| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Rosuvastatin-d6 calcium has the same molecular target as non‑deuterated rosuvastatin: it inhibits 3‑hydroxy‑3‑methylglutaryl‑coenzyme A (HMG‑CoA) reductase (HMGCR). HMGCR is the rate‑limiting enzyme in cholesterol biosynthesis, converting HMG‑CoA to mevalonate. By inhibiting HMGCR, rosuvastatin reduces de novo cholesterol synthesis, leading to increased LDL receptor expression and enhanced clearance of LDL‑cholesterol from the circulation. The deuterium label does not alter the pharmacological activity, and the compound is not used for activity studies; it is an analytical internal standard.
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| ln Vitro |
Rosuvastatin-d6 calcium has no intrinsic biological activity distinct from rosuvastatin. As a stable isotope‑labeled internal standard, it is not used in activity assays. Non‑deuterated rosuvastatin is a potent HMG‑CoA reductase inhibitor with an IC₅0 in the low nanomolar range, used clinically to lower LDL‑cholesterol and reduce cardiovascular risk. The d6 label does not affect the compound's activity, but the labeled version is not intended for pharmacological evaluation.
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| ln Vivo |
No in vivo activity data for Rosuvastatin-d6 calcium are reported, as it is an analytical standard. Unlabeled rosuvastatin is an FDA‑approved medication (Crestor®) for the treatment of hypercholesterolemia and prevention of cardiovascular events. Rosuvastatin-d6 calcium is used as an internal standard in pharmacokinetic studies to quantify unlabeled rosuvastatin in animal plasma and tissues. It is not administered to animals for therapeutic purposes.
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| Enzyme Assay |
Rosuvastatin-d6 calcium is not evaluated in enzyme/receptor binding assays. As an analytical standard, its properties are characterized by chemical methods: HPLC (purity ≥98%), LC‑MS (to confirm isotopic enrichment ≥95% D), and NMR. The compound is used to spike into biological samples for the quantification of unlabeled rosuvastatin. No bioactivity assays are performed.
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| Cell Assay |
No cellular experiments are performed on Rosuvastatin-d6 calcium. For analytical studies, cells are cultured and treated with unlabeled rosuvastatin, and a known amount of Rosuvastatin-d6 calcium is added to the cell lysate or culture supernatant as an internal standard. Rosuvastatin is extracted (e.g., by protein precipitation with acetonitrile or methanol) and quantified by LC‑MS/MS using multiple reaction monitoring (MRM). The ratio of the peak area of unlabeled rosuvastatin to deuterated internal standard is used to calculate the concentration.
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| Animal Protocol |
No animal experiments are performed directly on Rosuvastatin-d6 calcium. For pharmacokinetic studies, unlabeled rosuvastatin is administered to animals (e.g., rats or mice) by oral gavage or intravenous injection. Blood samples are collected at various time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 24 h). A known amount of Rosuvastatin-d6 calcium is added to each plasma sample as an internal standard. Rosuvastatin is extracted, and the concentration in each sample is quantified by LC‑MS/MS. The pharmacokinetic parameters (Cmax, Tmax, AUC, t½, clearance, oral bioavailability) for rosuvastatin are then calculated.
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| ADME/Pharmacokinetics |
Rosuvastatin-d6 calcium (C22H21D₆FN3O₆S·½Ca, MW = 506.61, purity ≥98.5% by HPLC, isotopic enrichment ≥95% D, CAS 1279031‑70‑7) is a white to off‑white solid powder. For storage, the powder should be kept at 4degC for up to 3 years, sealed, and protected from light and moisture. For in vitro use, stock solutions in DMSO or methanol (1‑10 mg/mL) can be prepared and stored at -20degC for up to 1 month or at -80degC for up to 6 months, sealed and protected from moisture. For analytical use, working solutions are typically prepared fresh. The compound is stable under these conditions for extended periods. No PK data are generated for the labeled compound itself.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Rosuvastatin-d6 calcium are reported. Rosuvastatin (non‑deuterated) is a widely prescribed medication with a well‑established safety profile. Common adverse effects include myalgia, elevated liver enzymes, and, rarely, rhabdomyolysis. The deuterated version is used at trace concentrations (ng/mL to microg/mL) as an internal standard and is not administered as a test article. Standard laboratory safety precautions for handling chemicals should be followed.
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| Additional Infomation |
Rosuvastatin-d6 calcium is a stable isotope‑labeled internal standard for the quantification of rosuvastatin in biological samples by LC‑MS/MS. Rosuvastatin is a potent, competitive inhibitor of HMG‑CoA reductase, belonging to the statin class of lipid‑lowering agents. It is indicated for the treatment of dyslipidemia, hypercholesterolemia, and the prevention of cardiovascular events. Rosuvastatin is the active ingredient in the branded drug Crestor®. The d6 label (six deuterium atoms, typically on the isopropyl group of the rosuvastatin molecule) provides a mass shift of +6 Da for mass spectrometry analysis, allowing accurate quantification of the parent drug in the presence of its metabolites and endogenous compounds. This product is for research use only and is not intended for human or veterinary consumption.
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| Molecular Formula |
C22H21D6FN3O6S.1/2CA
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|---|---|
| Molecular Weight |
506.61
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| Appearance |
Solid powder
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| Synonyms |
Rosuvastatin calcium d6
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9739 mL | 9.8695 mL | 19.7390 mL | |
| 5 mM | 0.3948 mL | 1.9739 mL | 3.9478 mL | |
| 10 mM | 0.1974 mL | 0.9870 mL | 1.9739 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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