WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319524
CAS#: 147098-20-2 (calcium)
Description: Rosuvastatin, also known as S-4522 and ZD 4522, is a member of the drug class of statins, used in combination with exercise, diet, and weight-loss to treat high cholesterol and related conditions, and to prevent cardiovascular disease. Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins. Its approximate elimination half life is 19 h and its time to peak plasma concentration is reached in 3–5 h following oral administration. Putative beneficial effects of rosuvastatin therapy on chronic heart failure may be negated by increases in collagen turnover markers as well as a reduction in plasma coenzyme Q10 levels in patients with chronic heart failure.
Hodoodo Cat#: H319524
Name: Rosuvastatin calcium
CAS#: 147098-20-2 (calcium)
Chemical Formula: C44H54CaF2N6O12S
Exact Mass: 0.00
Molecular Weight: 1,001.140
Elemental Analysis: C, 52.79; H, 5.44; Ca, 4.00; F, 3.80; N, 8.39; O, 19.18; S, 6.40
Related CAS #: 147098-20-2 (calcium) 287714-41-4 (free acid)
Synonym: S-4522; S 4522; S4522; ZD 4522; ZD-4522; ZD4522; ZD 4522 calcium salt; Rosuvastatin calcium, trade name: Crestor.
IUPAC/Chemical Name: calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate
InChi Key: LALFOYNTGMUKGG-JGMJEEPBSA-L
InChi Code: InChI=1S/2C22H28FN3O6S.Ca/c2*1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32;/h2*5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30);/q;;+2/p-2/b2*10-9+;
SMILES Code: CC(C1=NC(=NC(=C1/C=C/C(O)CC(O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.CC(C1=NC(=NC(=C1/C=C/C(O)CC(O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.[Ca+2]
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO and water.
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | Rosuvastatin Calcium (Rosuvastatin hemicalcium) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. |
| In vitro activity: | Significant (p < 0.001) suppression of thermally induced egg albumin and bovine serum albumin protein denaturation in a concentration gradient way was represented by rosuvastatin at the concentration of 100–6400 μg/mL. The values of the highest percentage protection from protein denaturation observed for piroxicam and rosuvastatin at the highest concentration were 1088 ± 11.32 and 1225 ± 9.83 in the case of the egg albumin assay and 87.35 ± 2.53 and 82.80 ± 4.03 in the case of bovine serum protein denaturation. Based on the results obtained, it can be delineated that rosuvastatin possesses good potential for arresting protein denaturation, as depicted in Figure 1A,B. Reference: ACS Omega. 2021 Jan 26; 6(3): 2074–2084. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7841959/ |
| In vivo activity: | Next, the effect of rosuvastatin on LPS-induced lung injury was determined using H&E staining. As shown in Figure 2A, tissues in the LPS group were found to be severely damaged; however, pre-treatment with rosuvastatin reduced infiltration of the inflammatory cells and thickening of the alveolar walls. The acute lung-injury scores correlated well with the morphologic changes (Figure 2B). The concentrations of TNF-α, MPO, IL-1β and IL-10 in the lung tissue homogenates were increased in the LPS group compared to those in the control group and significantly decreased in the rosuvastatin treatment group compared to those in the LPS group (Figure 2C–F). Reference: J Inflamm Res. 2021; 14: 1537–1549. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8057837/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.8 | 48.71 | |
