(R)-Terazosin (Synonyms: (R)-特拉唑嗪)
目录号: PL05332 纯度: ≥99%
CAS No. :109351-34-0
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中文名称
(R)-Terazosin
中文别名
盐酸特拉唑嗪
英文名称
(R)-Terazosin
英文别名
Methanone,[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl][(2R)-tetrahydro-2-furanyl]-;Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(tetrahydro-2-furanyl)carbonyl]-, (R)-;Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[[(2R)-tetrahydro-2-furanyl]carbonyl]- (9CI);(R)-Terazosin
Cas No.
109351-34-0
分子式
C19H25N5O4
分子量
387.43
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
(R)-Terazosin 是 Terazosin 的活性 R 型对映体, 是一种有效的 α1-肾上腺素受体拮抗剂,对 α1a,α1b 和 α1d-肾上腺素受体的 Ki 值分别为 6.51 nM,1.01 nM 和 1.97 nM。
生物活性
(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with K i values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
性状
Solid
IC50 & Target[1][2]
Ki: 6.51 nM (α1a-adrenoceptor), 1.01 nM (α1b-adrenoceptor) and 1.97 nM (α1d-adrenoceptor)
体外研究(In Vitro)
(R)-Terazosin is low affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 3.85 μM, 0.33 μM and 0.37 μM, respectively.
(R)-Terazosin may prove to be a useful probe in understanding the functional role of subtypes of adrenoceptors in various tissues. Because it is a weaker antagonist at α2B sites than its enantiomer, it may be possible to use (R)-Terazosin to differentiate between pharmacological effects mediated by subtypes of α2-adrenoceptors in animal studies. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(R)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC 30 of 5.69. (R)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA 2 values of 7.5 and 5.31, respectively. 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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Hancock AA, et al. Actions of terazosin and its enantiomers at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro. J Recept Signal Transduct Res. 1995 Sep-Dec;15(7-8):863-85.
溶解度数据
In Vitro: DMSO : 75 mg/mL (193.58 mM; Need ultrasonic)配制储备液
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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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