Terazosin hydrochloride dihydrate

Terazosin hydrochloride dihydrate (Heitrin dihydrate) 是一种竞争性和口服活性的 α1-肾上腺素受体(α1-adrenoceptor) 拮抗剂,是一种喹唑啉衍生物,通过舒张血管和打开膀胱的方式起作用。它可用于研究良性前列腺增生 (BPH) 和高血压。

CAS号

70024-40-7

分子式

C19H25N5O4·HCl·2H2O

主要靶点

Adrenergic Receptor

仅限科研使用

Cat No : CM00539

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Synonyms

Heitrin dihydrate|Flotrin dihydrate|Dysalfa dihydrate|Terazosin HCl Dihydrate|盐酸特拉唑嗪(二水合物)



产品信息

Terazosin HCl is a selective α1-adrenoceptor antagonist, used for treatment of symptoms of an enlarged prostate (BPH).

CAS号 70024-40-7
分子式 C19H25N5O4·HCl·2H2O
主要靶点 Adrenergic Receptor
主要通路 G蛋白偶联受体|神经科学
分子量 459.92
纯度 99.97%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Heitrin dihydrate|Flotrin dihydrate|Dysalfa dihydrate|Terazosin HCl Dihydrate|盐酸特拉唑嗪(二水合物)

体内活性

Terazosin significantly inhibits vascular endothelial growth factor induced angiogenesis in nude mice with an IC50 of 7.9 mM, showing that it has a more potent anti-angiogenic than cytotoxic effect. Terazosin also effectively inhibits vascular endothelial growth factor induced proliferation and tube formation in cultured human umbilical vein endothelial cells (IC50 9.9 and 6.8 mM, respectively). [4]

体外活性

Terazosin results in a significant loss of cell viability, via induction of apoptosis in a dose-dependent manner in prostate cancer cells. Terazosin suppresses prostate growth potentially via α 1-adrenoceptor-independent actions gains further support from another study documenting that Doxazosin inhibits proliferation of human vascular smooth muscle cells independently of an antagonistic effect on α1-adrenoceptor. [1] Terazosin blocks HERG currents in Xenopus oocytes with IC50 of 113.2 mM, while Terazosin blocks HERG channel inhibition in human HEK 293 cells with IC50 of 17.7 mM. [2] Terazosin or genistein treatment inhibits the growth of DU-145 cells in a dose-dependent manner, whereas has no effect on normal prostate epithelial cells. Terazosin results in the genistein-induced arrest of DU-145 cells in G2/M phase being overridden and an increase in apoptotic cells, as evidenced by procaspase-3 activation and PARP cleavage. [3] Terazosin induces cytotoxicity in PC-3 and human benign prostatic cells with an IC50 of more than 100 mM. [4]

溶解度

Ethanol:<1 mg/mL,DMSO:25 mg/mL (54.4 mM),H2O:<1 mg/mL

参考文献

1.Kyprianou N, et al. Cancer Res. 2000 Aug 15;60(16):4550-5.
2.Thomas D, et al. Naunyn Schmiedebergs Arch Pharmacol,2004, 369(5), 462-472.
3.Chang KL, et al. Cancer Lett. 2009 Apr 8;276(1):14-20.
4.Pan SL, et al. J Urol,2003, 169(2), 724-729.

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