Rosuvastatin | CAS# 287714-41-4 | HMG-CoA reductase inhibitor

MedKoo Cat#: 574290 | Name: Rosuvastatin

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Description:

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

Rosuvastatin is a potent HMG-CoA reductase inhibitor. Formulations containing rosuvastatin reduce low-density lipoprotein (LDL) and C-reactive protein and increase high-density lipoprotein (HDL) in humans.

Chemical Structure

Rosuvastatin

CAS#287714-41-4 (free acid)

Theoretical Analysis

MedKoo Cat#: 574290

Name: Rosuvastatin

CAS#: 287714-41-4 (free acid)

Chemical Formula: C22H28FN3O6S

Exact Mass: 481.1683

Molecular Weight: 481.54

Elemental Analysis: C, 54.87; H, 5.86; F, 3.95; N, 8.73; O, 19.93; S, 6.66

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 weeks
10mg	USD 550.00	2 weeks

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Related CAS #

147098-20-2 (calcium) 287714-41-4 (free acid)

Synonym

Rosuvastatin, ZD 4522, ZD4522, ZD-4522

IUPAC/Chemical Name

7-[4-(4-fluorophenyl)-6E-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3R,5S-dihydroxy-6-heptenoic acid

InChi Key

BPRHUIZQVSMCRT-VEUZHWNKSA-N

InChi Code

InChI=1S/C22H28FN3O6S/c1-13(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/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30)/b10-9+/t16-,17-/m1/s1

SMILES Code

O[C@@H](C[C@@H](O)CC(O)=O)/C=C/C(C(C1=CC=C(F)C=C1)=NC(N(C)[S](C)(=O)=O)=N2)=C2C(C)C

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, DMF, and ethanol

Shelf Life

>3 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

Instruction

View handling instruction

Biological target:

Rosuvastatin is an inhibitor of HMG-CoA reductase (IC50 = 5 nM). It inhibits cholesterol synthesis in isolated rat hepatocytes with an IC50 value of 0.16 nM. Rosuvastatin reduces plasma total cholesterol, triglyceride, LDL-C, and oxidized LDL-C levels in Ldlr-/- mice fed a high-fat diet. It decreases the area of aortic atherosclerotic lesions in the same model.

In vitro activity:

In HeLa cells infected with T. gondii, rosuvastatin showed a significant reduction in both the number of infected cells and the proliferation index of the intracellular parasite, when compared with conventional treatment. There were also reduced levels of cytokines IL-6 and IL-17. Therefore, it was concluded that rosuvastatin exhibited antiproliferative activity. Reference: Exp Parasitol. 2017 Oct;181:75-81. https://pubmed.ncbi.nlm.nih.gov/28774497/

In vivo activity:

Rosuvastatin lessened random skin flap tissue edema and promoted skin flap survival. Rosuvastatin also promoted angiogenesis, reduced oxidative stress, induced autophagy, and reduced pyroptosis. Rosuvastatin improves the survival rate of random skin flaps. Reference: Int Immunopharmacol. 2023 May;118:110059. https://pubmed.ncbi.nlm.nih.gov/37001384/

	Solvent	mg/mL	mM
Solubility
	DMF	5.0	10.38
	DMSO	5.0	10.38
	Ethanol	1.0	2.08

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 481.54 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. Aksoy HN, Ceylan C. Comparison of the Effects of Statins on A549 Nonsmall-Cell Lung Cancer Cell Line Lipids Using Fourier Transform Infrared Spectroscopy: Rosuvastatin Stands Out. Lipids. 2021 May;56(3):289-299. doi: 10.1002/lipd.12296. Epub 2021 Feb 21. PMID: 33611813. 2. Sanfelice RA, Machado LF, Bosqui LR, Miranda-Sapla MM, Tomiotto-Pellissier F, de Alcântara Dalevedo G, Ioris D, Reis GF, Panagio LA, Navarro IT, Bordignon J, Conchon-Costa I, Pavanelli WR, Almeida RS, Costa IN. Activity of rosuvastatin in tachyzoites of Toxoplasma gondii (RH strain) in HeLa cells. Exp Parasitol. 2017 Oct;181:75-81. doi: 10.1016/j.exppara.2017.07.009. Epub 2017 Aug 1. PMID: 28774497. 3. Ye H, Li F, Shen Y, Wu X, Zhao L, Zhang H, Yang J, Shui X. Rosuvastatin promotes survival of random skin flaps through AMPK-mTOR pathway-induced autophagy. Int Immunopharmacol. 2023 May;118:110059. doi: 10.1016/j.intimp.2023.110059. Epub 2023 Mar 29. PMID: 37001384. 4. Evangelista FF, Costa-Ferreira W, Mantelo FM, Beletini LF, de Souza AH, de Laet Sant'Ana P, de Lima KK, Crestani CC, Falavigna-Guilherme AL. Rosuvastatin revert memory impairment and anxiogenic-like effect in mice infected with the chronic ME-49 strain of Toxoplasma gondii. PLoS One. 2021 Apr 15;16(4):e0250079. doi: 10.1371/journal.pone.0250079. PMID: 33857221; PMCID: PMC8049280.

