1. Epigenetics
  2. Small Interfering RNA (siRNA)
  3. Olpasiran sodium

Olpasiran sodium  (Synonyms: AMG 890 sodium; ARC-LPA sodium)

Cat. No.: HY-153492A Purity: 98.82%
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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.

For research use only. We do not sell to patients.

RNA, (Cm-sp-Am-Gm-Cm-Cm-Cm-Cm-Um-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)A-(2′-deoxy-2′-fluoro)U-Um-Gm-Um-Um-Am-Um-Am-Cm-Gm-(3′→3′)-sp-dA), 5′-[O-[(23S,28S)-37-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]-23,28-bis[[[2-[2-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]ethoxy]ethyl]amino]carbonyl]-21,26,31-trioxo-3,6,9,12,15,18,35-heptaoxa-22,27,32-triazaheptatriacont-1-yl] hydrogen phosphorothioate], complex with RNA (Um-sp-(2′-deoxy-2′-fluoro)C-sp-Gm-(2′-deoxy-2′-fluoro)U-Am-(2′-deoxy-2′-fluoro)U-Am-Am-Cm-Am-Am-(2′-deoxy-2′-fluoro)U-Am-(2′-deoxy-2′-fluoro)A-Gm-(2′-deoxy-2′-fluoro)G-Gm-(2′-deoxy-2′-fluoro)G-Cm-sp-(2′-deoxy-2′-fluoro)U-sp-Gm) (1:1), sodium salt

Olpasiran sodium Chemical Structure

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Description

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[1][2].

In Vitro

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.

In Vivo

Olpasiran sodium (s.c.; single dose) reduces serum lipoprotein(a) by >98% transiently and sustains reductions of >85% for more than 5 weeks in transgenic mice[1].
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.

Animal Model: Double transgenic Lp(a) mice (female, 8-13 weeks old, expresses human apo(a) and human apoB-100)[2]
Dosage: 0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
Administration: S.c.; single dose
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).
Clinical Trial
Molecular Weight

15438.7 (free acid)

Formula

C490H610F11N164Na42O306P41S7

Appearance

Solid

Color

White to off-white

SMILES

[Olpasiran (sodium)]

Shipping

Room temperature in continental US; may vary elsewhere.

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

Purity: 98.82%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Olpasiran sodium
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