(S)-Terazosin (Synonyms: (S)-特拉唑嗪)
目录号: PL14263 纯度: ≥99%
CAS No. :109351-33-9
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中文名称
(S)-Terazosin
中文别名
(S)-特拉唑嗪
英文名称
(S)-Terazosin
英文别名
Methanone,[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl][(2S)-tetrahydro-2-furanyl]-;Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[[(2S)-tetrahydro-2-furanyl]carbonyl]- (9CI);Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(tetrahydro-2-furanyl)carbonyl]-, (S)-;(S)-Terazosin;[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-[(2S)-oxolan-2-yl]methanone;MLS001165675;BIDD:GT0682;HMS2233L04;SMR000550495;A834431;[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]-[(2S)-2-oxolanyl]methanone;[4-(4-azanyl-6,7-dimethoxy-quinazolin-2-yl)piperazin-1-yl]-[(2S)-oxolan-2-yl]methanone;(S)-(4-(4-Ami
Cas No.
109351-33-9
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
(S)-Terazosin 是 Terazosin 的有活性的 S 型异构体,也是一种有效的,高亲和力的 α-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 3.91 nM,0.79 nM 和 1.16 nM。(S)-Terazosin 对 α2a,α2B 和 α2c-肾上腺素受体也具有高亲和力,Ki 值分别为 729 nM,3.5 nM 和 46.4 nM。
生物活性
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with K i values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with K i values of 729 nM, 3.5 nM and 46.4 nM, respectively.
性状
Solid
IC50 & Target[1][2]
Ki: 3.91 nM (α1a-adrenoceptor), 0.79 nM (α1b-adrenoceptor) and 1.16 nM (α1d-adrenoceptor); 729 nM (α2a-adrenoceptor), 3.5 nM (α2Ba-adrenoceptor) and 46.4 nM (α2c-adrenoceptor)
体外研究(In Vitro)
The racemic compound and its enantiomers show high and apparently equal affinity for subtypes of α1-adrenoceptors with Ki values in the low nanomolar range, and showed potent antagonism of α1-adrenoceptors in isolated tissues, with the enantiomers approximately equipotent to the racemate at each α1-adrenoceptor subtype. At α2b sites, (R)-Terazosin binds less potently than either the (S)-Terazosin or racemate. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(S)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC30 of 6.93. (s)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA2 values of 8.3 and 6.12, 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 : 150 mg/mL (387.17 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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