L748337,99.67%
产品编号:Bellancom-103211| CAS NO:244192-94-7| 分子式:C26H31N3O5S| 分子量:497.61
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L748337
产品介绍 | 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。 | ||||||||||||||||
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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. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases. | ||||||||||||||||
体外研究 |
L748337 (1 μM) inhibits iNOS expression in B16F10 cells. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 |
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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体内研究 |
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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性状 | Solid | ||||||||||||||||
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
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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。 | ||||||||||||||||
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) | ||||||||||||||||
参考文献 |
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