Rosuvastatin - CAS 287714-41-4
Catalog number: 287714-41-4
Category: Inhibitor
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Molecular Formula:
C22H28FN3O6S
Molecular Weight:
481.54
COA:
Inquire
Targets:
HMG-CoA Reductase (HMGCR)
Description:
Rosuvastatin, also called as ZD 4522 or Crestor, a synthetic statin, in the phase III HYDRA trial for Hypercholesterolaemia, is a competitive inhibitor of HMG-CoA reductase (IC50= 11 nM).
Purity:
98%
Appearance:
Solid powder
Synonyms:
(E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acidCalcium, RosuvastatinCrestorrosuvastatinrosuvastatin calciumZD 4522ZD4522ZD-4522
Solubility:
Soluble in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -32℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Boiling Point:
745.6±70.0 °C | Condition: Press: 760 Torr
Melting Point:
161.9 °C
Density:
1.368 g/cm3
InChIKey:
BPRHUIZQVSMCRT-VEUZHWNKSA-N
InChI:
1S/C22H28FN3O6S/c1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30)/b10-9+/t16-,17-/m1/s1
Canonical SMILES:
CC(C)C1=NC(=NC(=C1C=CC(CC(CC(=O)O)O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C
Current Developer:
AstraZeneca; Shionogi
1.RP1-13D10.2 Is a Novel Modulator of Statin-Induced Changes in Cholesterol.
Mitchel K1, Theusch E1, Cubitt C1, Dosé AC1, Stevens K1, Naidoo D1, Medina MW2. Circ Cardiovasc Genet. 2016 Apr 12. pii: CIRCGENETICS.115.001274. [Epub ahead of print]
BACKGROUND: -Numerous genetic contributors to cardiovascular disease risk have been identified through genome-wide association studies (GWAS); however, identifying the molecular mechanism underlying these associations is not straightforward. The JUPITER trial of rosuvastatin users identified a sub-genome wide association of rs6924995, a SNP ~10kb downstream ofMYLIP(akaIDOL, inducible degrader of LDLR), with LDL cholesterol statin response. Interestingly, though this signal was initially attributed toMYLIP, rs6924995 lies withinRP1-13D10.2, an uncharacterized long noncoding RNA.
2.The Topical Application of Rosuvastatin in Preventing Knee Intra-Articular Adhesion in Rats.
Wu H1, Germanov AV2, Goryaeva GL3, Yachmenev AN4, Gordienko DI2, Kuzin VV2, Skoroglyadov AV1. Med Sci Monit. 2016 Apr 26;22:1403-9.
BACKGROUND Intra-articular adhesion is one of the common complications of post knee surgery and injury. The formation of joint adhesion can lead to serious dysfunction. Rosuvastatin (ROS) is a new 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, with multiple biological effects. In our study, the object was to evaluate the effectiveness of ROS in the prevention of post-operative knee adhesion in rats. MATERIAL AND METHODS Femoral condyle exposing surgery was performed on 45 healthy Sprague Dawley rats. Gelatin sponges soaked with 20 mg/kg of ROS, 10 mg/kg of ROS, or saline were used to cover the surgical site. The post-operative knee joints were fixed in a flexed position with micro Kirschner wires for four weeks. ROS effectiveness for treating intra-articular adhesion was determined with visual score evaluation, hydroxyproline content, histological analyses, immunohistochemistry, and inflammatory and vascular endothelial growth factors expression.
3.Cholesterol Lowering in Intermediate-Risk Persons without Cardiovascular Disease.
Yusuf S1, Bosch J1, Dagenais G1, Zhu J1, Xavier D1, Liu L1, Pais P1, López-Jaramillo P1, Leiter LA1, Dans A1, Avezum A1, Piegas LS1, Parkhomenko A1, Keltai K1, Keltai M1, Sliwa K1, Peters RJ1, Held C1, Chazova I1, Yusoff K1, Lewis BS1, Jansky P1, Khunti K1, Toff WD1, Reid CM1, Varigos J1, Sanchez-Vallejo G1, McKelvie R1, Pogue J1, Jung H1, Gao P1, Diaz R1, Lonn E1; HOPE-3 Investigators. N Engl J Med. 2016 Apr 2. [Epub ahead of print]
Background Previous trials have shown that the use of statins to lower cholesterol reduces the risk of cardiovascular events among persons without cardiovascular disease. Those trials have involved persons with elevated lipid levels or inflammatory markers and involved mainly white persons. It is unclear whether the benefits of statins can be extended to an intermediate-risk, ethnically diverse population without cardiovascular disease. Methods In one comparison from a 2-by-2 factorial trial, we randomly assigned 12,705 participants in 21 countries who did not have cardiovascular disease and were at intermediate risk to receive rosuvastatin at a dose of 10 mg per day or placebo. The first coprimary outcome was the composite of death from cardiovascular causes, nonfatal myocardial infarction, or nonfatal stroke, and the second coprimary outcome additionally included revascularization, heart failure, and resuscitated cardiac arrest. The median follow-up was 5.
4.Beneficial Effects of Sarpogrelate and Rosuvastatin in High Fat Diet/Streptozotocin-Induced Nephropathy in Mice.
Kim DH1, Choi BH1, Ku SK2, Park JH1, Oh E1, Kwak MK1. PLoS One. 2016 Apr 20;11(4):e0153965. doi: 10.1371/journal.pone.0153965. eCollection 2016.
Chronic kidney disease (CKD) is a major complication of metabolic disorders such as diabetes mellitus, obesity, and hypertension. Comorbidity of these diseases is the factor exacerbating CKD progression. Statins are commonly used in patients with metabolic disorders to decrease the risk of cardiovascular complications. Sarpogrelate, a selective antagonist of 5-hydroxytryptamine (5-HT) 2A receptor, inhibits platelet aggregation and is used to improve peripheral circulation in diabetic patients. Here, we investigated the effects of sarpogrelate and rosuvastatin on CKD in mice that were subjected to a high fat diet (HFD) for 22 weeks and a single low dose of streptozotocin (STZ, 40 mg/kg). When mice were administrated sarpogrelate (50 mg/kg, p.o.) for 13 weeks, albuminuria and urinary cystatin C excretion were normalized and histopathological changes such as glomerular mesangial expansion, tubular damage, and accumulations in lipid droplets and collagen were significantly improved.
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CAS 287714-41-4 Rosuvastatin

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