General
Preferred name
ROSUVASTATIN
Synonyms
ROSUVASTATIN CALCIUM ()
Rosuvastatin (D6 Calcium) ()
Rosuvastatin (D6 Sodium) ()
Rosuvastatin (D3 Sodium) ()
ZD 4522 ()
ZD 4522 Calcium ()
Rosuvastatin hemicalcium ()
ZD4522 ()
Rosuvastatin sodium ()
ZD 4522 (Sodium) ()
X-Plended (Sodium) ()
Crestor (Sodium) ()
Rosuvastatin (Calcium) ()
Rosuvastatin (Sodium) ()
Rosuvastatin (ZD4522) calcium ()
ZD4522 calcium ()
Rosuvastatin (calcium salt) ()
Rosuvastatin-d6 (sodium salt) ()
NSC-758930 ()
NSC-747274 ()
ZD4522 (CALCIUM SALT) ()
Crestor ()
Ezallor sprinkle ()
ZD-4522 CALCIUM ()
Ezallor ()
Rosuvastatin (as calcium) ()
ZD-4522 (Calcium salt) ()
S-4522 ()
Rostar ()
Rosuvastatin calcium salt ()
Rozavel ()
ZD-4522 ()
Fortius ()
Suvikan ()
Creston ()
X-plended ()
P&D ID
PD009808
CAS
287714-41-4
147098-18-8
147098-20-2
2070009-41-3
Tags
available
drug
probe
Approved by
PMDA
FDA
First approval
2003
Drug indication
Hypercholesterolaemia
Elevated C-reactive protein
Drug Status
approved
Max Phase
4.0
Probe info
Probe selectivity
protein-selective
Probe type
calculated probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
4
No orthogonal probes found
Similar probes
1
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA
Rosuvastatin is a competitive inhibitor of HMG-CoA reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. Rosuvastatin acts primarily in the liver. Decreased hepatic cholesterol concentrations stimulate the upregulation of hepatic low density lipoprotein (LDL) receptors which increases hepatic uptake of LDL. Rosuvastatin also inhibits hepatic synthesis of very low density lipoprotein (VLDL). The overall effect is a decrease in plasma LDL and VLDL. ; In vitro and in vivo animal studies also demonstrate that rosuvastatin exerts vasculoprotective effects independent of its lipid-lowering properties. Rosuvastatin exerts an anti-inflammatory effect on rat mesenteric microvascular endothelium by attenuating leukocyte rolling, adherence and transmigration (PMID: 11375257). The drug also modulates nitric oxide synthase (NOS) expression and reduces ischemic-reperfusion injuries in rat hearts (PMID: 15914111). Rosuvastatin increases the bioavailability of nitric oxide (PMID: 11375257, 12031849, 15914111) by upregulating NOS (PMID: 12354446) and by increasing the stability of NOS through post-transcriptional polyadenylation (PMID: 17916773). It is unclear as to how rosuvastatin brings about these effects though they may be due to decreased concentrations of mevalonic acid. ; ;
DESCRIPTION
Selective PARP-10 inhibitor
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
1
Compound Sets
29
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine BioReference Compounds
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
Other bioactive compounds
Prestwick Chemical Library
Probe Miner (suitable probes)
ReFrame library
Selleckchem Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
74
Properties
(calculated by RDKit )
Molecular Weight
481.17
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
3
Rotatable Bonds
10
Ring Count
2
Aromatic Ring Count
2
cLogP
2.4
TPSA
140.92
Fraction CSP3
0.41
Chiral centers
2.0
Largest ring
6.0
QED
0.47
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Autophagy
HMG-CoA Reductase (HMGCR)
HMG-CoA Reductase
Potassium Channel
HMGCR
Bacterial
COVID-19,HMG-CoA Reductase
Pathway
Metabolic Enzyme/Protease
Metabolism
Membrane Transporter/Ion Channel
Anti-infection
MOA
Inhibitor
HMGCR inhibitor
Indication
hyperlipidemia, dyslipidemia, hypertriglyceridemia, hypercholesterolemia, atherosclerosis
Disease Area
endocrinology, cardiology
Therapeutic Class
Anticholesteremic Agents
Source data