Rosuvastatin
Based on 27 publication(s) in Google Scholar
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 287714-41-4
- Formula: C22H28FN3O6S
- Molecular Weight:481.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Rosuvastatin
More- Cell Metab. 2025 Sep 2;37(9):1907-1925.e14. [Abstract]
- MedComm (2020). 2024 Aug 31;5(9):e681. [Abstract]
- Adv Sci (Weinh). 2024 Jul 5:e2403451. [Abstract]
- Biosens Bioelectron. 2025 Nov 15:288:117807. [Abstract]
- Phytomedicine. 2025 Jun 19:145:157014. [Abstract]
- Phytomedicine. 2024 Jul:129:155621. [Abstract]
- Cell Death Discov. 2024 May 29;10(1):263. [Abstract]
- Acta Pharmacol Sin. 2023 Jul;44(7):1416-1428. [Abstract]
- Free Radic Biol Med. 2026 Jun 24:254:360-369. [Abstract]
- Front Bioeng Biotechnol. 2022 Mar 17;10:826093. [Abstract]
- Eur J Pharmacol. 2023 Sep 15:955:175911. [Abstract]
- Front Cell Dev Biol. 2022 Mar 3;10:806081. [Abstract]
- Front Cell Dev Biol. 2021 May 6;9:651579. [Abstract]
- ACS Omega. 2025 Oct 29;10(44):52562-52575. [Abstract]
- Cell Signal. 2025 Jul:131:111753. [Abstract]
- J Inflamm Res. 2021 Apr 16:14:1537-1549. [Abstract]
- FASEB J. 2026 May 15;40(9):e71873. [Abstract]
- Pharm Res. 2025 Oct 27. [Abstract]
- Front Oncol. 2021 May 10:11:595285. [Abstract]
- PLoS One. 2026 Feb 20;21(2):e0339967. [Abstract]
- Exp Ther Med. 2021 Oct;22(4):1189. [Abstract]
- bioRxiv. 2026 May 25.
- Vasc Endovasc Rev. 2025 Nov 7.
- Biomed Pharmacother. 2025 Oct 21:192:118665. [Abstract]
- J Nephropharmacol. 2025 Sep 20:e12798
- World J Methodol. 2025 Jun 20;15(2):99580. [Abstract]
- bioRxiv. 2024 November 08.
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Bio/Physico-chemical Assay
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WB
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
0.23 nM
Compound: ros, rosuvastatin
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Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs
Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs
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[PMID: 17560788] |
| Hepatocyte | IC50 |
0.23 nM
Compound: 1, rosuvastatin
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Inhibition of cholesterol synthesis in rat hepatocytes
Inhibition of cholesterol synthesis in rat hepatocytes
|
[PMID: 17764936] |
| Hepatocyte | IC50 |
0.23 nM
Compound: 26
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Inhibition of cholesterol synthesis in rat hepatocytes
Inhibition of cholesterol synthesis in rat hepatocytes
|
[PMID: 18540668] |
| Hepatocyte | IC50 |
0.27 nM
Compound: Rosuvastatin
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Inhibition of cholesterol synthesis in rat hepatocyte
Inhibition of cholesterol synthesis in rat hepatocyte
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[PMID: 17574412] |
| Hepatocyte | IC50 |
0.27 nM
Compound: rosuvastatin
|
Inhibition of cholesterol synthesis in rat hepatocyte
Inhibition of cholesterol synthesis in rat hepatocyte
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[PMID: 18155906] |
| Hepatocyte | IC50 |
0.3 nM
Compound: Rosuvastatin
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Inhibition of cholesterol synthesis in rat hepatocytes assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 4 hrs before addition of [14C]-acetic acid by liquid scintillation counting
Inhibition of cholesterol synthesis in rat hepatocytes assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 4 hrs before addition of [14C]-acetic acid by liquid scintillation counting
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[PMID: 21183342] |
| Hepatocyte | IC50 |
0.3 nM
Compound: rosuvastatin
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Inhibition of cholesterol synthesis in rat hepatocytes
Inhibition of cholesterol synthesis in rat hepatocytes
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[PMID: 18072721] |
| Hepatocyte | IC50 |
0.6 nM
Compound: rosuvastatin
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Inhibition of cholesterol synthesis in rat hepatocytes assessed as incorporation of [14C]acetate into cholesterol
Inhibition of cholesterol synthesis in rat hepatocytes assessed as incorporation of [14C]acetate into cholesterol
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[PMID: 18412317] |
| L6 | IC50 |
210 nM
Compound: 1, rosuvastatin
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Inhibition of cholesterol synthesis in L6 myocytes
Inhibition of cholesterol synthesis in L6 myocytes
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[PMID: 17764936] |
| L6 | IC50 |
250 nM
Compound: Rosuvastatin
|
Inhibition of cholesterol synthesis in rat L6 cells assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 3 hrs before addition of [14C]-acetic acid by scintillation counting
Inhibition of cholesterol synthesis in rat L6 cells assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 3 hrs before addition of [14C]-acetic acid by scintillation counting
