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Pravastatin sodium

Katalog-Nr.GC14538 Copy One-Click Copy Product Info

Pravastatin sodium is a reversible competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with an IC50 of 5.6μM. Pravastatin sodium is commonly used in the research of hypercholesterolemia and various cardiovascular diseases.

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Pravastatin sodium Chemische Struktur

Cas No.: 81131-70-6

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10mM (in 1mL DMSO)
35,00 $
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10mg
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50mg
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100mg
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200mg
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Sample solution is provided at 25 µL, 10mM.



Description of Pravastatin sodium

Pravastatin sodium is a reversible competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with an IC50 of 5.6μM. Pravastatin sodium is commonly used in the research of hypercholesterolemia and various cardiovascular diseases[1]. HMG-CoAR is located in the cytoplasm of eukaryotic cells and some prokaryotes. The enzyme utilizes NADPH to reduce HMG-CoA to mevalonate, serving as the rate-limiting enzyme in the first stage of cholesterol biosynthesis. Critical catalytic residues of this enzyme include Lys691, Glu559, Asp767, and His866[2]. Pravastatin sodium binds to the pocket of HMG-CoAR where HMG-CoA would bind, through van der Waals forces, thereby reducing the synthesis of cholesterol[3].

In vitro, treatment with Pravastatin sodium (1μg/mL) alleviates high glucose-induced migration dysfunction in cytotrophoblast (CTB) cells incubated at varying glucose concentrations [4]. Treatment of endothelial colony-forming cells (ECFCs) with Pravastatin sodium (0-2000μM) significantly enhances cell proliferation, migration, and tube formation capabilities.Pravastatin sodium increases the phosphorylation of protein kinase B (AKT) and endothelial nitric oxide synthase (eNOS), as well as the expression levels of heme oxygenase-1 (HO-1), vascular endothelial growth factor A (VEGF-A), and placental growth factor (PlGF). Pravastatin sodium decreases the expression levels of soluble fms-like tyrosine kinase-1 (sFlt-1) and endothelial protein C receptor (Eng) [5].

In vivo, oral administration of Pravastatin sodium (20mg/kg/day) to diabetic rats for 8 weeks resulted in an increase in body weight. Pravastatin sodium significantly reduced the levels of glycogen phosphorylase, lactate dehydrogenase, and glucose-6-phosphatase, thereby improving liver enzyme abnormalities caused by diabetes. Pravastatin sodium also decreased fasting blood glucose levels and increased hepatic glycogen content [6]. Oral treatment with Pravastatin sodium (20mg/kg/day) for 14 days in mice with cardiac fibrosis induced by isoproterenol led to a reduction in CK-MB, serum triglycerides, collagen I and III levels in heart tissue, cardiac inflammatory cells, and cardiac fibrosis levels [7].

References:
[1] Raasch RH. Pravastatin sodium, a new HMG-CoA reductase inhibitor. DICP. 1991 Apr;25(4):388-94.
[2] Miziorko HM. Enzymes of the mevalonate pathway of isoprenoid biosynthesis. Arch Biochem Biophys. 2011 Jan 15;505(2):131-43.
[3] Istvan ES. Structural mechanism for statin inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Am Heart J. 2002 Dec;144(6 Suppl):S27-32.
[4] Pantho AF, Mohamed S, Govande JV, et al. Pravastatin Protects Cytotrophoblasts from Hyperglycemia-Induced Preeclampsia Phenotype. Cells. 2024 Sep 13;13(18):1534.
[5] Meyer N, Brodowski L, Richter K, et al. Pravastatin Promotes Endothelial Colony-Forming Cell Function, Angiogenic Signaling and Protein Expression In Vitro. J Clin Med. 2021 Jan 6;10(2):183.
[6] Kaya HK, Demirtas B, Yokus B, et al. Comparative effects of pravastatin and rosuvastatin on carbohydrate metabolism in an experimental diabetic rat model. Acta Pharm. 2024 Mar 30;74(1):117-130.
[7] Rana A, Singh TU, Sharma M, et al. Pravastatin attenuates isoprenaline induced cardiac fibrosis in a mouse model. Biotech Histochem. 2023 Nov;98(8):567-577.

Protocol of Pravastatin sodium

Cell experiment [1]:

Cell lines

ECFC cells

Preparation Method

ECFC cells were seeded into 6-well plates with 5 × 10 4 cells per well and cultured for 24h. The cell monolayers were scratched with a sterile P1000 pipette tip to create a wound. They were treated with different concentrations (0, 2, 20, 200, and 2000μM) of Pravastatin sodium. Phase contrast microscopic images were immediately obtained after scratching and then again after 18h.

Reaction Conditions

0, 2, 20, 200, and 2000μM; 18h

Applications

Pravastatin sodium significantly improve the migration of ECFC cells.

Animal experiment [2]:

Animal models

Wistar albino rats

Preparation Method

Female Wistar albino rats were used and diabetes was induced by intraperitoneal injection of streptozotocin. Thereafter, 10 and 20mg/kg/day doses of Pravastatin sodium were administered by oral gavage to the diabetic rats for 8 weeks. At the end of the experiment, the levels of fasting blood glucose, liver glycogen, and liver enzymes related to carbohydrate metabolism were measured.

Dosage form

10 and 20mg/kg/day for 8 weeks; p.o.

Applications

Pravastatin sodium significantly reduced the liver glycogen synthase and pyruvate kinase levels, but increased the glycogen phosphorylase level in diabetic rats.

References:
[1] Meyer N, Brodowski L, Richter K, et al. Pravastatin Promotes Endothelial Colony-Forming Cell Function, Angiogenic Signaling and Protein Expression In Vitro. J Clin Med. 2021 Jan 6;10(2):183.
[2] Kaya HK, Demirtas B, Yokus B, et al. Comparative effects of pravastatin and rosuvastatin on carbohydrate metabolism in an experimental diabetic rat model. Acta Pharm. 2024 Mar 30;74(1):117-130.

Chemical Properties of Pravastatin sodium

Cas No. 81131-70-6 SDF
Chemical Name sodium;(3R,5R)-3,5-dihydroxy-7-[(1S,2S,6S,8S)-6-hydroxy-2-methyl-8-[(2S)-2-methylbutanoyl]oxy-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]heptanoate
Canonical SMILES CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC(CC(CC(=O)[O-])O)O)O.[Na+]
Formula C23H35O7.Na M.Wt 446.51
Löslichkeit ≥ 13.15 mg/mL in DMSO, ≥ 100.4 mg/mL in EtOH with ultrasonic, ≥ 98.8 mg/mL in Water Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Pravastatin sodium

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2396 mL 11.198 mL 22.3959 mL
5 mM 447.9 μL 2.2396 mL 4.4792 mL
10 mM 224 μL 1.1198 mL 2.2396 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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