| DMSO:PBS (pH 7.2) (1:1) | 0.5 | 0.50 | |
| DMF | 20.0 | 19.98 | |
| Water | 1.0 | 1.00 |
The following data is based on the product molecular weight 1,001.14 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Qasim S, Alamgeer, Kalsoom S, Shahzad M, Bukhari IA, Vohra F, Afzal S. Rosuvastatin Attenuates Rheumatoid Arthritis-Associated Manifestations via Modulation of the Pro- and Anti-inflammatory Cytokine Network: A Combination of In Vitro and In Vivo Studies. ACS Omega. 2021 Jan 14;6(3):2074-2084. doi: 10.1021/acsomega.0c05054. PMID: 33521447; PMCID: PMC7841959. 2. Chen A, Chen Z, Zhou Y, Wu Y, Xia Y, Lu D, Fan M, Li S, Chen J, Sun A, Zou Y, Qian J, Ge J. Rosuvastatin protects against coronary microembolization-induced cardiac injury via inhibiting NLRP3 inflammasome activation. Cell Death Dis. 2021 Jan 12;12(1):78. doi: 10.1038/s41419-021-03389-1. PMID: 33436548; PMCID: PMC7804109. 3. Xu HR, Yang Q, Xiang SY, Zhang PH, Ye Y, Chen Y, Xu KW, Ren XY, Mei HX, Shen CX, Ma HY, Smith FG, Jin SW, Wang Q. Rosuvastatin Enhances Alveolar Fluid Clearance in Lipopolysaccharide-Induced Acute Lung Injury by Activating the Expression of Sodium Channel and Na,K-ATPase via the PI3K/AKT/Nedd4-2 Pathway. J Inflamm Res. 2021 Apr 16;14:1537-1549. doi: 10.2147/JIR.S299267. PMID: 33889010; PMCID: PMC8057837. 4. Geng J, Xu H, Fu W, Yu X, Xu G, Cao H, Lin G, Sui D. Rosuvastatin protects against endothelial cell apoptosis in vitro and alleviates atherosclerosis in ApoE-/- mice by suppressing endoplasmic reticulum stress. Exp Ther Med. 2020 Jul;20(1):550-560. doi: 10.3892/etm.2020.8733. Epub 2020 May 8. PMID: 32537013; PMCID: PMC7282009. |
| In vitro protocol: | 1. Qasim S, Alamgeer, Kalsoom S, Shahzad M, Bukhari IA, Vohra F, Afzal S. Rosuvastatin Attenuates Rheumatoid Arthritis-Associated Manifestations via Modulation of the Pro- and Anti-inflammatory Cytokine Network: A Combination of In Vitro and In Vivo Studies. ACS Omega. 2021 Jan 14;6(3):2074-2084. doi: 10.1021/acsomega.0c05054. PMID: 33521447; PMCID: PMC7841959. 2. Chen A, Chen Z, Zhou Y, Wu Y, Xia Y, Lu D, Fan M, Li S, Chen J, Sun A, Zou Y, Qian J, Ge J. Rosuvastatin protects against coronary microembolization-induced cardiac injury via inhibiting NLRP3 inflammasome activation. Cell Death Dis. 2021 Jan 12;12(1):78. doi: 10.1038/s41419-021-03389-1. PMID: 33436548; PMCID: PMC7804109. |
| In vivo protocol: | 1. Xu HR, Yang Q, Xiang SY, Zhang PH, Ye Y, Chen Y, Xu KW, Ren XY, Mei HX, Shen CX, Ma HY, Smith FG, Jin SW, Wang Q. Rosuvastatin Enhances Alveolar Fluid Clearance in Lipopolysaccharide-Induced Acute Lung Injury by Activating the Expression of Sodium Channel and Na,K-ATPase via the PI3K/AKT/Nedd4-2 Pathway. J Inflamm Res. 2021 Apr 16;14:1537-1549. doi: 10.2147/JIR.S299267. PMID: 33889010; PMCID: PMC8057837. 2. Geng J, Xu H, Fu W, Yu X, Xu G, Cao H, Lin G, Sui D. Rosuvastatin protects against endothelial cell apoptosis in vitro and alleviates atherosclerosis in ApoE-/- mice by suppressing endoplasmic reticulum stress. Exp Ther Med. 2020 Jul;20(1):550-560. doi: 10.3892/etm.2020.8733. Epub 2020 May 8. PMID: 32537013; PMCID: PMC7282009. |
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