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Rosuvastatin

瑞舒伐他汀
Catalog No.
B1123
HMG-CoA还原酶的竞争性抑制剂
组合的产品项目
规格价格库存 数量
50mg
¥ 1,054.00
Ship with 10-15 days
100mg
¥ 1,336.00
Ship with 10-15 days

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A

背景

Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM.

文献引用

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt481.54
Cas No.287714-41-4
FormulaC22H28FN3O6S
Solubility≥48.2 mg/mL in DMSO; ≥10.78 mg/mL in H2O with ultrasonic; ≥12.4 mg/mL in EtOH with ultrasonic
Chemical Name(E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
SDFDownload SDF
Canonical SMILESCC(C)C1=NC(=NC(=C1C=CC(CC(CC(=O)O)O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C
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试验操作

Cell experiment:[1]

Cell lines

Rat isolated hepatocytes

Reaction Conditions

1.12 nM (IC50)

Applications

Rosuvastatin inhibited the incorporation of sodium [14C]acetate into cholesterol with an IC50 value of 1.12 nM, and its inhibitory activity on cholesterol biosynthesis was approximately 100 times more potent than pravastatin.

Animal experiment:[1]

Animal models

Normolipemic male beagle dogs

Dosage form

3 mg/kg/day

Administered orally for 14 days

Applications

In male beagle dogs with normal cholesterol levels, rosuvastatin (3 mg/kg/day) administration for 14 days decreased plasma cholesterol levels by 26%, higher than 18% in the pravastatin treatment group.

Note

The technical data provided above is for reference only.

References:

1. Watanabe M, Koike H, Ishiba T, 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. Bioorganic & Medicinal Chemistry, 1997, 5(2): 437-444.

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