AZD8233 sodium
Based on 1 Customer Validation
AZD8233 sodium is an orally active antisense oligonucleotide targeting PCSK9 mRNA. AZD8233 sodium highly specifically reduces PCSK9 mRNA. AZD8233 sodium lowers LDL cholesterol. AZD8233 sodium can be used in research on dyslipidemia.
For research use only. We do not sell to patients.
- Purity : 94.99%
- Molecular Weight:6920.84 (free acid)
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
In Vitro
AZD8233 (5-134 nM; 8 h; 12 h post-transfection) silenced PCSK9 comparably to P-12c in human HepG2 cells at 5 nM, while P-12c exhibited markedly superior efficiency at higher doses[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human HepG2 cells
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Concentration:5, 15, 44, and 134 nM
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Incubation Time:8 h (incubation); 12 h post-transfection (RNA analysis)
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Result:No numerical PCSK9 silencing value for AZD8233 alone was reported.
P-12c displayed comparable PCSK9 silencing efficacy to AZD8233 at 5 nM, while P-12c exhibited markedly superior efficiency at 15, 44, and 134 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:heterozygous human PCSK9 transgenic (huPCSK9 Tg) (male, 5 months old)[1]
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Dosage:0.25, 0.5, 1, 2.5, and 5 mg/kg
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Administration:s.c.; days 1, 5, 8, 15, and 23
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Result:Liver exposure increased dose-dependently.
Liver exposure of 4 µg/g (3 and 5 µg/g; 5th and 95th percentiles) was predicted to result in 80% reduction in plasma PCSK9.
A dose of AZD8233 0.5 mg/kg was required to reduce PCSK9 by 80%.
The liver exposure-PCSK9 model estimated IC50 = 2.0 µg/g (1.4 and 2.9 µg/g; 5th and 95th percentiles) and Hill coefficient h = 2.2 (1.6 and 3.8).
Concomitant dose-dependent reductions of human plasma PCSK9 and LDL cholesterol were observed.
Chemical Information
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Appearance Solid
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Molecular Weight 6920.84 (free acid)
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Color White to off-white
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SMILES
[AZD8233 (sodium)]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2242 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)