2. Neuronal Signaling
  3. Transthyretin (TTR)
  4. Eplontersen sodium

Eplontersen sodium 是 Eplontersen (HY-148089) 的钠盐形式。Eplontersen sodium 是一种三触角的、N-乙酰半乳糖胺 (GalNAc3)-缀合的反义寡核苷酸，能够靶向 甲状腺素运载蛋白 TTR 的 mRNA，抑制变体和野生型 TTR 产生。错误折叠的 TTR 诱导心脏和周围神经的淀粉样原纤维形成，并介导淀粉样 TTR (ATTR) 蛋白变性疾病。

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DNA, d([2′-O-(2-methoxyethyl)]m5rU-sp-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]rG-G-sp-T-sp-T-sp-A-sp-m5C-sp-A-sp-T-sp-G-sp-A-sp-A-sp-[2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rC-sp-[2′-O-(2-methoxyethyl)]m5rC-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

Eplontersen sodium Chemical Structure

CAS No. : 2131025-75-5

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规格 价格 是否有货 数量
1 mg ￥2380
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Other Forms of Eplontersen sodium:

Eplontersen sodium 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Eplontersen sodium the sodium salt form of Eplontersen (HY-148089). Eplontersen sodium 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].

体外研究
(In Vitro)

Eplontersen sodium 介导 N-乙酰半乳糖胺部分将寡核苷酸靶向至带有去唾液酸糖蛋白受体的细胞[3]。

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

Eplontersen sodium 相关抗体:
体内研究
(In Vivo)

Eplontersen sodium (682884) (0.6, 2, 6 mg/kg, s.c., once a week for 3 weeks) 在转基因 C57BL/6 小鼠体内剂量依赖地抑制 TTR 蛋白表达，但不影响表达人类转甲状腺素蛋白 (TTR) 的正常生长[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[3]
Dosage: 0.6-6 mg/kg
Administration: sc, 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.
Clinical Trial
分子量

9046.10

Formula

C296H417N77Na20O156P20S13
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料
参考文献

Eplontersen sodium 相关分类

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  • 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.

Keywords:

Eplontersen2131025-75-5Transthyretin (TTR)thyroxine-binding prealbuminN-acetyl galactosamineGalNAc3transthyretinTTRMisfolded TTRamyloid fibrilsheartperipheral nervesageingantisense oligonucleotideasialoglycoprotein receptorhepatitis B virusATTR variant polyneuropathyATTR cardiomyopathyInhibitorinhibitorinhibit

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