In vitro protocol:

In vivo protocol:

1. Ye H, Li F, Shen Y, Wu X, Zhao L, Zhang H, Yang J, Shui X. Rosuvastatin promotes survival of random skin flaps through AMPK-mTOR pathway-induced autophagy. Int Immunopharmacol. 2023 May;118:110059. doi: 10.1016/j.intimp.2023.110059. Epub 2023 Mar 29. PMID: 37001384. 2. Evangelista FF, Costa-Ferreira W, Mantelo FM, Beletini LF, de Souza AH, de Laet Sant'Ana P, de Lima KK, Crestani CC, Falavigna-Guilherme AL. Rosuvastatin revert memory impairment and anxiogenic-like effect in mice infected with the chronic ME-49 strain of Toxoplasma gondii. PLoS One. 2021 Apr 15;16(4):e0250079. doi: 10.1371/journal.pone.0250079. PMID: 33857221; PMCID: PMC8049280.

1: Li M, Noordam R, Trompet S, Winter EM, Jukema JW, Arbous MS, Rensen PCN, Kooijman S. The impact of statin use on sepsis mortality. J Clin Lipidol. 2024 Jul 27:S1933-2874(24)00215-0. doi: 10.1016/j.jacl.2024.07.006. Epub ahead of print. PMID: 39299824. 2: Shah VT. LIpid Response to Statins ± Ezetimibe In Mumbai (LIRIM): A Cross- sectional Observational Study. J Assoc Physicians India. 2024 Sep;72(9):64-72. doi: 10.59556/japi.72.0622. PMID: 39291519. 3: Ramzy S, Althobaiti YS, Almalki AH. Eco-friendly second derivative synchronous fluorescence spectroscopic method for simultaneous determination of rosuvastatin and ezetimibe in pharmaceutical capsules. Spectrochim Acta A Mol Biomol Spectrosc. 2024 Sep 10;325:125123. doi: 10.1016/j.saa.2024.125123. Epub ahead of print. PMID: 39288605. 4: Streekstra EJ, Keuper-Navis M, van den Heuvel JJMW, van den Broek P, Stommel MWJ, de Boode W, Botden S, Bervoets S, O'Gorman L, Greupink R, Russel FGM, van de Steeg E, de Wildt SN. Enteroids to Study Pediatric Intestinal Drug Transport. Mol Pharm. 2024 Sep 16. doi: 10.1021/acs.molpharmaceut.4c00339. Epub ahead of print. PMID: 39279643. 5: Mahajan K, Puri R, Duell PB, Dutta D, Yadav R, Kumar S, Sharma JB, Patel P, Dsouza S, Gupta A, Khan A, Wong ND. Rapid achievement of low-density lipoprotein cholesterol goals within 1 month after acute coronary syndrome during combination therapy with rosuvastatin, ezetimibe and bempedoic acid: Initial experience from the LAI-REACT study. J Clin Lipidol. 2024 Jun 6:S1933-2874(24)00200-9. doi: 10.1016/j.jacl.2024.06.001. Epub ahead of print. PMID: 39278778. 6: de Mello TF, Goedert AB, de Souza JSS, da Cruz JVR, da Silva AS, Knorst JK, Muller YMR, Silva FRMB, Leite GAA. Prolonged exposure to rosuvastatin from pre- puberty to adulthood impairs sperm quality in mice and leads to paternally mediated developmental toxicity. Reprod Toxicol. 2024 Sep 12;130:108717. doi: 10.1016/j.reprotox.2024.108717. Epub ahead of print. PMID: 39276807. 7: Liu J, Jiao W, Li F, Xie Y, Meng M, Hao J. Rosuvastatin inhibit ox-LDL- induced platelet activation by the p38/MAPK pathway. Clin Hemorheol Microcirc. 2024 Sep 13. doi: 10.3233/CH-242359. Epub ahead of print. PMID: 39269826. 8: Elhadad ZM, Kassem AB, Amrawy AME, Salahuddin A, El-Bassiouny NA. Comparative Study Between the Effects of High Doses of Rosuvastatin and Atorvastatin on Ventricular Remodeling in Patients with ST-Segment Elevation Myocardial Infarction. Cardiovasc Drugs Ther. 2024 Sep 12. doi: 10.1007/s10557-024-07621-w. Epub ahead of print. PMID: 39264503. 9: Susekov AV. [Rationale for Increasing Doses of Statins in Everyday Clinical Practice]. Kardiologiia. 2024 Aug 31;64(8):79-88. Russian. doi: 10.18087/cardio.2024.8.n2709. PMID: 39262357. 