Rosuvastatin calcium | S-4522 | ZD 4522 | CAS#147098-20-2 | 287714-41-4 | HMG-CoA reductase inhibitor

MedKoo Cat#: 319524 | Name: Rosuvastatin calcium

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Rosuvastatin calcium

CAS#147098-20-2 (calcium)

Theoretical Analysis

MedKoo Cat#: 319524

Name: Rosuvastatin calcium

CAS#: 147098-20-2 (calcium)

Chemical Formula: C44H54CaF2N6O12S

Exact Mass: 0.0000

Molecular Weight: 1001.14

Elemental Analysis: C, 52.79; H, 5.44; Ca, 4.00; F, 3.80; N, 8.39; O, 19.18; S, 6.40

Price and Availability

Size	Price	Availability
1g	USD 150.00	Ready to ship
2g	USD 250.00	Ready to ship
5g	USD 450.00	Ready to ship
10g	USD 750.00	Ready to ship
20g	USD 1,250.00	Ready to ship
50g	USD 1,950.00	Ready to ship
100g	USD 2,950.00	Ready to ship
200g	USD 3,950.00	Ready to ship

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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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#CRB60719

QC Data

View QC data: current batch, Lot#CRB60719

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

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	mg/mL	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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

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:

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.

1: Yang Y, Wu YX, Hu YZ. Rosuvastatin Treatment for Preventing Contrast-Induced Acute Kidney Injury After Cardiac Catheterization: A Meta-Analysis of Randomized Controlled Trials. Medicine (Baltimore). 2015 Jul;94(30):e1226. doi: 10.1097/MD.0000000000001226. Review. PubMed PMID: 26222855; PubMed Central PMCID: PMC4554112. 2: Drapkina OM, Eliashevich SO. [Efficacy and Safety of Rosuvastatin in Patients of Different Risk Groups of Developing Cardiovascular Diseases]. Kardiologiia. 2015;55(2):72-81. Review. Russian. PubMed PMID: 26164992. 3: Laufs U. [Lipid lowering by rosuvastatin: how do statins differ?]. Dtsch Med Wochenschr. 2015 Mar;140(5):313. doi: 10.1055/s-0041-100713. Epub 2015 Mar 3. Review. German. PubMed PMID: 25734669. 4: Adams SP, Sekhon SS, Wright JM. Lipid-lowering efficacy of rosuvastatin. Cochrane Database Syst Rev. 2014 Nov 21;11:CD010254. doi: 10.1002/14651858.CD010254.pub2. Review. PubMed PMID: 25415541. 5: Kostapanos MS, Rizos CV, Elisaf MS. Benefit-risk assessment of rosuvastatin in the treatment of atherosclerosis and related diseases. Drug Saf. 2014 Jul;37(7):481-500. doi: 10.1007/s40264-014-0169-4. Review. PubMed PMID: 24788803. 6: Toth PP. An update on the benefits and risks of rosuvastatin therapy. Postgrad Med. 2014 Mar;126(2):7-17. doi: 10.3810/pgm.2014.03.2736. Review. PubMed PMID: 24685964. 7: Wang Z, Ge J. Managing hypercholesterolemia and preventing cardiovascular events in elderly and younger Chinese adults: focus on rosuvastatin. Clin Interv Aging. 2014;9:1-8. doi: 10.2147/CIA.S41356. Epub 2013 Dec 9. Review. PubMed PMID: 24353409; PubMed Central PMCID: PMC3861292. 8: Takagi H, Umemoto T; ALICE (All-Literature Investigation of Cardiovascular Evidence) Group. A meta-analysis of randomized head-to-head trials for effects of rosuvastatin versus atorvastatin on apolipoprotein profiles. Am J Cardiol. 2014 Jan 15;113(2):292-301. doi: 10.1016/j.amjcard.2013.08.043. Epub 2013 Oct 3. Review. PubMed PMID: 24230979. 9: Hu M, Tomlinson B. Evaluation of the pharmacokinetics and drug interactions of the two recently developed statins, rosuvastatin and pitavastatin. Expert Opin Drug Metab Toxicol. 2014 Jan;10(1):51-65. doi: 10.1517/17425255.2014.851667. Epub 2013 Oct 25. Review. PubMed PMID: 24156555. 10: Mahalwar R, Khanna D. Pleiotropic antioxidant potential of rosuvastatin in preventing cardiovascular disorders. Eur J Pharmacol. 2013 Jul 5;711(1-3):57-62. doi: 10.1016/j.ejphar.2013.04.025. Epub 2013 May 3. Review. PubMed PMID: 23648561. 11: Takagi H, Niwa M, Mizuno Y, Yamamoto H, Goto SN, Umemoto T. Effects of rosuvastatin versus atorvastatin on small dense low-density lipoprotein: a meta-analysis of randomized trials. Heart Vessels. 2014 May;29(3):287-99. doi: 10.1007/s00380-013-0358-6. Epub 2013 May 5. Review. PubMed PMID: 23644555. 12: Aggarwal RK, Showkathali R. Rosuvastatin calcium in acute coronary syndromes. Expert Opin Pharmacother. 2013 Jun;14(9):1215-27. doi: 10.1517/14656566.2013.789860. Epub 2013 Apr 11. Review. PubMed PMID: 23574635. 13: DiNicolantonio JJ, Lavie CJ, Serebruany VL, O'Keefe JH. Statin wars: the heavyweight match--atorvastatin versus rosuvastatin for the treatment of atherosclerosis, heart failure, and chronic kidney disease. Postgrad Med. 2013 Jan;125(1):7-16. doi: 10.3810/pgm.2013.01.2620. Review. PubMed PMID: 23391667. 14: Zateĭshchikov DA. [Features of the use of rosuvastatin in clinical practice]. Kardiologiia. 2012;52(11):80-5. Review. Russian. PubMed PMID: 23237400. 15: Drapkina OM, Korneeva ON. [How to prolong life of patients at high cardiovascular risk. Features of rosuvastatin]. Kardiologiia. 2012;52(8):89-92. Review. Russian. PubMed PMID: 23098406. 16: Barrios V, Escobar C. Rosuvastatin and diabetes: when the evidences talk. Cardiovasc Hematol Agents Med Chem. 2013 Jun;11(2):115-24. Review. PubMed PMID: 23094943. 17: Gogolashvili NG. [Atorvastatin or rosuvastatin? Select from the perspective of evidence-based medicine]. Kardiologiia. 2012;52(7):84-92. Review. Russian. PubMed PMID: 22839720. 18: Nohara R. [COSMOS (coronary atherosclerosis study measuring effects of rosuvastatin using intravascular ultrasound in Japanese subjects) trial]. Nihon Rinsho. 2011 Nov;69 Suppl 9:341-4. Review. Japanese. PubMed PMID: 22724226. 19: Nicholls SJ, Uno K, Kataoka Y. Clinical experience with rosuvastatin in the management of hyperlipidemia and the reduction of cardiovascular risk. Expert Rev Cardiovasc Ther. 2011 Nov;9(11):1383-90. doi: 10.1586/erc.11.145. Review. PubMed PMID: 22059787. 20: Toth PP, Dayspring TD. Drug safety evaluation of rosuvastatin. Expert Opin Drug Saf. 2011 Nov;10(6):969-86. doi: 10.1517/14740338.2012.626764. Review. PubMed PMID: 21999163.