|
[PMID: 21183342] |
| L6 | IC50 |
250 nM
Compound: rosuvastatin
|
Inhibition of cholesterol synthesis in rat L6 cells
Inhibition of cholesterol synthesis in rat L6 cells
|
[PMID: 18072721] |
| L6 | IC50 |
250 nM
Compound: rosuvastatin
|
Inhibition of cholesterol synthesis in rat L6 myocyte
Inhibition of cholesterol synthesis in rat L6 myocyte
|
[PMID: 18155906] |
| L6 | IC50 |
65 nM
Compound: rosuvastatin
|
Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol
Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol
|
[PMID: 18412317] |
| L6 | IC50 |
720 nM
Compound: ros, rosuvastatin
|
Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs
Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs
|
[PMID: 17560788] |
| L6 | IC50 |
720 nM
Compound: 26
|
Inhibition of cholesterol synthesis in rat L6 myocytes
Inhibition of cholesterol synthesis in rat L6 myocytes
|
[PMID: 18540668] |
| Ventricular myocyte | IC50 |
250 nM
Compound: Rosuvastatin
|
Inhibition of cholesterol synthesis in rat myocyte
Inhibition of cholesterol synthesis in rat myocyte
|
[PMID: 17574412] |
Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 287714-41-4
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Appearance Solid
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Molecular Weight 481.54
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Formula C22H28FN3O6S
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Color White to off-white
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SMILES
O=C(O)C[C@H](O)C[C@H](O)/C=C/C1=C(C(C)C)N=C(N(C)S(=O)(C)=O)N=C1C2=CC=C(F)C=C2
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Synonyms
ZD 4522
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (27)
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Journal Impact Factor
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Most Recent
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Cell Metab
Tumor-associated Schwann cell remodeling under metabolic stress via lactate sensing orchestrates pancreatic ductal adenocarcinoma development. [Abstract]2025 Sep 2;37(9):1907-1925.e14. PMID: 40803319 -
MedComm (2020)
Statins, but not proprotein convertase subtilisin-kexin type 9 inhibitors, lower chemerin in hypercholesterolemia via low-density lipoprotein receptor upregulation. [Abstract]2024 Aug 31;5(9):e681. PMID: 39220103
Rosuvastatin purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Aug 31;5(9):e681. [Abstract]
Chemerin levels in the medium of HepG2 cells cultured for 48 h, in the absence (control) or presence of atorvastatin, evolocumab, or Rosuvastatin, were measured.
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Adv Sci (Weinh)
Short-Term Statin Therapy Induces Hepatic Insulin Resistance Through HNF4α/PAQR9/PPM1α Axis Regulated AKT Phosphorylation. [Abstract]2024 Jul 5:e2403451. PMID: 38970167
Rosuvastatin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jul 5:e2403451. [Abstract]
Western blotting of PAQR9 in mouse primary hepatocytes under the treatment of DMSO, simvastatin (Sim), atorvastatin (Ator), and rosuvastatin (Rosu) (10 μM; 24–48 h) was performed.
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Biosens Bioelectron
Drug functionalized organic electromechanical transistor for rapid and sensitive detection of C-reactive protein. [Abstract]2025 Nov 15:288:117807. PMID: 40712486 -
Phytomedicine
Theaflavin-3,3'-digallate stabilizes vulnerable plaques by reprogramming metabolic homeostasis in neovascularization via HK2/TIGAR. [Abstract]2025 Jun 19:145:157014. PMID: 40570559 -
Phytomedicine
Gut microbiome and metabolomic profiles reveal the antiatherosclerotic effect of indole-3-carbinol in high-choline-fed ApoE-/- mice. [Abstract]2024 Jul:129:155621. PMID: 38678950 -
Cell Death Discov
Upregulation of rate-limiting enzymes in cholesterol metabolism by PKCδ mediates endothelial apoptosis in diabetic wound healing. [Abstract]2024 May 29;10(1):263. PMID: 38811564
Rosuvastatin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 May 29;10(1):263. [Abstract]
Rosuvastatin calcium (5 mg/kg i.p.) was administered. Images of the wound area in the rosuvastatin calcium-treated group and the control group were captured.
Rosuvastatin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 May 29;10(1):263. [Abstract]
Rosuvastatin calcium (5 mg/kg i.p.) was administered. The free cholesterol level of skin tissue after rosuvastatin calcium treatment for 12 days was measured. Each experiment was replicated at least thrice and representative images were shown.
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Acta Pharmacol Sin
2023 Jul;44(7):1416-1428. PMID: 36721007
Rosuvastatin purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Jul;44(7):1416-1428. [Abstract]
Rosuvastatin calcium (10 mg/kg body weight every second day, n = 5) was administered. The body weights of control and bavachin-treated mice were measured weekly from weeks 1 to 20.
