General
Preferred name
ROSUVASTATIN
Synonyms
ROSUVASTATIN CALCIUM ()
Rosuvastatin (D6 Calcium) ()
Rosuvastatin (D6 Sodium) ()
Rosuvastatin (D3 Sodium) ()
ZD 4522 ()
ZD 4522 Calcium ()
Rosuvastatin hemicalcium ()
Rosuvastatin sodium ()
Rosuvastatin (Calcium) ()
Rosuvastatin (Sodium) ()
ZD 4522 (Sodium) ()
X-Plended (Sodium) ()
Crestor (Sodium) ()
ZD4522 calcium ()
Rosuvastatin (ZD4522) calcium ()
Rosuvastatin (calcium salt) ()
Rosuvastatin-d6 (sodium salt) ()
ZD-4522 (Calcium salt) ()
Rosuvastatin (as calcium) ()
Fortius ()
Rostar ()
Crestor ()
Rozavel ()
NSC-747274 ()
ZD-4522 CALCIUM ()
ZD4522 (CALCIUM SALT) ()
Ezallor sprinkle ()
S-4522 ()
Ezallor ()
Suvikan ()
Rosuvastatin calcium salt ()
Rosuvastatin calcium component of roszet ()
NSC-758930 ()
Creston ()
Rosuvastatina ()
ZD-4522 ()
ZD4522 ()
Rosuvastatine ()
X-plended ()
P&D ID
PD009808
CAS
287714-41-4
147098-18-8
147098-20-2
2070009-41-3
Tags
available
probe
drug
Approved by
PMDA
FDA
First approval
2003
Drug indication
Hypercholesterolaemia
Disorder of lipid metabolism
HIV-1 infection
Elevated C-reactive protein
Drug Status
approved
Max Phase
4.0
Probe info
Probe type
calculated probe
Probe selectivity
protein-selective
Probe sources
Probe Miner (suitable probes)
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Marketed formulations may contain rosuvastatin calcium (PubChem CID 5282455). (GtoPdb)
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. ; ;
PRICE 70
DESCRIPTION Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM[2]. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[1][2][3].
DESCRIPTION Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM[2]. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[1][2][3].
DESCRIPTION Selective PARP-10 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity. (TargetMol Bioactive Compound Library)
DESCRIPTION Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects. (TargetMol Bioactive Compound Library)
DESCRIPTION Rosuvastatin is a statin medication and a competitive inhibitor of the enzyme HMG-CoA reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. It is used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke. (Enamine Bioactive Compounds)
Cell lines
2
Organisms
1
Compound Sets
30
AdooQ Bioactive Compound Library
A10810
A11122
Cayman Chemical Bioactives
18813
12029
23359
ChEMBL Approved Drugs
CHEMBL1744447
CHEMBL1496
ChEMBL Drugs
CHEMBL1744447
CHEMBL1496
Concise Guide to Pharmacology 2017/18
2954
Concise Guide to Pharmacology 2019/20
2954
Concise Guide to Pharmacology 2021/22
2954
Concise Guide to Pharmacology 2023/24
2954
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB01098
DrugBank Approved Drugs
DB01098
DrugCentral
2406
DrugCentral Approved Drugs
2406
DrugMAP
DMMIQ7G
DrugMAP Approved Drugs
DMMIQ7G
Enamine Bioactive Compounds
EBC-13301
Enamine BioReference Compounds
Guide to Pharmacology
2954
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1496
MedChem Express Bioactive Compound Library
HY-17504
HY-17504B
NCATS Inxight Approved Drugs
413KH5ZJ73
Other bioactive compounds
Prestwick Chemical Library
Probe Miner (suitable probes)
P04035/501472
ReFrame library
Selleckchem Bioactive Compound Library
Rosuvastatin-calcium(Crestor)
TargetMol Bioactive Compound Library
T1510
T1676
The Spectrum Collection
Tocris Bioactive Compound Library
6343
External IDs
83
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
Related compounds
Custom attributes
(extracted from source data)
Target
Autophagy
HMG-CoA Reductase (HMGCR)
HMGCR
Bacterial
Potassium Channel
COVID-19,HMG-CoA Reductase
Pathway
Metabolic Enzyme/Protease
Membrane Transporter/Ion Channel
Metabolism
Anti-infection
Primary Target
HMG-CoA Reductase
MOA
Inhibitor
HMGCR inhibitor
Indication
hyperlipidemia, dyslipidemia, hypertriglyceridemia, hypercholesterolemia, atherosclerosis
Disease Area
endocrinology, cardiology
Therapeutic Class
Anticholesteremic Agents
Source data