Olpasiran sodium
Based on 1 Customer Validation
Olpasiran (AMG 890, ARC-LPA) sodium is an N-acetyl galactosamine (GalNAc)-conjugated, hepatocyte-targeted siRNA. Olpasiran sodium directly inhibits LPA messenger RNA translation in hepatocytes and potently reduce Lp(a) concentration. Olpasiran sodium can be used for the research of cardiovascular disease, such as atherosclerosis.
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- Pureté: 98.82%
- Formule: C490H610F11N164Na42O306P41S7
- Masse moléculaire:15438.7 (free acid)
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Olpasiran sodium (150 fM-3 nM; 24 h) potently silences LPA reporter gene expression in Huh7 human hepatocellular carcinoma cells with an EC50 of 34.5 pM[2].
Olpasiran sodium (0.1-1 nM; 24 h) potently silences LPA reporter gene expression in Hep3B human hepatocellular carcinoma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Olpasiran sodium (3-10 mg/kg; s.c.; single dose) reduces serum lipoprotein(a) by >80% for up to 45 days after nadir in cynomolgus monkeys[1].
Olpasiran sodium (0.5-2.0 mg/kg; s.c.; single dose) produces dose-dependent, durable reductions in serum Lp(a) concentrations in double transgenic Lp(a) mice, with a single 2.0 mg/kg dose achieving the most profound suppression (to <10% of baseline) lasting at least 43 days[2].
Olpasiran sodium (1.0 mg/kg; s.c.; single dose) potently and durably reduces serum apo(a) concentrations in single transgenic apo(a) mice, with a single 1.0 mg/kg dose achieving >80% suppression lasting at least 5 weeks[2].
Olpasiran sodium (0.1-10.0 mg/kg; s.c.; single dose) produces dose-dependent, durable reductions in serum Lp(a) concentrations in Macaca fascicularis (cynomolgus monkeys), with single 3.0 mg/kg and 10.0 mg/kg doses achieving >80% suppression lasting up to 45 days after the nadir[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Double transgenic Lp(a) mice (female, 8-13 weeks old, expresses human apo(a) and human apoB-100)[2]
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Dosage:0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
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Administration:S.c.; single dose
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Result:Produced a sustained reduction in serum Lp(a) concentrations, with levels remaining below baseline for at least 43 days (0.5 mg/kg).
Resulted in more than 80% reduction in serum Lp(a) concentration, with levels remaining below pre-dose values for at least 5 weeks (1.0 mg/kg).
Produced the greatest magnitude and duration of Lp(a) reduction, with levels dropping to less than 10% of baseline by day 8 and remaining suppressed through day 43 (2.0 mg/kg).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Masse moléculaire 15438.7 (free acid)
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Formule C490H610F11N164Na42O306P41S7
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Color White to off-white
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SMILES
[Olpasiran (sodium)]
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Synonyms
AMG 890 sodium; ARC-LPA sodium
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureté et documentation
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Fiche technique (270 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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Instruction de manipulation (2242 KB)
Références
[1]. Sohn W, et al. Pharmacokinetics, Pharmacodynamics, and Tolerability of Olpasiran in Healthy Japanese and Non-Japanese Participants: Results from a Phase I, Single-dose, Open-label Study. Clin Ther. 2022;44(9):1237-1247. [Content Brief]
[2]. Koren MJ, et al. Preclinical development and phase 1 trial of a novel siRNA targeting lipoprotein(a). Nat Med. 2022;28(1):96-103. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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