Fig. 1 · Structure

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Rosuvastatin

Cat. No. A11122 CAS 287714-41-4

HMG-CoA reductase inhibitor

Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
Hepatocyte IC50 0.23 nM Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs [PMID: 17560788]
Hepatocyte IC50 0.3 nM 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 [PMID: 21183342]
L6 IC50 250 nM 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 720 nM Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs [PMID: 17560788]

In Vitro Studies

In recombinant WT RyR1 incubated with Rosuvastatin, ryanodine binding yielded an EC50 of 0.50 ± 0.12 µM at 10 µM free Ca2+. In RAW264.7 mouse macrophages, Rosuvastatin at 5 µM induced CCR7 gene expression, with maximal induction at the 6 hour time point. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Ryanodine Binding in Recombinant WT RyR1

Biochemical assay · recombinant WT RyR1 [1]

Recombinant WT RyR1 was incubated with Rosuvastatin at room temperature for 30 min. Ryanodine binding yielded an EC50 of 0.50 ± 0.12 µM and an Emax of 2.02 ± 0.04 at 10 µM free Ca2+.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
[3H]ryanodine bindingEC50 at 10 µM free Ca2+: EC50: 0.50 ± 0.12 µM[1]

Literature-Reported Treatment Conditions

Treatment concentration
0.01 to 100 µM
Exposure duration
at room temperature for 30 min
Method
incubated
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Rosuvastatin; Compound label in the paper: Rosuvastatin Acid

Evidence for Rosuvastatin as the sodium form reported in the paper, not the free base/neutral form supplied as A11122; no salt equivalence, dose conversion or lot validation.

Results > Dose-dependent activation of RyR1 by rosuvastatin (S44); Methods > Radiometric rosuvastatin and ryanodine binding assays (S125); Fig. 3 legend (S150, S151)

[3H]ryanodine binding: [3H]ryanodine binding; comparator: absence of rosuvastatin — Results > Dose-dependent activation of RyR1 by rosuvastatin (S44); Fig. 3 legend (S150)

CCR7 Gene Expression in Mouse Macrophages

Cell-based study · RAW264.7 macrophages (a mouse cell line) [2]

RAW264.7 mouse macrophages were treated with Rosuvastatin in serum-free media at 5 µM. CCR7 gene expression was induced at 1 hour, with maximal induction at the 6 hour time point and the greatest induction by Rosuvastatin among the statins.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
CCR7; determined by RT-PCRReported result 5 µM: CCR7 gene expression was also induced by statins at 1 hour with maximal induction at the 6 hour time point, with the greatest induction by rosuvastatin.[2]

Literature-Reported Treatment Conditions

Treatment concentration
5 µM
Exposure duration
1, 3, 6, and 24 hours post treatment
Method
serum-free media containing
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Rosuvastatin

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Statins induce SREBP regulation of CCR7 expression (S35, S37); Materials and Methods > Cell Culture and Treatments (S96, S97, S98); Figure 4 legend (S137)

CCR7; determined by RT-PCR: CCR7; determined by RT-PCR; comparator: DMSO — Results > Statins induce SREBP regulation of CCR7 expression (S37); Materials and Methods > Cell Culture and Treatments (S97); Figure 4 legend (S137)

In Vivo Studies

In male mice with metabolic disorders, Rosuvastatin was administered at 3 mg/kg of body weight every day during the HFD for the last 16 weeks. Bacteroidetes abundance in the HFD-Rosu group was not significantly different compared to the HFD group. Rosuvastatin significantly reduced total cholesterol levels compared with HFD-fed mice. [3]

Bacteroidetes Abundance in Mice Fed a High-Fat Diet

Animal study · Male 4-week-old C57BL/6N mice; metabolic disorders such as obesity, hyperglycemia, and hyperlipidemia; n = 6 [3]

Male mice with metabolic disorders received Rosuvastatin at 3 mg/kg of body weight every day during the HFD for the last 16 weeks. Bacteroidetes abundance in the HFD-Rosu group was 33.7 ± 29.1%, which was not significantly different compared to the HFD group.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
abundance of BacteroidetesBacteroidetes relative abundance HFD-Rosu group: 33.7 ± 29.1%[3]

