2-Hydroxy atorvastatin calcium salt
Based on 1 Customer Validation
2-Hydroxy atorvastatin calcium salt is an orally active OATP1B1 substrate and inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (3-hydroxy-3-methylglutaryl-coenzyme A reductase). 2-Hydroxy atorvastatin calcium salt enters cells via OATP1B1-mediated cellular uptake and inhibits de novo hepatic cholesterol synthesis. As an active metabolite of Atorvastatin (HY-B0589), 2-Hydroxy atorvastatin calcium salt contributes to the inhibitory activity against plasma HMG-CoA reductase. 2-Hydroxy atorvastatin calcium salt can be biotransformed into an inactive lactone form, which can be hydrolyzed back to its active acid form chemically or enzymatically. 2-Hydroxy atorvastatin (calcium salt) can be used in the research of hypercholesterolemia.
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 265989-46-6
- Formula: C33H35FN2O6.1/2Ca
- Molecular Weight:594.69
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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3-hydroxy-3-methylglutaryl-coenzyme A reductase |
2-Hydroxy atorvastatin (calcium salt) (0.10-40.00 ng/mL; up to 88 days, 3 freeze-thaw cycles, up to 120 min, 24 h) is accurately and precisely quantified by the validated HPLC-MS-MS assay in human plasma over a 0.10-40.00 ng mL−1 range, with a limit of detection of 0.07 ng mL−1, and demonstrates reliable stability across multiple storage and processing conditions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 265989-46-6
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Appearance Solid
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Molecular Weight 594.69
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Formula C33H35FN2O6.1/2Ca
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Color White to off-white
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SMILES
FC1=CC=C(C2=C(C3=CC=CC=C3)C(C(NC4=CC=CC=C4O)=O)=C(C(C)C)N2CC[C@@H](O)C[C@@H](O)CC(O)=O)C=C1.[Ca].[1/2]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 12.5 mg/mL (21.02 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.10 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.10 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Lau YY, et al. effect of OATP1B transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers. Clinical pharmacology and therapeutics. 2007 Feb;81(2):194-204. [Content Brief]
[2]. Borek-Dohalský V, et al. Validated HPLC-MS-MS method for simultaneous determination of atorvastatin and 2-hydroxyatorvastatin in human plasma-pharmacokinetic study. Analytical and bioanalytical chemistry. 2006 Sep;386(2):275-85. [Content Brief]
[3]. Backman JT, et al. Rifampin markedly decreases and gemfibrozil increases the plasma concentrations of atorvastatin and its metabolites. Clinical pharmacology and therapeutics. 2005 Aug;78(2):154-67. [Content Brief]
[4]. Lennernäs H, et al. Clinical pharmacokinetics of atorvastatin. Clinical pharmacokinetics. 2003;42(13):1141-60. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6815 mL | 8.4077 mL | 16.8155 mL | 42.0387 mL |
| 5 mM | 0.3363 mL | 1.6815 mL | 3.3631 mL | 8.4077 mL | |
| 10 mM | 0.1682 mL | 0.8408 mL | 1.6815 mL | 4.2039 mL | |
| 15 mM | 0.1121 mL | 0.5605 mL | 1.1210 mL | 2.8026 mL | |
| 20 mM | 0.0841 mL | 0.4204 mL | 0.8408 mL | 2.1019 mL |
2-Hydroxy atorvastatin calcium salt Related Classifications
HY-128828 Related Classifications
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