Name: Pravastatin (CS-514) Sodium
Brand: Selleck Chemicals
SKU: S3036
Rating: 5 (10 reviews)

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.94%

99.94

Relaterade mål	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Övrigt HMG-CoA Reductase Inhibitorer	Mevastatin SR-12813 Clinofibrate Dihydrolanosterol 7-ketocholesterol Cerivastatin sodium

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	446.51	Formel	C₂₃H₃₅O₇.Na	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	81131-70-6	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	CS-514 Sodium			Smiles	CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC(CC(CC(=O)[O-])O)O)O.[Na+]

Löslighet (Solubility)

In vitro
Batch:

DMSO : 89 mg/mL (199.32 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : 89 mg/mL

Ethanol : 89 mg/mL

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	4.4mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	0.295mg/ml (0.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC₅₀/Ki	HMG-CoA reductase 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.
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/8880225/ [2] https://pubmed.ncbi.nlm.nih.gov/9935036/ [3] https://pubmed.ncbi.nlm.nih.gov/7888289/ [4] https://pubmed.ncbi.nlm.nih.gov/17875761/ [5] https://pubmed.ncbi.nlm.nih.gov/17687635/

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT04356209	Recruiting	Breast Cancer	Institut du Cancer de Montpellier - Val d''Aurelle	September 28 2020	Phase 2
NCT03456102	Completed	Tuberculosis	Johns Hopkins University	March 9 2020	Phase 2

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Pravastatin (CS-514) Sodium HMG-CoA Reductase Hämmare

Molekylvikt: 446.51