| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L409113-1ml |
1ml |
现货  |
|
| 别名 | 来曲唑 (CGS 20267) |
|---|---|
| 英文别名 | 4,4'-(1H-1,2,4-triazol-1-ylmethylene)bis-benzonitrile |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Letrozole (CGS 20267) |
| 生化机理 | 来曲唑（CGS 20267）是第三代芳香化酶抑制剂，在无细胞实验中的 IC50 值为 0.07-20 nM。在临床研究中，它对血浆中 17α-OH 孕酮、促甲状腺激素（TSH）、黄体生成素（LH）、促卵泡激素（FSH）或雄烯二酮的水平没有影响，也不影响正常的尿电解质排泄或甲状腺功能。来曲唑可诱导自噬。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 细胞色素 P450 19A1 抑制剂 |
| 产品介绍 |
Letrozole has been used: · in organoid growth assay to determine its inhibitory capacity(48) · to investigate steroid receptor coactivator-1 (SRC-1) mediated endogenous estrogen regulation of hippocampal PSD-95(49) · to determine its effects on tumor-induced hyperalgesia(50) · for hormonal manipulation in rats(51) · to study its effects on lipocalin-2 (Lcn2)(52) · to determine its effects on mechanical hyperalgesia and aromatase expression(53) Letrozole是非甾体类芳香酶抑制剂，其 IC50 为1-13 nM；是第三代aromatase抑制剂，无细胞试验中IC50为0.07-20 nM。在临床研究中，对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用，不影响正常的尿电解质排泄或甲状腺功能。 Information Letrozole (CGS 20267) Letrozole (CGS 20267) is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH Letrozole potently inhibits aromatase derived from a variety of different sources including human placental microsomes, particulate fractions of human breast cancer, rat ovarian microsomes, MCF-7 cells transfected with aromatase (MCF-7Ca), JEG-3 human choriocarcinoma cells , CHO cells, hamster ovarian tissue, and particulate fractions of human breast cancer with IC50 of 11, 2, 7, 0.07, 0.07, 1.4, 20 and 0.8 nM. In the non-cellular systems, the IC50 of letrozole is calculated to be 1-13 nM. Letrozole maximally inhibits estradiol production in vitro in LH-stimulated hamster ovarian tissue at 0.1 μM with an IC50 of 0.02 μM and does not significantly affect progesterone production up to 350 μM. In ACTH-stimulated rat adrenal tissue in vitro, aldosterone production is inhibited by with an IC50 of 210 μM. Letrozole inhibits growth of the MCF-7 epithelial breast cancer cells in a dose-dependent way with IC50 of 1 nM. Inhibition can be observesed even at the very low concentrations tested (0.1 nM). Treatment of normal MCF-12A epithelial cells with letrozole did not affect their growth even when high letrozole concentrations (100 nM) or prolonged culture times. Letrozole (10 nM) significantly suppressed the stimulatory effects of 4-androstene-3,17-dione (100 nM) or testosterone (100 nM) on MCF-7 cell proliferation. Concurrent administration of 17-β-estradiol with letrozole (10 nM) decreased the stimulatory effect of the enzymatic activity of MMP-2 and - 9 released by estradiol. In vivo Letrozole inhibits aromatase in vivo with ED50 of 1-3 μg/kg p.o.. Letrozole displays anti-endocrine effects. Letrozole inhibits androstenedione-induced uterine hypertrophy in immature rats with ED50 of 1-3 μg/kg. In the adult female rat, Letrozole (0.3-1 mg/kg daily p.o., 14 days) completely interrupts ovarian cyclicity and reduces uterine weight and serum estradiol (E2) concentrations to a similar extent to that seen after ovariectomy. Letrozole induces dose-dependent regression of estrogen-dependent, 9,10-dimethylbenz-a-anthracene (DMBA)-induced mammary tumors in adult female rats. The ED50 for Letrozole is determined to be 10 - 30 µg/kg/day, with complete inhibition at a daily dose of 10 µg/day. Letrozole produces dose-dependent inhibition of tumor growth of MCF-7 cells transfected with human aromatase gene (MCF-7Ca) implanted athymic nude mice, with complete inhibition at 20 mg/kg per day p.o.. cell lines： Concentrations：~100 nM Incubation Time：1 days Powder Purity:≥99% |
| ALogP | 2.749 |
|---|---|
| hba_count | 2 |
| Rotatable Bond | 3 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | N#CC1=CC=C(C=C1)C([N]2C=NC=N2)C3=CC=C(C=C3)C#N |
| 分子量 | 285.3 |
| Reaxy-Rn | 6813913 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6813913&ln= |
| DMSO(mg / mL) Max Solubility | 57 |
|---|---|
| DMSO(mM) Max Solubility | 199.79 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 6813913 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6813913&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | conforms to structure |
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