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Cat.No.S3036
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
|---|---|
| Other HMG-CoA Reductase Inhibitors | Mevastatin SR-12813 Clinofibrate Cerivastatin sodium Dihydrolanosterol 7-ketocholesterol |
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In vitro |
DMSO
: 89 mg/mL
(199.32 mM)
Water : 89 mg/mL Ethanol : 89 mg/mL |
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In vivo |
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| Molecular Weight | 446.51 | Formula | C23H35O7.Na |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 81131-70-6 | Download SDF | Storage of Stock Solutions |
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| Synonyms | CS-514 Sodium | Smiles | CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC(CC(CC(=O)[O-])O)O)O.[Na+] | ||
| Targets/IC50/Ki |
HMG-CoA reductase
5.6 μM
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|---|---|
| In vitro |
Pravastatin-Na at 10 μM inhibits the sterol synthesis at a level greater than 50% in PBMC. Pravastatin produces relaxation of isolated aortic rings, with maximum vasorelaxations of 62.8% at 10 μM and latency of ~8 min. Pravastatin (< 10 μM) stimulates NOS activity and NO release within 10 min in cultured bovine aortic endothelial cells. L-arginine potentiates NO production in response to Pravastatin (< 10 μM) in cultured bovine aortic endothelial cells. Pravastatin results in a dose-dependent inhibition of macrophage cholesterol synthesis in human monocyte derived macrophages(HMDM), mouse peritoneal macrophages (MPM) and a J-774 A.1 macrophagelike cell lines. Small concentrations of pravastatin (< 0.19 μg/mL) increases the cellular cholesterol esterification rate after incubation with LDL, but higher concentrations (< 100 μg/mL) results in an inhibition of the esterification. Pravastatin (< 0.5 mM) decreases Rho/ROCK pathway activity in human colon and ileum explants, which leads to decreased CCN2 mRNA levels. Pravastatin (<1 mM) also induces CCN2 inhibition in primary human smooth muscle cells. Pravastatin (< 0.5 mM) decreases type I collagen and fibronectin mRNA levels in both human colon and ileum explants and primary human smooth muscle cells.
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| In vivo |
Pravastatin (40 mg, single dose) causes a reduction in cholesterol synthesis in human monocyte derived macrophages by 62% in healthy subjects and 47% in hypercholesterolaemic patients. Pravastatin (40 mg/day, 8 weeks) results in a 55% inhibition of cholesterol synthesis and a 57% increase in LDL degradation in hypercholesterolaemic patients. Pravastatin (30 mg/kg/d) results in decreased length of the dystrophic lesions by 34% and recovery of muscular structure in Male Wistar rats receiving irradiation, associated with decreased CCN2 level.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04356209 | Recruiting | Breast Cancer |
Institut du Cancer de Montpellier - Val d''Aurelle |
September 28 2020 | Phase 2 |
| NCT03456102 | Completed | Tuberculosis |
Johns Hopkins University |
March 9 2020 | Phase 2 |
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