Letrozole
(Synonyms: 来曲唑; CGS 20267) 目录号 : GC10726
An aromatase inhibitor
Cas No.:112809-51-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Letrozole is a novel and potent type (II) aromatase inhibitor with IC50 of 11.5 nM. It belongs to the reversible non-steroidal compound family which can inhibit Arom. However, there is no evidence that it can affect the adrenal steroidogenesis.[1]
Normally, Type II inhibitors have a common feature of heterocyclic azole moiety, which can be binded to the heme–iron in aromatase. It contains a structure of 1,2,4-triazole moieties which can coordinate the heme–iron of cytochrome P450. Meanwhile, benzonitrile substituted letrozole can mimic a unique enzyme structure of the substrate androstenedione.[2]
Letrozole administration can reduce spine synapse and axon outgrowth and it also will decrease the expression of estrogen receptor (ER). While, the synaptic proteins including GAP-43 can impaire the long-termpotentiation.[1] Letrozole is proved to promote FSH release from the hypothalamic pituitary axis by responding to decreased estrogen (E) feedback.[3]
References:
[1] Chen Bian, Yangang Zhao, Qiang Guo, Ying Xiong, Wenqin Cai, Jiqiang Zhang. Aromatase inhibitor letrozole downregulates steroid receptor coactivator-1 in specific brain regions that primarily related to memory, neuroendocrine and integration. The Journal of Steroid Biochemistry and Molecular Biology. May 2014. 141: 37-43.
[2] Hakki Türker Akçay, Riza Bayrak. Computational studies on the anastrozole and letrozole, effective chemotherapy drugs against breast cancer. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy. 25 March 2014. 122: 142-152.
[3] Lindsay Malloch, Alice Rhoton-Vlasak. An assessment of current clinical attitudes toward letrozole use in reproductive endocrinology practices. Fertility and Sterility. December 2013. 100(6): 1740-1744.
| Cas No. | 112809-51-5 | SDF | |
| 别名 | 来曲唑; CGS 20267 | ||
| 化学名 | 4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile | ||
| Canonical SMILES | C1=CC(=CC=C1C#N)C(C2=CC=C(C=C2)C#N)N3C=NC=N3 | ||
| 分子式 | C17H11N5 | 分子量 | 285.3 |
| 溶解度 | ≥ 14.265mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5051 mL | 17.5254 mL | 35.0508 mL |
| 5 mM | 0.701 mL | 3.5051 mL | 7.0102 mL |
| 10 mM | 0.3505 mL | 1.7525 mL | 3.5051 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。