cell Assay |
In vitro cellular experiments for L-748337 involve treating cells expressing β3-AR with the compound and measuring its effects on receptor-mediated signaling. The inhibition of β3-AR-mediated cAMP production is assessed. Its effects on MAPK signaling and Erk1/2 phosphorylation are measured by Western blot.
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| 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. In vivo animal experiments for L-748337 are not extensively documented. As a β3-AR antagonist, it could be evaluated in animal models of cancer, NAFLD, or cardiovascular diseases. Its effects on disease progression and metabolic parameters would be assessed. |
| ADME/Pharmacokinetics |
L-748337 has a molecular weight of 497.61 g/mol and a molecular formula of C26H31N3O5S. It is a solid at room temperature. It is soluble in DMSO. It is typically stored at +4°C for short-term storage or at -20°C for long-term storage. Its purity is typically ≥98%.
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| Toxicity/Toxicokinetics |
L-748337 is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. As with all research chemicals, standard safety precautions should be followed when handling. Its safety would need to be established for therapeutic applications.
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| References |
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| Additional Infomation |
L-748337 is a selective and competitive β3-adrenergic receptor antagonist with Ki values of 4 nM for β3, 390 nM for β1, and 204 nM for β2. It is used in research on cancer, NAFLD, and cardiovascular diseases. The compound is available from various chemical suppliers for research purposes.
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| Molecular Formula |
C26H31N3O5S
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|---|---|
| Molecular Weight |
497.61
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| Exact Mass |
497.198
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| CAS # |
244192-94-7
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| PubChem CID |
10028830
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| Appearance |
White to off-white solid powder
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| LogP |
4.631
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
35
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| Complexity |
715
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(=O)NCC1=CC(=CC=C1)OC[C@H](CNCCC2=CC=C(C=C2)NS(=O)(=O)C3=CC=CC=C3)O
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| InChi Key |
AWIONHVPTYTSHZ-DEOSSOPVSA-N
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| 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
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| Chemical Name |
N-[[3-[(2S)-3-[2-[4-(benzenesulfonamido)phenyl]ethylamino]-2-hydroxypropoxy]phenyl]methyl]acetamide
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| Synonyms |
L748337; L 748337; L-748337
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~200.96 mM)
Ethanol : ~30 mg/mL (~60.29 mM) |
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| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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