Pelacarsen sodium
Based on 1 Customer Validation
Pelacarsen sodium (ISIS 681257 sodium) is a GalNAc3-conjugated 2′-MOE-modified antisense oligonucleotide. Pelacarsen sodium reduces apo (a).
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- Reinheit : 98.67%
- CAS. Nr.: 2172851-58-8
- Formel: C296H419N71Na20O163P20S13
- Molecular Weight:8636 (free acid)
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
In Vitro
Pelacarsen (5-150 μg/mL) sodium has a high binding rate to mouse plasma proteins, 96.3% and 94.1% at 5 μg/mL and 150 μg/mL, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pelacarsen (1-12 mg/kg; s.c.) sodium in cynomolgus monkeys is rapidly absorbed[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human LPA transgenic mice[2]
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Dosage:0.3, 1, 3, 10 mg/kg
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Administration:Subcutaneous injection, once weekly, 6 weeks
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Result:Showed dose-dependent reductions in liver apo(a) mRNA and plasma apo(a) protein levels.
Showed ED50 values of 0.32 mg/kg/week and 0.54 mg/kg/week for liver apo(a) mRNA and plasma apo(a) protein, respectively.
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Animal Model:CD-1 mice[2]
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Dosage:4, 40, 140 mg/kg
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Administration:Subcutaneous injection, loading doses on days 1, 3, 5, 7, then once weekly thereafter, up to 28 days
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Result:Distributed rapidly to liver and kidney.
Showed a tissue elimination half-life of 6-9 days.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2172851-58-8
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Appearance Solid
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Molecular Weight 8636 (free acid)
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Formel C296H419N71Na20O163P20S13
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Color White to off-white
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SMILES
[Pelacarsen (sodium)]
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Synonyms
AKCEA-APO(a)-LRx sodium; ISIS 681257 sodium; TQJ230 sodium
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reinheit & Dokumentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2242 KB)
Verweise
[1]. Yeang C, et al. Effect of Pelacarsen on Lipoprotein(a) Cholesterol and Corrected Low-Density Lipoprotein Cholesterol. J Am Coll Cardiol. 2022 Mar 22;79(11):1035-1046. [Content Brief]
[2]. Yu RZ, Graham MJ, Post N, et al. Disposition and Pharmacology of a GalNAc3-conjugated ASO Targeting Human Lipoprotein (a) in Mice. Mol Ther Nucleic Acids. 2016;5(5):e317. [Content Brief]
[3]. Yu RZ, Gunawan R, Post N, et al. Disposition and Pharmacokinetics of a GalNAc3-Conjugated Antisense Oligonucleotide Targeting Human Lipoprotein (a) in Monkeys. Nucleic Acid Ther. 2016;26(6):372-380. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Pelacarsen sodium Related Classifications
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