Abiraterone Acetate-d4 (Synonyms: CB-7630-d4) |
| カタログ番号GC46775 |
アビラテロン アセテート-d4 (CB7630-d4) は、重水素標識アビラテロン アセテートです。酢酸アビラテロン (CB7630) は、抗アンドロゲン活性を有する CYP17A1 の経口、強力、選択的、不可逆的阻害剤です。酢酸アビラテロンは、アビラテロン (CB7598) のプロドラッグ形態です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2122245-63-8
Sample solution is provided at 25 µL, 10mM.
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Abiraterone acetate-d4 is intended for use as an internal standard for the quantification of abiraterone acetate by GC- or LC-MS. Abiraterone acetate is an inhibitor of the cytochrome P450 (CYP) isoform CYP17A1 (IC50s = 17 and 18 nM for inhibition of C17,20-lyase and 17α-hydroxylase activities, respectively).1 It is also a prodrug form of abiraterone .2 Abiraterone acetate reduces plasma testosterone levels, increases plasma luteinizing hormone levels, and reduces ventral prostate, seminal vesicle, testis, and kidney weight in mice when administered at doses of 0.1 and 0.5 mmol/kg per day. It also reduces severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral load in the culture supernatant of infected Vero E6 cells (EC90 = 8.4 μM) and is active in a plaque reduction assay (EC50 = 1.94 μM).3 Formulations containing abiraterone acetate have been used in combination therapy for the treatment of metastatic castration-resistant prostate cancer.
1.Potter, G.A., Barrie, S.E., Jarman, M., et al.Novel steroidal inhibitors of human cytochrome P45017α (17α-hydroxylase-C17,20-lyase): Potential agents for the treatment of prostatic cancerJ. Med. Chem.38(13)2463-2471(1995) 2.Barrie, S.E., Potter, G.A., Goddard, P.M., et al.Pharmacology of novel steroidal inhibitors of cytochrome P45017α (17α-hydroxylase/C17-20 lyase)J. Steroid Biochem. Mol. Biol.50(5-6)267-273(1994) 3.Yuan, S., Chan, J.F.W., Chik, K.K.H., et al.Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening systemPharmacol. Res.159104960(2020)
| Cas No. | 2122245-63-8 | SDF | |
| 同義語 | CB-7630-d4 | ||
| Canonical SMILES | C[C@]12C(C[C@@H](OC(C)=O)CC2)=CC[C@]3([H])[C@]1([H])CC[C@@]4(C)[C@@]3([H])CC=C4C5=C([2H])N=C([2H])C([2H])=C5[2H] | ||
| Formula | C26H29D4NO2 | M.Wt | 395.6 |
| 溶解度 | Methanol: Soluble | Storage | Store at 4°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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5278 mL | 12.639 mL | 25.2781 mL |
| 5 mM | 505.6 μL | 2.5278 mL | 5.0556 mL |
| 10 mM | 252.8 μL | 1.2639 mL | 2.5278 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 20 reference(s) in Google Scholar.)
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