普伐他汀钠, HMG-CoA 还原酶抑制剂

HMG-CoA 还原酶抑制剂
  • 10mM in DMSO
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P407896-1ml
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Compound libraries (12326)

基本描述

英文别名 CS-514 Sodium | sodium (3R,5R)-3,5-dihydroxy-7-((1S,2S,6S,8S,8aR)-6-hydroxy-2-methyl-8-((S)-2-methylbutanoyloxy)-1,2,6,7,8,8a-hexahydronaphthalen-1-yl)heptanoate
规格或纯度 10mM in DMSO
英文名称 Pravastatin sodium
生化机理 普伐他汀钠(CS-514)是一种抑制固醇合成的 HMG-CoA 还原酶抑制剂,其 IC50 值为 5.6 μM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 HMG-CoA 还原酶抑制剂
产品介绍

Pravastatin sodium是一种HMG-CoA还原酶抑制剂,能抑制甾醇合成,其IC50为5.6 μM。An HMGCR inhibitor which blocks cholesterol synthesis.

Information

Pravastatin sodium Pravastatin sodium (CS-514) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
In vitro

Pravastatin-Na at 10 μM inhibits the sterol synthesis at a level greater than 50% in PBMC. Pravastatin produces relaxation of isolated aortic rings, with maximum vasorelaxations of 62.8% at 10 μM and latency of ~8 min. Pravastatin (< 10 μM) stimulates NOS activity and NO release within 10 min in cultured bovine aortic endothelial cells. L-arginine potentiates NO production in response to Pravastatin (< 10 μM) in cultured bovine aortic endothelial cells. Pravastatin results in a dose-dependent inhibition of macrophage cholesterol synthesis in human monocyte derived macrophages(HMDM), mouse peritoneal macrophages (MPM) and a J-774 A.1 macrophagelike cell lines. Small concentrations of pravastatin (< 0.19 μg/mL) increases the cellular cholesterol esterification rate after incubation with LDL, but higher concentrations (< 100 μg/mL) results in an inhibition of the esterification. Pravastatin (< 0.5 mM) decreases Rho/ROCK pathway activity in human colon and ileum explants, which leads to decreased CCN2 mRNA levels. Pravastatin (<1 mM) also induces CCN2 inhibition in primary human smooth muscle cells. Pravastatin (< 0.5 mM) decreases type I collagen and fibronectin mRNA levels in both human colon and ileum explants and primary human smooth muscle cells.

In vivo

Pravastatin (40 mg, single dose) causes a reduction in cholesterol synthesis in human monocyte derived macrophages by 62% in healthy subjects and 47% in hypercholesterolaemic patients. Pravastatin (40 mg/day, 8 weeks) results in a 55% inhibition of cholesterol synthesis and a 57% increase in LDL degradation in hypercholesterolaemic patients. Pravastatin (30 mg/kg/d) results in decreased length of the dystrophic lesions by 34% and recovery of muscular structure in Male Wistar rats receiving irradiation, associated with decreased CCN2 level.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥98%

AI解读

关联靶点(人)

HMGCR Tclin 3-羟基-3-甲基戊二酰辅酶A还原酶(3-hydroxy-3-methylglutaryl-coenzyme A reductase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES [Na+].CCC(C)C(=O)OC1CC(O)C=C2C=CC(C)C(CCC(O)CC(O)CC([O-])=O)C12
分子量 446.51

化学和物理性质

溶解性 Solubility (25°C) In vitro      

安全和危险性(GHS)

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

1. Ruifeng Liang, Wenjing Ge, Bingjie Li, Weifeng Cui, Xiaofan Ma, Yuying Pan, Gengsheng Li.  (2022)  Evodiamine decreased the systemic exposure of pravastatin in non-alcoholic steatohepatitis rats due to the up-regulation of hepatic OATPs.  PHARMACEUTICAL BIOLOGY,  60  (1): (359-373).  [PMID:35171063] [10.1080/13880209.2022.2036767]
2. Wei Wu, Rui Cheng, Zhenzhou Jiang, Luyong Zhang, Xin Huang.  (2021)  UPLC–MS/MS method for the simultaneous quantification of pravastatin, fexofenadine, rosuvastatin, and methotrexate in a hepatic uptake model and its application to the possible drug–drug interaction study of triptolide.  BIOMEDICAL CHROMATOGRAPHY,  35  (7): (e5093).  [PMID:33634891] [10.1002/bmc.5093]
3. Binbin Sun, Zeyu Zhong, Fan Wang, Jiong Xu, Feng Xu, Weimin Kong, Zhaoli Ling, Nan Shu, Ying Li, Tong Wu, Mian Zhang, Liang Zhu, Xiaodong Liu, Li Liu.  (2018)  Atorvastatin impaired glucose metabolism in C2C12 cells partly via inhibiting cholesterol-dependent glucose transporter 4 translocation.  BIOCHEMICAL PHARMACOLOGY,  150  (108).  [PMID:29338971] [10.1016/j.bcp.2018.01.021]

参考文献

1. Ruifeng Liang, Wenjing Ge, Bingjie Li, Weifeng Cui, Xiaofan Ma, Yuying Pan, Gengsheng Li.  (2022)  Evodiamine decreased the systemic exposure of pravastatin in non-alcoholic steatohepatitis rats due to the up-regulation of hepatic OATPs.  PHARMACEUTICAL BIOLOGY,  60  (1): (359-373).  [PMID:35171063] [10.1080/13880209.2022.2036767]
2. Wei Wu, Rui Cheng, Zhenzhou Jiang, Luyong Zhang, Xin Huang.  (2021)  UPLC–MS/MS method for the simultaneous quantification of pravastatin, fexofenadine, rosuvastatin, and methotrexate in a hepatic uptake model and its application to the possible drug–drug interaction study of triptolide.  BIOMEDICAL CHROMATOGRAPHY,  35  (7): (e5093).  [PMID:33634891] [10.1002/bmc.5093]
3. Binbin Sun, Zeyu Zhong, Fan Wang, Jiong Xu, Feng Xu, Weimin Kong, Zhaoli Ling, Nan Shu, Ying Li, Tong Wu, Mian Zhang, Liang Zhu, Xiaodong Liu, Li Liu.  (2018)  Atorvastatin impaired glucose metabolism in C2C12 cells partly via inhibiting cholesterol-dependent glucose transporter 4 translocation.  BIOCHEMICAL PHARMACOLOGY,  150  (108).  [PMID:29338971] [10.1016/j.bcp.2018.01.021]

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