Conditions shared by the study groups

Treatment course
every day during the HFD for the last 16 weeks
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Rosuvastatin 3 mg/kg of body weightHFD-fed mice group (n = 6)HFD-Rosu group: 33.7 ± 29.1%; not significantly different compared to the HFD group.[3]
Rosuvastatin 3 mg/kg of body weight
Model: Male 4-week-old C57BL/6N mice; metabolic disorders such as obesity, hyperglycemia, and hyperlipidemia; n = 6
Reported limits: Not stated in the sentences used: route, vehicle.
Methods and source locations

Compound reported in the paper: Rosuvastatin

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Animals and Experimental Protocol (S1, S2, S3, S4); Materials and Methods > Fecal Microbiota Transplantation (FMT) (S33); Results > Effects of Statins and Diet on the Composition of the Gut Microbiota (S54, S56, S60); FIGURE 1 legend (S80)

abundance of Bacteroidetes: abundance of Bacteroidetes; comparator: HFD-fed mice group (n = 6) — Results > Effects of Statins and Diet on the Composition of the Gut Microbiota (S54, S56, S60)

Rosuvastatin 3 mg/kg of body weight · Materials and Methods > Animals and Experimental Protocol (S3); Results > Effects of Statins and Diet on the Composition of the Gut Microbiota (S56, S60)

Total Cholesterol in Mice Fed a High-Fat Diet

Animal study · Male 4-week-old C57BL/6N mice; metabolic disorders such as obesity, hyperglycemia, and hyperlipidemia; n = 6 [3]

Male mice with metabolic disorders received Rosuvastatin at 3 mg/kg of body weight every day during the HFD for the last 16 weeks. Rosuvastatin significantly reduced total cholesterol levels compared with HFD-fed mice.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
total cholesterolReported result rosuvastatin (HFD-Rosu: 3 mg/kg of body weight, n = 6) was administered every day during the HFD for the last 16 weeks; rosuvastatin significantly reduced total cholesterol levels.[3]

Conditions shared by the study groups

Treatment course
every day during the HFD for the last 16 weeks
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Rosuvastatin 3 mg/kg of body weightHFD-fed mice group (n = 6)rosuvastatin (HFD-Rosu: 3 mg/kg of body weight, n = 6) was administered every day during the HFD for the last 16 weeks; rosuvastatin significantly reduced total cholesterol levels.[3]
Rosuvastatin 3 mg/kg of body weight
Model: Male 4-week-old C57BL/6N mice; metabolic disorders such as obesity, hyperglycemia, and hyperlipidemia; n = 6
Reported limits: Not stated in the sentences used: route, vehicle.
Methods and source locations

Compound reported in the paper: Rosuvastatin

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Animals and Experimental Protocol (S1, S2, S3, S4); Materials and Methods > Metabolic Measurements (S12); Materials and Methods > Fecal Microbiota Transplantation (FMT) (S33); Results > Effects of Statins on Metabolic Improvements (S44); FIGURE 1 legend (S80)

total cholesterol: total cholesterol; comparator: HFD-fed mice group (n = 6) — Materials and Methods > Animals and Experimental Protocol (S3); Materials and Methods > Metabolic Measurements (S12); Results > Effects of Statins on Metabolic Improvements (S44)

Rosuvastatin 3 mg/kg of body weight · Materials and Methods > Animals and Experimental Protocol (S3); Results > Effects of Statins on Metabolic Improvements (S44)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 287714-41-4
Applications HMG-CoA reductase inhibitor
Formula C22H28FN3O6S
Molecular Weight 481.5
Synonyms Crestor
SMILES
CC(C)C1=NC(=NC(=C1/C=C/[C@H](C[C@H](CC(=O)O)O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Weninger G, Reiken S, Yuan Q, et al. Structural basis for rosuvastatin-induced activation of skeletal muscle ryanodine receptor 1. Nat Commun (2026). PMID: 42830339 DOI: 10.1038/s41467-026-77372-9 Source material
  2. [2] Feig JE, Shang Y, Rotllan N, et al. Statins promote the regression of atherosclerosis via activation of the CCR7-dependent emigration pathway in macrophages. PLoS One (2011). PMID: 22163030 DOI: 10.1371/journal.pone.0028534 Source material
  3. [3] Kim J, Lee H, An J, et al. Alterations in Gut Microbiota by Statin Therapy and Possible Intermediate Effects on Hyperglycemia and Hyperlipidemia. Front Microbiol (2019). PMID: 31551944 DOI: 10.3389/fmicb.2019.01947 Source material

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