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My CartCAS：70024-40-7
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 70024-40-7 |
| Name | Terazosin Hydrochloride Dihydrate |
| Molecular Formula | C19H30ClN5O6 |
| Molecular Weight | 459.92 |
| Solubility | Soluble in DMSO(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00941408 |
| SMILES | COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4CCCO4)N)OC.O.O.Cl |
| InChIKey | NZMOFYDMGFQZLS-UHFFFAOYSA-N |
| InChI | InChI=1S/C19H25N5O4.ClH.2H2O/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14;;;/h10-11，14H，3-9H2，1-2H3，(H2，20，21，22);1H;2*1H2 |
| PubChem CID | 63016 |
| Target Point | Adrenergic Receptor |
| Passage | Endocrinology & Hormones;GPCR & G Protein；Neuronal Signaling |
| Background | It is a competitive α1-adrenoceptor antagonist. It can be used in the study of benign prostatic hyperplasia (BPH) and hypertension. |
| Biological Activity | Terazosin Hydrochloride Dihydrate 是一种长效选择性α1-肾上腺素受体拮抗剂，也能阻断 HERG 钾通道，具有治疗前列腺癌的活性。[1-5] |
| In Vitro | 盐酸特拉唑嗪二水合物不能区分大鼠肾脏和大脑皮层、COS 细胞和人类前列腺中的α1-肾上腺素受体亚型[1]。特拉唑嗪通过诱导前列腺癌细胞凋亡以剂量依赖的方式导致细胞活力显著下降，凋亡活性与它们拮抗α1-肾上腺素受体的能力无关[2]。特拉唑嗪阻断爪蟾卵母细胞中的 HERG 电流的 IC(50)值为113.2 μmol，抑制人 HEK 293 细胞中 HERG 通道的 IC(50)值为17.7 μmol。特拉唑嗪能阻断 HERG 钾通道[3]。特拉唑嗪以剂量依赖的方式抑制了 DU-145 细胞的生长，但对正常前列腺上皮细胞没有影响；加入 1 μg/mL的特拉唑嗪(单独使用无活性)可增强 5 μg/mL的染料木素的生长抑制作用；与特拉唑嗪联合处理可使染料木素诱导的 DU-145 细胞停滞在 G2/M 期，并使凋亡细胞增加；与单用染料木素相比，联合用药还能显著降低细胞凋亡调节蛋白 Bcl-XL、血管内皮生长因子 165 和血管内皮生长因子 121 的水平[4]。特拉唑嗪可诱导 PC-3 细胞和人类良性前列腺细胞产生细胞毒性，IC50 值超过 100 μmol；特拉唑嗪能明显抑制血管内皮生长因子诱导的裸鼠血管生成，其 IC50 值为 7.9 μmol；特拉唑嗪还能有效抑制血管内皮生长因子诱导的人脐静脉内皮细胞增殖和管形成(IC50 分别为 9.9 和 6.8 μmol)[5]。 |
| In Vivo | 对携带 PC-3 前列腺癌异种移植体的 SCID 小鼠施用多沙唑嗪可显著抑制肿瘤生长[2]。 |
| Data Literature Source | [1]. Michel MC，et al. Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol. 1996 Feb;16(1):21-8. [2]. Kyprianou N，et al. Suppression of human prostate cancer cell growth by alpha1-adrenoceptor antagonists doxazosin and terazosin via induction of apoptosis. Cancer Res. 2000 Aug 15;60(16):4550-5. [3]. Thomas D，et al. Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin，doxazosin，and terazosin. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):462-72. [4]. Chang KL，et al. Combined effects of terazosin and genistein on a metastatic，hormone-independent human prostate cancer cell line. Cancer Lett. 2009 Apr 8;276(1):14-20. [5]. Pan SL，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. |
| Unit | Bottle |
| Specification | 100mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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