1133429-16-9
Chemical Structure
Rosuvastatin-d3
Synonym(s): ZD 4522 d3
- CAS No.: 1133429-16-9
- Formula:C22H25D3FN3O6S
- Molecular Weight:484.56
IUPAC Name: (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-(methyl-d3)methylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid
InChIKey: BPRHUIZQVSMCRT-UJWYGDJLSA-N
SMILES: FC(C=C1)=CC=C1C2=NC(N(C([2H])([2H])[2H])S(=O)(C)=O)=NC(C(C)C)=C2/C=C/[C@@H](O)C[C@@H](O)CC(O)=O
Biological Activity: Rosuvastatin-d3 (ZD 4522-d3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
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Rosuvastatin-d3 | Rosuvastatin-d3 (ZD 4522-d3) is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. | |||||||||||||||||||||
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Rosuvastatin-d6 | Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels. | |||||||||||||||||||||
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Rosuvastatin | 99.67% | Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7. [Content Brief]
