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Eplontersen 

Cat. No.: HY-148089
Handling Instructions

Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases.

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

Eplontersen Chemical Structure

Eplontersen Chemical Structure

CAS No. : 1637600-16-8

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Description

Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases[1][2][3].

IC50 & Target

TTR[1], asialoglycoprotein receptor[3]

In Vitro

Eplontersen mediates N-acetylgalactosamine moiety targeting the oligonucleotide to cells bearing an asialoglycoprotein receptor[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Eplontersen (682884) (0.6, 2, 6 mg/kg; s.c.; once a week for 3 weeks) inhibits TTR protein expression in a dose-dependent manner in vivo, without affecting normal growth in transgenic C57BL/6 mice expressing human transthyretin (TTR)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Transgenic C57BL/6 mice expressing human transthyretin (TTR) (8-week-old)[3]
Dosage: 0.6, 2, 6 mg/kg
Administration: Subcutaneous injection; once a week for 3 weeks; performed tail bleeds at various time point; sacrificed mice 72 h following the final administration
Result: Decreased TTR mRNA level to 15%, and reduced plasma TTR protein levels to 21% at 6 mg/kg on day 17 after injection.
Showed no significant effect on plasma ALT and AST level, no inhibition on body weight, organ weight, spleen weight, and kidney weight as well.
CAS No.
SMILES

[Eplontersen]

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Eplontersen
Cat. No.:
HY-148089
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