CGP 20712 A

(Synonyms: CGP 20712 mesylate)
目录号: PL14249
CGP 20712 A (CGP 20712 mesylate) 是一种高选择性 β1-adrenoceptor 拮抗剂,IC50 为 0.7 nM,是对 β2 肾上腺素受体的选择性约为 10,000 倍。
CAS No. :105737-62-0
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中文名称
CGP 20712 A
英文名称
CGP 20712 A
英文别名
CGP 20712A;1-[2-((3-CARBAMOYL-4-HYDROXY)PHENOXY)ETHYLAMINO]-3-[4-(1-METHYL-4-TRIFLUOROMETHYL-2-IMIDAZOLYL)PHENOXY]-2-PROPANOL DIHYDROCHLORIDE;CGP 20712 DIHYDROCHLORIDE;CGP-20712A methanesulfonate salt;2-hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)imidazol-2-yl]phenoxy]propyl]amino]ethoxy]benzamide,methanesulfonic acid;(±)-2-Hydroxy-5-[2-[[2-hydroxy-3-[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl]phenoxy]propyl] amino]ethoxy]-benzamide methanesulfonate salt;CGP 20712 A;CGP 20712 mesylate
Cas No.
105737-62-0
分子式
C23H25N4O5F3.CH4O3S
分子量
590.57
包装储存
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述
CGP 20712 A (CGP 20712 mesylate) 是一种高选择性 β1-adrenoceptor 拮抗剂,IC50 为 0.7 nM,是对 β2 肾上腺素受体的选择性约为 10,000 倍。
产品详情
CGP 20712 A (CGP 20712 mesylate) 是一种高选择性 β1-adrenoceptor 拮抗剂,IC50 为 0.7 nM,是对 β2 肾上腺素受体的选择性约为 10,000 倍。
生物活性
CGP 20712 A (CGP 20712 mesylate) is a highly selective β1-adrenoceptor antagonist with an IC 50 of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors.
性状
Solid
IC50 & Target[1][2]
IC50: 0.7 nM (β1-adrenoceptor)
体外研究(In Vitro)
In myocytes, the activation of adenylate cyclase causes by β2-adrenoceptors is not detected in the presence of 10 nM, 100 nM or 1000 nM CGP 20712 A (CGP 20712 mesylate), which selectively antagonized beta1-adrenoceptors. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Pretreatment of 8-day-old rats with 5 mg/kg CGP 20712 A do not change the plasma ACTH response to insulin injection. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Dooley DJ, et al. CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors. Eur J Pharmacol. 1986 Oct 14;130(1-2):137-9.
[2]. Kitagawa Y, et al. Determination of beta-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective beta-antagonists. Br J Pharmacol. 1995 Sep;116(1):1635-43.
溶解度数据
In Vitro: DMSO : 100 mg/mL (169.33 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Dooley DJ, et al. CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors. Eur J Pharmacol. 1986 Oct 14;130(1-2):137-9.
[2]. Kitagawa Y, et al. Determination of beta-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective beta-antagonists. Br J Pharmacol. 1995 Sep;116(1):1635-43.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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