2. Anti-infection Epigenetics
  3. Small Interfering RNA (siRNA) HBV
  4. Elebsiran

Elebsiran (VIR-2218) 是一种靶向并降解乙型肝炎病毒 (HBV) 和丁型肝炎病毒 (HDV) RNA 转录物的 siRNA。Elebsiran 可显著降低乙肝病毒表面抗原 (HBsAg) 水平并降低病毒载量。Elebsiran 通过 GalNAc 配体与肝细胞表面的唾液酸缺失糖蛋白受体 (ASGPR) 结合，实现肝脏靶向递送，并显示出改善的肝脏安全性。Elebsiran 可用于慢性 HBV/HDV 感染的研究。

该游离形式化合物不稳定，推荐具有相同生物学活性的稳定盐形式 Elebsiran sodium。

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Elebsiran

Elebsiran Chemical Structure

CAS No. : 2648009-64-5

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Elebsiran 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

Elebsiran (VIR-2218) is a siRNA that targets and degrades hepatitis B virus (HBV) and hepatitis D virus (HDV) RNA transcripts. Elebsiran leads to a significant decrease in HBV surface antigen (HBsAg) and a reduction in viral load. Elebsiran binds to the sialic acid-depleted glycoprotein receptor (ASGPR) on the surface of liver cells through the GalNAc ligand, achieving liver-targeted delivery and demonstrating improved liver safety. Elebsiran can be used for the study of chronic HBV/HDV infections[1][2][3].

体外研究
(In Vitro)

Elebsiran (0.1 pM-100 nM) 可有效降低乙肝表面抗原水平以及丁型肝炎病毒的传染性，与 Tobevibart (HY-P990015) 联合治疗时，可产生叠加效应[1]。
Elebsiran 在 HepG2.2.15 细胞中表现出与 ALN-HBV 相当的抗病毒活性，但其细胞毒性显著降低[3]。

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

Elebsiran 相关抗体:
药代动力学
(Parmacokinetics)[2]
Species Dose Route Indicator value
Monkey 10 mg/kg s.c. Tmax 24 h
Rat 10 mg/kg s.c. Tmax 7 h
Monkey 10 mg/kg s.c. Cmax 135000 ng/g
Rat 10 mg/kg s.c. Cmax 97000 ng/g
Monkey 10 mg/kg s.c. AUClast 37200000 h·ng/g
Rat 10 mg/kg s.c. AUClast 6610000 h·ng/g
Monkey 10 mg/kg s.c. T1/2 160 h
Rat 10 mg/kg s.c. T1/2 93.1 h
体内研究
(In Vivo)

Elebsiran (9 mg/kg，皮下注射，单剂量) 在小鼠体内具有抗乙肝病毒和丁肝病毒的活性[1]。
Elebsiran (12-100 mg/kg，皮下注射，第 0、21、28、35 和 42 天共注射 5 次) 在所有剂量组中均未引起 ALT 显著升高，并表现出对小鼠肝脏的高度安全性[3]。

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

Animal Model: HBV/HDV-coinfected liver-chimeric model established in liver-chimeric mice[1]
Dosage: 9 mg/kg alone or with 15 mg/kg muHBC34 (the murinized version of Tobevibart)
Administration: Subcutaneous injection (s.c.), single dose
Result: Significant decreased of 0.6 log for HBsAg, 0.5 log for HBV DNA and 0.7 log for HDV RNA compared to the vehicle control on day 14 post-treatment.
Led to the strongest reductions in HBsAg, HBV DNA and HDV RNA levels relative to the vehicle group with muHBC34.
Animal Model: Chimeric mouse model established male PXB mice at 12 to 18 weeks[3]
Dosage: 12 mg/kg, 36 mg/kg, and 100 mg/kg
Administration: Subcutaneous injection (s.c.), on Days 0, 21, 28, 35, and 42
Result: Observed a clear dose-dependent increase in hALT1 levels, whereas no relationship between hALT1 and dose level.
Clinical Trial
分子量

14976.67

Formula

C485H618F9N158Na40O294P39S6
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Elebsiran 相关分类

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  • 稀释计算器

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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.

Keywords:

Elebsiran2648009-64-5VIR-2218VIR2218VIR 2218Small Interfering RNA (siRNA)HBVHepatitis B virussiRNAvirologyHBV surface antigenInhibitorinhibitorinhibit

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