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盐酸特拉唑嗪 /Terazosin HCl {[allProObj[0].p_purity_real_show]}

货号:A283609 同义名: Terazosin (hydrochloride);Hytrin

Terazosin HCl is a selective antagonist for alpha-adrenergic receptor, used for treatment for hypertension and prostate enlargement (BPH) through lowering the blood pressure with elimination half-life of ‎12 hours.

Terazosin HCl 化学结构 CAS号:63074-08-8
Terazosin HCl 化学结构
CAS号:63074-08-8
Terazosin HCl 3D分子结构
CAS号:63074-08-8
Terazosin HCl 化学结构 CAS号:63074-08-8
Terazosin HCl 3D分子结构 CAS号:63074-08-8
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Terazosin HCl 纯度/质量文件 产品仅供科研

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产品名称 Adrenergic Receptor α-adrenergic receptor β-adrenergic receptor 其他靶点 纯度
Ivabradine HCl 98%
Maprotiline hydrochloride 98%
Cisatracurium besylate 98%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine HCl 98%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

97%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Doxazosin mesylate 98%
Tolazoline HCl 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Terazosin HCl 生物活性

靶点
  • α-adrenergic receptor

描述 Terazosin hydrochloride is one of long-acting α-blockers and commonly used agent for treating BPH(benign prostatic hyperplasia) and/or hypertension. LD50s of terazosin were 277 and 293 mg kg−1 for male and female rats, respectively, after i.v. administration of the drug[3]. Use of oral terazosin hydrochloride (1.5 mg, orally or subcutaneously) elevated flap survival rates to control levels in nicotine-treated rats[4]. Moreover, terazosin reduces tumor vascularity and induces apoptosis in TCC(transitional cell carcinoma) of the bladder[5].

Terazosin HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00000620 Atherosclerosis ... 展开 >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease 收起 << Phase 3 Completed - United States, Minnesota ... 展开 >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada 收起 <<
NCT03339258 Stress Disorders, Post-Traumat... 展开 >>ic 收起 << Phase 2 Recruiting June 2021 United States, California ... 展开 >> San Francisco VA Medical Center Recruiting San Francisco, California, United States, 94121 Contact: Andrew Levihn-Coon, B.A.    415-221-4810 ext 23809    andrew.levihn-coon@va.gov 收起 <<
NCT01323998 - Completed - -

Terazosin HCl 参考文献

[1]Pan SL, Guh JH, et al. Identification of apoptotic and antiangiogenic activities of terazosin in human prostate cancer and endothelial cells. J Urol. 2003 Feb;169(2):724-9.

[2]Stone EA, Zhang Y, et al. Brain alpha 1-adrenergic neurotransmission is necessary for behavioral activation to environmental change in mice. Neuroscience. 1999;94(4):1245-52.

[3]Oh EY, Bae SK, Kwon JW, You M, Lee DC, Lee MG. Pharmacokinetic and pharmacodynamic consequences of inhibition of terazosin metabolism via CYP3A1 and/or 3A2 by DA-8159, an erectogenic, in rats. Br J Pharmacol. 2007 May;151(1):24-34. doi: 10.1038/sj.bjp.0707192. Epub 2007 Mar 12. PMID: 17351661; PMCID: PMC2012980.

[4]Karien RG, Maisel RH. Terazosin blockade of nicotine-induced skin flap necrosis in the rat. Arch Otolaryngol Head Neck Surg. 1997 Aug;123(8):837-40. doi: 10.1001/archotol.1997.01900080069008. PMID: 9260549.

[5]Tahmatzopoulos A, Lagrange CA, Zeng L, Mitchell BL, Conner WT, Kyprianou N. Effect of terazosin on tissue vascularity and apoptosis in transitional cell carcinoma of bladder. Urology. 2005 May;65(5):1019-23. doi: 10.1016/j.urology.2004.12.015. PMID: 15882756; PMCID: PMC2274913.

Terazosin HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.80mL

2.36mL

1.18mL

23.59mL

4.72mL

2.36mL

Terazosin HCl 技术信息

CAS号63074-08-8
分子式C19H26ClN5O4
分子量 423.894
别名 Terazosin (hydrochloride);Hytrin;A-45975;Hyprin;Vasocard;Terazocin HCl;Blavin;Fosfomic;Flumarc;Terazosine;Zayasel;Terazosin hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 16 mg/mL(37.75 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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