Pravastatin sodium - 10mM in DMSO , HMG-CoA reductase inhibitor, CAS No.81131-70-6, HMG-CoA reductase inhibitor

CAS: 81131-70-6 Cat. No.: P407896 Molecular Weight: 446.5 EC Number: 617-202-5

GRADE & PURITY 10mM in DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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%

Specifications

Synonyms

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

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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

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.

Action Type

INHIBITOR

Mechanism of action

HMG-CoA reductase inhibitor

Names and Identifiers

• Isomeric SMILES: CC[C@H](C)C(=O)O[C@H]1C[C@@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@H](C[C@H](CC(=O)[O-])O)O)O.[Na+]
• WGK Germany: 2
• RTECS: QJ7185000
• Molecular Weight: 446.5
• Reaxy-Rn: 25328261
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25328261&ln=

Associated Targets(Human)

HMGCR Tclin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (1 Activities)

Discover Target: HMGCR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro
• Specific Rotation[α]: 155° (C=0.5,H2O)
• Melt Point(°C): 171°C-173°C

References

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,      [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,      [PMID:29338971] [10.1016/j.bcp.2018.01.021]