17β-hydroxy Exemestane-d3 |
| カタログ番号GC46471 |
多様な生物学的活性を持つ神経ペプチド
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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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)
| 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 | ||
| Formula | C20H23D3O2 | M.Wt | 301.4 |
| 溶解度 | Chloroform: Soluble,Methanol: Soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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