L748337
Cat. No.:YN322425
CAS No. :244192-94-7
产品名称: | L748337 |
CAS No.: | 244192-94-7 |
Chemical Name: | N-[[3-[(2S)-2-hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide |
Synonyms: | |
分子量: | 497.6 |
分子式: | C26H31N3O5S |
SMILES: | CC(NCC1=CC=CC(OC[C@@H](O)CNCCC2=CC=C(NS(C3=CC=CC=C3)(=O)=O)C=C2)=C1)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | L748337 是一种有效的 β3-肾上腺素能受体 (β3-adrenergic receptor) 拮抗剂,对 β1 和 β2 受体具有选择性。L748337 对 β3-、β2- 和 β1-肾上腺素受体的Ki值分别为 4.0 nM、204 nM 和 390 nM。L748337 主要与 Gi结合激活 MAPK 信号并增加 Erk1/2 的磷酸化,其 pEC50值为 11.6。L748337 可用于癌症、非酒精性脂肪性肝病 (NAFLD) 及心血管相关等疾病的研究。 |
IC50和靶点: | [{name:"Beta-3 adrenergic receptor:4 nM (Ki)"},{name: "Beta-2 adrenergic receptor:204 nM (Ki)"},{name: "Beta-1 adrenergic receptor:390 nM (Ki)"}] |
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Clinical Trial: | |
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Candelmore, M.R., Deng, L., Tota, L., et al.Potent and selective human β3-adrenergic receptor antagonistsJ. Pharmacol. Exp. Ther.290(2),649-655(1999)
Sato, M., Hutchinson, D.S., Evans, B.A., et al.The β3-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 β3-adrenoceptorMol. Pharmacol.74(5),1417-1428(2008)