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MedKoo Cat#: 464675 | Name: Rosuvastatin lactone
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Description:

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

Rosuvastatin lactone is the lactone form of the HMG-CoA reductase inhibitor rosuvastatin. It is found in vivo following rosuvastatin administration. Rosuvastatin lactone is an inhibitor of the cytochrome P450 (CYP) isoforms CYP2C9.1 and CYP2C9.3 (IC50s = 8.52 and 4.1 µM, respectively).

Chemical Structure

Rosuvastatin lactone
Rosuvastatin lactone
CAS#503610-43-3

Theoretical Analysis

MedKoo Cat#: 464675

Name: Rosuvastatin lactone

CAS#: 503610-43-3

Chemical Formula: C22H26FN3O5S

Exact Mass: 463.1577

Molecular Weight: 463.52

Elemental Analysis: C, 57.01; H, 5.65; F, 4.10; N, 9.07; O, 17.26; S, 6.92

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Synonym
Rosuvastatin lactone; (+)-Rosuvastatin lactone; (+) Rosuvastatin lactone; Rosuvastatin-5S-lactone; RSTL;
IUPAC/Chemical Name
N-(4-(4-fluorophenyl)-5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide
InChi Key
SOEGVMSNJOCVHT-VEUZHWNKSA-N
InChi Code
InChI=1S/C22H26FN3O5S/c1-13(2)20-18(10-9-17-11-16(27)12-19(28)31-17)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)32(4,29)30/h5-10,13,16-17,27H,11-12H2,1-4H3/b10-9+/t16-,17-/m1/s1
SMILES Code
O[C@H]1CC(O[C@H](/C=C/C2=C(N=C(N=C2C3=CC=C(F)C=C3)N(S(C)(=O)=O)C)C(C)C)C1)=O
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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 lactone is an inhibitor of the cytochrome P450 (CYP) isoforms CYP2C9.1 and CYP2C9.3 (IC50s = 8.52 and 4.1 µM, respectively).
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 30.0 64.72
DMSO 15.0 32.36
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 463.52 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.

Recalculate based on batch purity %
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:
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.
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.
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