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Free Radic Biol Med
Rosuvastatin ameliorates high-altitude cerebral edema by promoting blood-brain barrier integrity via the regulation of energy metabolism. [Abstract]2026 Jun 24:254:360-369. PMID: 42341957 -
Front Bioeng Biotechnol
Application of 3D Hepatic Plate-Like Liver Model for Statin-Induced Hepatotoxicity Evaluation. [Abstract]2022 Mar 17;10:826093. PMID: 35372314 -
Eur J Pharmacol
Combining idebenone and rosuvastatin prevents atherosclerosis by suppressing oxidative stress and NLRP3 inflammasome activation. [Abstract]2023 Sep 15:955:175911. PMID: 37451421 -
Front Cell Dev Biol
Atorvastatin Induces Mitochondria-Dependent Ferroptosis via the Modulation of Nrf2-xCT/GPx4 Axis. [Abstract]2022 Mar 3;10:806081. PMID: 35309902 -
Front Cell Dev Biol
2021 May 6;9:651579. PMID: 34026753 -
ACS Omega
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug-Drug Interaction In Vitro. [Abstract]2025 Oct 29;10(44):52562-52575. PMID: 41244417 -
Cell Signal
Rosuvastatin inhibits carcinogenesis through Ca2+ triggered endoplasmic reticulum stress pathway in pancreatic cancer. [Abstract]2025 Jul:131:111753. PMID: 40107481 -
J Inflamm Res
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. [Abstract]2021 Apr 16:14:1537-1549. PMID: 33889010 -
FASEB J
Simvastatin Restores Cisplatin Sensitivity by Suppressing the Caveolin-1-Mediated PI3K/AKT Signaling Pathway in Cisplatin-Resistant Cervical Cancer Cells. [Abstract]2026 May 15;40(9):e71873. PMID: 42087353 -
Pharm Res
Profiling Interactions Between Bicyclol and SLC/ABC Transporters: Advancing Clinical Safety and Efficacy in Combination Therapy. [Abstract]2025 Oct 27. PMID: 41145746 -
Front Oncol
Synergistic Effect of Statins and Abiraterone Acetate on the Growth Inhibition of Neuroblastoma via Targeting Androgen Receptor. [Abstract]2021 May 10:11:595285. PMID: 34041015 -
PLoS One
Rosuvastatin protects against oxLDL-induced endothelial cell oxidative stress and attenuates atherosclerotic plaque formation in ApoE-/- mice through the NF-κB pathway. [Abstract]2026 Feb 20;21(2):e0339967. PMID: 41719299 -
Exp Ther Med
Rosuvastatin protects PC12 cells from hypoxia/reoxygenation-induced injury by inhibiting endoplasmic reticulum stress-induced apoptosis. [Abstract]2021 Oct;22(4):1189. PMID: 34475979 -
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Biomed Pharmacother
Integrated pharmacokinetic properties and tissue distribution of Corydalis saxicola Bunting total alkaloids in HFHCD-induced mice: Implications for pharmacokinetic variability in MASH treatment. [Abstract]2025 Oct 21:192:118665. PMID: 41124864 -
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World J Methodol
Anticonvulsant potential of rosuvastatin in combination with carbamazepine and valproate in animal models of epilepsy. [Abstract]2025 Jun 20;15(2):99580. PMID: 40548212 -
Solvent & Solubility
DMSO : ≥ 100 mg/mL (207.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44. [Content Brief]
[2]. Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78. [Content Brief]
[3]. Feng PF, et al. Intracellular Mechanism of Rosuvastatin-Induced Decrease in Mature hERG Protein Expression on Membrane. Mol Pharm. 2019 Apr 1;16(4):1477-1488. [Content Brief]
[4]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0767 mL | 10.3834 mL | 20.7667 mL | 51.9168 mL |
| 5 mM | 0.4153 mL | 2.0767 mL | 4.1533 mL | 10.3834 mL | |
| 10 mM | 0.2077 mL | 1.0383 mL | 2.0767 mL | 5.1917 mL | |
| 15 mM | 0.1384 mL | 0.6922 mL | 1.3844 mL | 3.4611 mL | |
| 20 mM | 0.1038 mL | 0.5192 mL | 1.0383 mL | 2.5958 mL | |
| 25 mM | 0.0831 mL | 0.4153 mL | 0.8307 mL | 2.0767 mL | |
| 30 mM | 0.0692 mL | 0.3461 mL | 0.6922 mL | 1.7306 mL | |
| 40 mM | 0.0519 mL | 0.2596 mL | 0.5192 mL | 1.2979 mL | |
| 50 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 1.0383 mL | |
| 60 mM | 0.0346 mL | 0.1731 mL | 0.3461 mL | 0.8653 mL | |
| 80 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6490 mL | |
| 100 mM | 0.0208 mL | 0.1038 mL | 0.2077 mL | 0.5192 mL |