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/ Terazosin HCl/盐酸特拉唑嗪

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

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

Terazosin HCl 是一种选择性 α1-肾上腺素受体拮抗剂，适用于高血压及良性前列腺增生相关研究。

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

货号：A283609 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ 98%
Maprotiline HCl ✔ 98%
Cisatracurium besylate ✔ 96%
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 α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

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

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

 		98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		99%
Alfuzosin HCl ✔ 98%
Terazosin HCl ✔ 99%
Atipamezole ✔ 95%
Phentolamine methanesulfonate salt ✔ 99%
Carvedilol ✔ 99%
Doxazosin mesylate ✔ 99%
Tolazoline HCl ✔ 98%
Esmolol HCl ✔ 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

 		99%
Zenidolol HCl ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

 		98%
Acebutolol HCl ✔ 97+%
Carteolol HCl ✔ 98+%
Betaxolol ✔ 99%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

 		97%
Bisoprolol ✔ 97%
Sotalol HCl ✔ 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

 		99%
Metoprolol ✔ 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/盐酸特拉唑嗪 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/盐酸特拉唑嗪 细胞实验

Cell Line
Concentration Treated Time Description References
HeLa cells 1/2 MIC (2 mg/mL) 1 hour Evaluate the effect of Terazosin on S. Typhimurium invasion into HeLa cells. Terazosin significantly reduced bacterial invasion. Antibiotics (Basel). 2022 Mar 30;11(4):465
RAW264.7 macrophages 1/2 MIC (2 mg/mL) 16 hours Evaluate the effect of Terazosin on S. Typhimurium intracellular replication in macrophages. Terazosin significantly reduced bacterial intracellular replication. Antibiotics (Basel). 2022 Mar 30;11(4):465
RAW 264.7 cells 10 µM 18-24 hours TZ exhibited a protective effect against H2O2-induced apoptosis, as demonstrated by LDH release assay, active caspase-3 Western blot, and caspase activity assay. Nat Chem Biol. 2015 Jan;11(1):19-25
RAW 264.7 cells 10 µM 18-24 hours TZ suppressed apoptosis induced by LPS and IFN-γ, as verified by Annexin V staining and LDH release assay. Nat Chem Biol. 2015 Jan;11(1):19-25
Mouse embryonic stem cell-derived motor neurons (mESC-MNs) 0.625, 1.25, 2.5 µM 24 hours To evaluate the protective effect of Terazosin against oxidative stress-induced cell death, results showed Terazosin completely protected cells from death at the highest concentration EBioMedicine. 2022 Sep;83:104202
Human neuroblastoma cells 10 µM 24 hours Increased ATP content and reduced α-synuclein accumulation J Clin Invest. 2019 Oct 1;129(10):4539-4549
MIN6 cells 20 µM 24 hours Terazosin selectively activated GPR119, leading to increased cAMP and ATP synthesis, consequently enhancing insulin secretion. Cell Prolif. 2025 Mar;58(3):e13764
Caco-2 cells 10 and 100 nM 24 hours To evaluate the effect of Terazosin on cell viability under H2O2 and 2-DG-induced stresses, results showed that Terazosin significantly improved cell survival. Int J Mol Sci. 2021 Dec 30;23(1):416
Chromobacterium violaceum CV026 1/2 MIC (2 mg/mL) 24 hours Evaluate the effect of Terazosin on QS-controlled pigment production. Terazosin significantly reduced pigment release. Antibiotics (Basel). 2022 Mar 30;11(4):465
Hepatic microsomes 0.5, 1, 2, 5, 20, 50, 100 µM 30 minutes To determine the kinetic parameters (Vmax, Km, CLint) for the disappearance of terazosin in hepatic microsomes and evaluate the inhibitory effect of DA-8159 on its metabolism. Results showed that DA-8159 significantly reduced the metabolic rate of terazosin (Vmax decreased by 13.8%, CLint decreased by 62.0%). Br J Pharmacol. 2007 May;151(1):24-34

