Rosuvastatin (ZD4522) calcium - Moligand™, 10mM in DMSO , HMG-CoA reductase inhibitor, CAS No.147098-20-2, HMG-CoA reductase inhibitor

CAS: 147098-20-2 Cat. No.: R408257 Molecular Weight: 500.57 EC Number: 627-028-1 PubChem CID: 5282455

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethan-3-ylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Rosuvastatin Calcium (ZD4522) is a competitive inhibitor ofHMG-CoA reductasewithIC50of 11 nM in a cell-free assay.
In vitro

Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells.

In vivo

Rosuvastatin is efficient on reducing plasma liquids. Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times. Rosuvastatin (20 mg/kg) inhibits ROS production, normalizes NO-dependent endothelial function and reduces platelet activation in diabetic rats induced by Streptozocin. Rosuvastatin displays cardioprotective effects in vivo. Rosuvastatin (80 mg) is shows to decrease infarct size and improve cardiac mechanical function after ischemia/reperfusion in animal model. The cardioprotective properties of Rosuvastatin may be due to the improvement of coronary blood flow, decrease in resistance of coronary arteries mediated by enhanced eNOS expression, and the subsequent increase in the production of vascular endothelial NO. Rosuvastatin (2.0 mg/kg) attenuates left ventricular hypertrophy produced by transaortic constriction in mice through regulation of Racl protein and NADPH oxidase activities.
Cell Data

cell lines：HL-60, U937, and NB-4 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

calcium (3R, 5S, E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethan-3-ylsulfonamido)pyrimidin-5-yl)-3, 5-dihydroxyhept-6-enoate

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Rosuvastatin Calcium (ZD4522) is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM in a cell-free assay.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

HMG-CoA reductase inhibitor

Names and Identifiers

• Isomeric SMILES: CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.[Ca+2]
• PubChem CID: 5282455
• Molecular Weight: 500.57

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Water: 5 mg/mL (38.11 mM); DMSO: Insoluble
• Specific Rotation[α]: -8° (C=1,CHCl3)
• Melt Point(°C): 160 °C

References

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