10: Aragona CO, Bianco A, Caruso R, Cerulli M, Cosentino N, Cittadini A, Gabriele M, Mallardo M, Marini R, Miserrafiti B, Palermo P, Galati A. Lipid- lowering therapy in patients with coronary heart disease: an Italian real-life survey. Results from the Survey on Risk FactOrs and CardiovascuLar secondary prEvention and drug strategieS (SOFOCLES) in Italy. Monaldi Arch Chest Dis. 2024 Sep 10. doi: 10.4081/monaldi.2024.2972. Epub ahead of print. PMID: 39259232. 11: Long A, Yamamiya I, Valentine M, Machnes Z, Hangai N, Anderson B, Wacheck V, Gao L. A phase I drug-drug interaction study to assess the effect of futibatinib on P-gp and BCRP substrates and of P-gp inhibition on the pharmacokinetics of futibatinib. Clin Transl Sci. 2024 Sep;17(9):e70012. doi: 10.1111/cts.70012. PMID: 39258521; PMCID: PMC11388056. 12: Shinde V, Penmetsa P, Nair KR, Dixit Y. A Neuropathy Mimic: Statin-Induced Myopathy Presenting as Guillain-Barré Syndrome. Cureus. 2024 Aug 8;16(8):e66483. doi: 10.7759/cureus.66483. PMID: 39246875; PMCID: PMC11380724. 13: Taherkhani M, Khanifar Z, Taherkhani A, Hajishah H, Tavasol A. Assessing the effect of high-dose rosuvastatin in elderly patients over 75 with acute coronary syndrome. BMC Cardiovasc Disord. 2024 Sep 6;24(1):474. doi: 10.1186/s12872-024-04142-0. PMID: 39243009; PMCID: PMC11378640. 14: Alfehaid LS, Farah S, Omer A, Weber BN, Alkhezi O, Tawfik YMK, Shah AM, Libby P, Buckley LF. Drug-Drug Interactions and the Clinical Tolerability of Colchicine Among Patients With COVID-19: A Secondary Analysis of the COLCORONA Randomized Clinical Trial. JAMA Netw Open. 2024 Sep 3;7(9):e2431309. doi: 10.1001/jamanetworkopen.2024.31309. PMID: 39240567; PMCID: PMC11380098. 15: Sherif AY, Alshora DH, Ibrahim MA, Jreebi A. Development and Evaluation of Solidified Supersaturated SNEDDS Loaded with Triple Combination Therapy for Metabolic Syndrome. AAPS PharmSciTech. 2024 Sep 6;25(7):209. doi: 10.1208/s12249-024-02928-1. PMID: 39237698. 16: Malani SK, Chigullapalli S, Sujanyal S, Sharma V. Rosuvastatin-Induced Myopathy: A Case Series. Cureus. 2024 Aug 5;16(8):e66180. doi: 10.7759/cureus.66180. PMID: 39233949; PMCID: PMC11373368. 17: Sinan UY, Keskin Meric B, Bursa N, Moumin G, Kaya A, Arat Ozkan A. Evaluation of preprocedural statin loading on clinical outcomes in patients undergoing elective percutaneous coronary intervention. Front Cardiovasc Med. 2024 Aug 20;11:1435989. doi: 10.3389/fcvm.2024.1435989. PMID: 39228664; PMCID: PMC11368834. 18: Atapour A, Momenzadeh M, Panahishokouh M, Badri S. Rosuvastatin-Induced Rhabdomyolysis as a Result of Drug Interaction With Sitagliptin: A Case Report. Clin Med Insights Case Rep. 2024 Sep 2;17:11795476241274162. doi: 10.1177/11795476241274162. PMID: 39224482; PMCID: PMC11367606. 19: Chavarriaga J, Penn LZ, Khurram N, Lajkosz K, Longo J, Chen E, Fleshner N, van der Kwast T, Hamilton RJ. Statin Concentration in Prostatic Tissue is Subtype- and Dose-dependent. Urology. 2024 Aug 31:S0090-4295(24)00760-X. doi: 10.1016/j.urology.2024.08.059. Epub ahead of print. PMID: 39222671. 20: Shen B, Luo F, Yuan N, Yin J, Chai Y, Sun L, Zhang L, Luo C. Outcomes and complications of hemodialysis in patients with renal cancer following bilateral nephrectomy. Open Med (Wars). 2024 Aug 23;19(1):20241009. doi: 10.1515/med-2024-1009. PMID: 39221033; PMCID: PMC11365463.

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