盐酸特拉唑嗪(二水合物) T6701

Product Introduction
Bioactivity


英文名: Terazosin hydrochloride dihydrate

描述: 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。

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]

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 25 mg/mL (54.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Inhibitor | bladder | Beta Receptor | inhibit | Flotrin Dihydrate | Terazosin HCl | Terazosin hydrochloride dihydrate | pressure | α1-adrenoceptor | Adrenergic Receptor | Heitrin | Dysalfa Dihydrate | Terazosin Hydrochloride | quinazoline | blood | Heitrin Dihydrate | benign | prostatic | Dysalfa | Flotrin | hyperplasia | Terazosin hydrochloride Dihydrate | high

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途