Terazosin HCl/盐酸特拉唑嗪 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice VTA 6-OHDA dopamine depletion model Oral administration via drinking water 0.03 mg/kg/day Daily administration for approximately 16 days To test the protective effect of Terazosin on PD-related cognitive dysfunction, results showed that Terazosin reduced interval timing variability in VTA dopamine-depleted mice NPJ Parkinsons Dis. 2023 Mar 2;9(1):32
Mice NAFPD model Intraperitoneal injection 1.5 mg/kg Daily for 6 weeks Terazosin treatment improved hyperglycemia, obesity, and pancreatic β-cell dysfunction in NAFPD mice. Cell Prolif. 2025 Mar;58(3):e13764
Female albino mice S. Typhimurium infection model Intraperitoneal injection 1/2 MIC (2 mg/mL) Single injection, observed for 5 days Evaluate the effect of Terazosin on S. Typhimurium pathogenesis. Terazosin significantly protected mice from S.Typhimurium pathogenesis. Antibiotics (Basel). 2022 Mar 30;11(4):465
Mice MPTP-induced PD model Intraperitoneal injection 10 μg/kg Once daily for 7 days Increased brain ATP levels, slowed or prevented neuron loss, partially restored dopamine levels and motor function J Clin Invest. 2019 Oct 1;129(10):4539-4549
Drosophila HS>rpr Drosophila model Oral 10 μM 24 hours TZ significantly improved the survival rate of HS>rpr flies, indicating its inhibitory effect on apoptosis. Nat Chem Biol. 2015 Jan;11(1):19-25
Zebrafish C9orf72 knockdown and TDP-43G348C overexpression models Added to water 2.5, 10, 50 µM From 6 hpf until analysis at 30 hpf To assess the ameliorative effect of Terazosin on motor neuron phenotypes, results showed Terazosin dose-dependently increased axon lengths EBioMedicine. 2022 Sep;83:104202
C57BL/6N mice DSS-induced ulcerative colitis and ethanol-induced gastric ulcer models Intraperitoneal injection (ulcerative colitis) and oral administration (gastric ulcer) 4 mg/kg/day (ulcerative colitis) and 1 mg/kg/day (gastric ulcer) Once daily for 7 days To evaluate the protective effects of Terazosin on ulcerative colitis and gastric ulcer, results showed that Terazosin significantly alleviated clinical symptoms and inflammatory responses. Int J Mol Sci. 2021 Dec 30;23(1):416
Sprague-Dawley rats Healthy male rats Intravenous and oral 5 mg/kg (i.v.); 5 mg/kg (p.o.) Single dose To evaluate the effect of DA-8159 on the pharmacokinetics and pharmacodynamics (blood pressure changes) of terazosin. Results showed that co-administration of DA-8159 and terazosin significantly increased the plasma concentration of terazosin (AUC increased by 57.4%-75.4%) and enhanced its blood pressure-lowering effect. Br J Pharmacol. 2007 May;151(1):24-34
SD rats and spontaneously hypertensive rats (SHRs) SD rats and SHRs Transdermal iontophoresis 7.5 mg/1.5 g TEH hydrogel 10 hours To evaluate the pharmacokinetic characteristics and antihypertensive effects of IDDS-TEH. Results showed that the blood concentration of IDDS-TEH was significantly higher than passive diffusion (p<0.05) and significantly reduced blood pressure in SHRs. Drug Deliv. 2021 Dec;28(1):454-462

Terazosin HCl/盐酸特拉唑嗪 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/盐酸特拉唑嗪 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/盐酸特拉唑嗪 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/盐酸特拉唑嗪 技术信息

CAS号63074-08-8
分子式C19H26ClN5O4
分子量 423.89
SMILES Code O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4OCCC4.[H]Cl
MDL No. MFCD00467965
别名 Terazosin (hydrochloride); Hytrin; A-45975; Hyprin; Vasocard; Terazocin HCl; Blavin; Fosfomic; Flumarc; Terazosine; Zayasel; Terazosin hydrochloride
运输蓝冰
InChI Key IWSWDOUXSCRCKW-UHFFFAOYSA-N
Pubchem ID 44383
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

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

Tags: Terazosin | 63074-08-8 | α1-Adrenoceptor Antagonist | GPCR/G Protein | Neuronal Signaling | Adrenergic Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Terazosin HCl/盐酸特拉唑嗪 纯度/质量文件 | Terazosin HCl/盐酸特拉唑嗪 亚型比较 | Terazosin HCl/盐酸特拉唑嗪 生物活性 | Terazosin HCl/盐酸特拉唑嗪 临床数据 | Terazosin HCl/盐酸特拉唑嗪 参考文献 | Terazosin HCl/盐酸特拉唑嗪 实验方案 | Terazosin HCl/盐酸特拉唑嗪 技术信息

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