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  3. Pelacarsen sodium

Pelacarsen sodium  (Synonyms: AKCEA-APO(a)-LRx sodium; ISIS 681257 sodium; TQJ230 sodium)

Cat. No.: HY-151123A Purity: 92.70%
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Pelacarsen sodium (ISIS 681257 sodium) is a GalNAc3-conjugated 2′-MOE-modified antisense oligonucleotide. Pelacarsen sodium reduces apo (a).

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

Gene Regulation Tool

DNA, d([2′-O-(2-methoxyethyl)]m5rU-sp-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rC-m5C-sp-G-sp-T-sp-T-sp-G-sp-G-sp-T-sp-G-sp-m5C-sp-T-sp-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]m5rU-sp-[2′-O-(2-methoxyethyl)]m5rU-sp-[2′-O-(2-methoxyethyl)]m5rC), 5′-[26-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]-14,14-bis[[3-[[6-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]hexyl]amino]-3-oxopropoxy]methyl]-8,12,19-trioxo-16-oxa-7,13,20-triazahexacos-1-yl hydrogen phosphate], sodium salt

Pelacarsen sodium Chemical Structure

CAS No. : 2172851-58-8

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Based on 1 publication(s) in Google Scholar

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Description

Pelacarsen sodium (ISIS 681257 sodium) is a GalNAc3-conjugated 2′-MOE-modified antisense oligonucleotide. Pelacarsen sodium reduces apo (a)[1][2][3].

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 (0.3-10 mg/kg; s.c.; once weekly; 6 weeks) sodium reduces liver apo (a) mRNA and plasma apo (a) protein levels in human LPA transgenic mice, with over 20-fold higher potency than the unconjugated ISIS 494372[2].
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.

Animal Model: Human LPA transgenic mice[2]
Dosage: 0.3, 1, 3, 10 mg/kg
Administration: Subcutaneous injection, once weekly, 6 weeks
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.
Animal Model: CD-1 mice[2]
Dosage: 4, 40, 140 mg/kg
Administration: Subcutaneous injection, loading doses on days 1, 3, 5, 7, then once weekly thereafter, up to 28 days
Result: Distributed rapidly to liver and kidney.
Showed a tissue elimination half-life of 6-9 days.
Clinical Trial
Molecular Weight

9076.00

Formula

C296H419N71Na20O163P20S13

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[Pelacarsen (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: 92.70%

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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Pelacarsen sodium
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HY-151123A
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