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17β-hydroxy Exemestane-d3 Sale

目录号 : GC46471

A neuropeptide with diverse biological activities

17β-hydroxy Exemestane-d3 Chemical Structure

规格 价格 库存 购买数量
500 μg
¥2,998.00
现货
1 mg
¥5,106.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

17β-hydroxy Exemestane-d3 is intended for use as an internal standard for the quantification of 17β-hydroxy exemestane and as a surrogate internal standard for related steroids such as exemestane by GC- or LC-MS. 17β-hydroxy Exemestane is the primary active metabolite of exemestane.1 It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11.2 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM).3,4 It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner.4,5 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.1

1.Goss, P.E., Qi, S., Cheung, A.M., et al.Effects of the steroidal aromatase inhibitor exemestane and the nonsteroidal aromatase inhibitor letrozole on bone and lipid metabolism in ovariectomized ratsClin. Cancer Res.10(17)5717-5723(2004) 2.Kamdem, L.K., Flockhart, D.A., and Desta, Z.In vitro cytochrome P450-mediated metabolism of exemestaneDrug Metab. Dispos.39(1)98-105(2011) 3.Buzzetti, F., Di Salle, E., Longo, A., et al.Synthesis and aromatase inhibition by potential metabolites of exemestane (6-methylenandrosta-1,4-diene-3,17-dione)Steroids58(11)527-532(1993) 4.Ariazi, E.A., LeitÃo, A., Oprea, T.I., et al.Exemestane's 17-hydroxylated metabolite exerts biological effects as an androgenMol. Cancer Ther.6(11)2817-2827(2007) 5.Varela, C.L., Amaral, C., Tavares da Silva, E., et al.Exemestane metabolites: Synthesis, stereochemical elucidation, biochemical activity and anti-proliferative effects in a hormone-dependent breast cancer cell lineEur. J. Med. Chem.87336-345(2014)

Chemical Properties

Cas No. N/A SDF
Canonical SMILES C=C1C2=CC(C=C[C@]2(C)[C@]3([H])[C@@]([C@@](CC([2H])([2H])[C@]4([2H])O)([H])[C@]4(C)CC3)([H])C1)=O
分子式 C20H23D3O2 分子量 301.4
溶解度 Chloroform: Soluble,Methanol: Soluble 储存条件 Store at -20°C
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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。
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。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.3179 mL 16.5893 mL 33.1785 mL
5 mM 0.6636 mL 3.3179 mL 6.6357 mL
10 mM 0.3318 mL 1.6589 mL 3.3179 mL
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