147098-18-8

147098-18-8 structure

Name: Rosuvastatin calcium
Chemical Name: sodium,7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate
CAS Number: 147098-18-8
Molecular Formula: C₂₂H₂₇FN₃NaO₆S
Molecular Weight: 503.520
Catalog: Signaling Pathways Autophagy Autophagy
Create Date: 2018-04-20 08:00:00
Modify Date: 2024-01-17 04:28:35
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].

Name	sodium,7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate
Synonyms	Sodium (6E)-7-{4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl}-3,5-dihydroxy-6-heptenoate Rosuvastatin Sodium 6-Heptenoic acid, 7-[4-(4-fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-, sodium salt, (6E)- (1:1)

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].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> Metabolic Enzyme/Protease >> HMG-CoA Reductase (HMGCR) Signaling Pathways >> Autophagy >> Autophagy Research Areas >> Metabolic Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
Target	IC50: 11 nM (HMG-CoA), 195 nM (hERG)[1][2]
In Vivo	Rosuvastatin Sodium (10 mg/kg, intraperitoneal) prolonges QTc in conscious and unrestraines guinea pigs from 201±1 to 210±2 ms[2]. Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins Sodium (VLDL) in diabetes mellitus rats induced by Streptozocin[4].
References	[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44. [2]. Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78. [3]. Feng PF, et al. Intracellular Mechanism of Rosuvastatin-Induced Decrease in Mature hERG Protein Expression on Membrane. Mol Pharm. 2019 Apr 1;16(4):1477-1488. [4]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.

Melting Point	128-131℃
Molecular Formula	C₂₂H₂₇FN₃NaO₆S
Molecular Weight	503.520
Exact Mass	503.150238
PSA	152.13000
LogP	2.14780

Hazard Codes	Xi

147098-18-8	147098-20-2
1659301-59-3	289042-12-2
355806-00-7	852820-97-4
2414245-11-5	854898-48-9
917805-80-2	917805-81-3