Atorvastatin lactone-d5 |
| Catalog No.GC49421 |
An internal standard for the quantification of atorvastatin lactone
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 125995-03-1
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
Atorvastatin lactone-d5 is intended for use as an internal standard for the quantification of atorvastatin lactone by GC- or LC-MS. Atorvastatin lactone is an active metabolite of the HMG-CoA reductase inhibitor atorvastatin.1,2 It is formed from atorvastatin by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A3 and UGT1A1 in insect cell-derived supersomes expressing the human enzymes, and hydrolyzes to form atorvastatin in human serum at room temperature.2,3 Atorvastatin lactone inhibits HMG-CoA reductase (IC50 = 0.007 µM for the rat liver enzyme).1 It also inhibits the cytochrome P450 (CYP) isoforms CYP2C9.1 and CYP2C9.3 (IC50s = 16.8 and 5.62 µM, respectively), as well as P-glycoprotein (P-gp; IC50 = 3.1-5.2 µM).4,5
1.Roth, B.D., Blankley, C.J., Chucholowski, A.W., et al.Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran-2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleusJ. Med. Chem.34(1)357-366(1990) 2.Schirris, T.J.J., Ritschel, T., Bilos, A., et al.Statin lactonization by uridine 5’-diphospho-glucuronosyltransferases (UGTs)Mol. Pharm.12(11)4048-4055(2015) 3.Jemal, M., Ouyang, Z., Chen, B.C., et al.Quantitation of the acid and lactone forms of atorvastatin and its biotransformation products in human serum by high-performance liquid chromatography with electrospray tandem mass spectrometryRapid Commun Mass Spectrom.13(11)1003-1015(1999) 4.Shiozawa, A., Yamaori, S., Kamijo, S., et al.Effects of acid and lactone forms of statins on S-warfarin 7-hydroxylation catalyzed by human liver microsomes and recombinant CYP2C9 variants (CYP2C9.1 and CYP2C9.3)Drug Metab. Pharmacokinet.36100364(2021) 5.Bogman, K., Peyer, A.-K., TÖrÖk, M., et al.HMG-CoA reductase inhibitors and P-glycoprotein modulationBr. J. Pharmacol.132(6)1183-1192(2001)
| Cas No. | 125995-03-1 | SDF | |
| Canonical SMILES | O=C(C1=C(C(C)C)N(CC[C@H](C[C@@H](O)C2)OC2=O)C(C3=CC=C(F)C=C3)=C1C4=C([2H])C([2H])=C([2H])C([2H])=C4[2H])NC5=CC=CC=C5 | ||
| Formula | C33H28D5FN2O4 | M.Wt | 545.7 |
| Solubility | DMSO : 25 mg/mL (46.24 mM; ultrasonic and warming and heat to 60°C) | Storage | -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. |
||
| 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 | 1.8325 mL | 9.1625 mL | 18.3251 mL |
| 5 mM | 0.3665 mL | 1.8325 mL | 3.665 mL |
| 10 mM | 0.1833 mL | 0.9163 mL | 1.8325 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 7 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *