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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 94.99%
- 分子量:6920.84 (free acid)
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
製品説明
体外実験
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.
体内実験
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.
化学情報
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性状 Solid
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分子量 6920.84 (free acid)
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Color White to off-white
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SMILES
[AZD8233 (sodium)]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2242 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)