L748337

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

L748337  纯度: 96.41%

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。

L748337

L748337 Chemical Structure

CAS No. : 244192-94-7

规格 价格 是否有货 数量
5 mg ￥5300 In-stock
10 mg   询价  
50 mg   询价  

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L748337 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively[1]. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6[2]. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases[1][2][3].

IC50 & Target[1]

Beta-3 adrenergic receptor

4 nM (Ki)

Beta-2 adrenergic receptor

204 nM (Ki)

Beta-1 adrenergic receptor

390 nM (Ki)

体外研究
(In Vitro)

L748337 (1 μM) inhibits iNOS expression in B16F10 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

L-748337 (intraperitoneal injection; 5 mg/kg; beginning 10 days until D18) decreases the growth of melanoma induced by B16F10 cell inoculation and decreases tumor vasculature in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Fifty male C57BL/6 J mice (8 weeks of age) bearing syngeneic B16F10 cell[1]
Dosage: 5 mg/kg
Administration: Beginning 10 days until D18
Result: Exhibited anti-cancer effects.

分子量

497.61

Formula

C26H31N3O5S
CAS 号

244192-94-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

Ethanol : 30 mg/mL (60.29 mM; Need ultrasonic and warming)

DMSO : 25 mg/mL (50.24 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. S Neidhold, et al. 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]. Masaaki Sato, et al. 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]. Ziwen Wang, et al. 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.

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