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β3-AR agonist 1

Catalog No.GC37983

β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).

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β3-AR agonist 1 Chemical Structure

Cas No.: 1283125-73-4

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Sample solution is provided at 25 µL, 10mM.

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Background

β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold)[1]. EC50: 18 nM (β3-AR)[1]

β3-AR agonist 1 (compound 15) shows dose-dependent β3-AR-mediated responses in marmoset urinary bladder smooth muscle, has a desirable metabolic stability and pharmacokinetic profile (Cmax and AUC), and do not obviously affect heart rate or mean blood pressure when administered intravenously (3 mg/kg) to anesthetized rats[1].

[1]. Wada Y, et al. Discovery of Novel Indazole Derivatives as Orally Available β3-Adrenergic Receptor Agonists Lacking Off-Target-Based Cardiovascular Side Effects. J Med Chem. 2017 Apr 27;60(8):3252-3265.

Chemical Properties

Cas No. 1283125-73-4 SDF
Canonical SMILES O=S(NC1=CC([C@@H](O)CNCCOC2=CC(NN=C3C)=C3C=C2)=CC=C1)(C4CCC4)=O
Formula C22H28N4O4S M.Wt 444.55
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2495 mL 11.2473 mL 22.4947 mL
5 mM 0.4499 mL 2.2495 mL 4.4989 mL
10 mM 0.2249 mL 1.1247 mL 2.2495 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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