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My CartCAS：120511-73-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 120511-73-1 |
| Name | Anastrozole |
| Molecular Formula | C17H19N5 |
| Molecular Weight | 293.37 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 601-715-6 |
| MDL | MFCD00866298 |
| SMILES | CC(C)(C#N)C1=CC(C(C)(C#N)C)=CC(CN2C=NC=N2)=C1 |
| InChIKey | YBBLVLTVTVSKRW-UHFFFAOYSA-N |
| InChI | InChI=1S/C17H19N5/c1-16(2,9-18)14-5-13(8-22-12-20-11-21-22)6-15(7-14)17(3,4)10-19/h5-7,11-12H,8H2,1-4H3 |
| PubChem CID | 2187 |
| Target Point | Aromatase |
| Passage | Endocrinology & Hormones |
| Background | Anastrozole is a selective aromatase inhibitor. |
| Biological Activity | Anastrozole 是一种选择性的芳香酶 (aromatase) 抑制剂，抑制胎盘芳香化酶，IC50 为 15 nM。[1] |
| In Vitro | Anastrozole是一种比较简单的非手性苄基三唑衍生物，可抑制人胎盘芳香化酶，IC50为15 nM。在同一试验中，它的效力是氨基乙酰亚胺(AG)的200倍，效力是4-OHA的两倍，三分之一是有效的Fadrozole [1]。 |
| In Vivo | 在第4天，在有或没有各种剂量的Anastrozole口服的情况下，每天给8只未成熟(22日龄)雌性大鼠的雄烯雄酮(AD)(30mg/kg)在花生油sc中给予3天，子宫被解剖，印迹和称重。在该周期的第2天或第3天给予0.1mg/kgAnastrozole的口服剂量完全阻断排卵。在相同的每日剂量(0.1mg/kg)下，Anastrozole完全消除了未成熟大鼠中外源性AD的子宫营养活性。在雄性尾壳猴中，每天两次口服0.1 mg/kg及以上的Anastrozole可使循环雌二醇浓度降低50-60％[1]。 |
| Animal Experiment | 小鼠[1]至少8只成年雌性大鼠的组，在受控照明(06.00-20.00小时)和温度(24±2℃)下饲养并进行4天的发情周期，用单剂量的Anastrozole治疗在第2天16.00小时或第3天在12.00小时(0.01-0.1mg/kg)，法倔唑(0.01-0.1mg/kg)或AG(5-20mg/kg)。然后确定在下一个周期的第1天在输卵管中是否存在卵。当没有发现卵子时，排卵被认为是阻塞的。 |
| Kinase Experiment | 使用人胎盘微粒体和Thompson和Siiteri以睾酮(0.5μM)作为底物的方法测量芳香酶抑制。通过使用来自豚鼠，狗和牛肾上腺的新鲜制备的线粒体测量[1，2，6，7-3H] - 烯 - 脱氧 - 皮质醇向皮质醇的转化来确定11-羟化酶抑制。将反应产物萃取到氯仿中并通过薄层色谱法分离[1]。 |
| Data Literature Source | [1]. Dukes M，et al. The preclinical pharmacology of 'Arimidex' (anastrozole; ZD1033)--a potent，selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45. |
| Unit | Bottle |
| Specification | 20mg 50mg 100mg |
Anastrozole 是一种选择性的芳香酶 (aromatase) 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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