AZD8233
AZD8233 is an orally active antisense oligonucleotide targeting PCSK9 mRNA. AZD8233 highly specifically reduces PCSK9 mRNA. AZD8233 lowers LDL cholesterol. AZD8233 can be used in research on dyslipidemia.
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- CAS. Nr.: 2604215-74-7
- Molecular Weight:6920.84
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2604215-74-7
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Molecular Weight 6920.84
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SMILES
[AZD8233]
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AZD8233 Related Classifications
HY-158827 Related Classifications
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