2. Epigenetics
  3. Small Interfering RNA (siRNA)
  4. Givosiran

Givosiran  (Synonyms: ALN-AS1)

目录号: HY-132610 纯度: 98.51%
COA 产品使用指南 技术支持

Givosiran (ALN-AS1) 是一种小干扰 RNA，靶向肝脏氨基纤维素合酶 1 (ALAS1) 信使 RNA。Givosiran 下调 ALAS1 mRNA 并阻止神经毒性 δ-氨基纤维酸 (ALA) 和胆色素原 (PBG) 的积累。Givosiran 在小鼠、大鼠和食蟹猴模型中均展现出强大的对 ALAS1 的抑制能力。Givosiran 可用于急性肝性卟啉症 (AHP) 的研究。

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RNA, (Cm-sp-Am-sp-Gm-Am-Am-Am-(2'-deoxy-2'-fluoro)G-Am-(2'-deoxy-2'-fluoro)G-Um-(2'-deoxy-2'-fluoro)G-Um-(2'-deoxy-2'-fluoro)C-Um-(2'-deoxy-2'-fluoro)C-Am-Um-Cm-Um-Um-Am), 3'-[[(2S,4R)-1-[29-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]- 14,14-bis[[3-[[3-[[5-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]-1-oxopentyl]amino]propyl]amino]-3-oxopropoxy]methyl]-1,12,19,25-tetraoxo-16-oxa13,20,24-triazanonacos-1-yl]-4-hydroxy-2-pyrrolidinyl]methyl hydrogen phosphate], complex with RNA (Um-sp-(2'-deoxy-2'-fluoro)A-sp-(2'-deoxy-2'-fluoro)A-(2'-deoxy-2'-fluoro)G-Am-(2'-deoxy-2'-fluoro)U-Gm-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)A-Cm-(2'-deoxy-2'-fluoro)A-Cm-(2'-deoxy-2'-fluoro)U-Cm-(2'-deoxy-2'-fluoro)U-Um-(2'-deoxy-2'-fluoro)U-Cm-(2'-deoxy-2'-fluoro)U-Gm-sp-Gm-sp-Um) (1:1)

Givosiran Chemical Structure

CAS No. : 1639325-43-1

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规格 价格 是否有货 数量
1 mg ￥2850
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Other Forms of Givosiran:

Givosiran 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran can be used for the research of acute hepatic porphyria (AHP)[1][2].

体内研究
(In Vivo)

Givosiran (10 mg/kg，皮下，单剂量) 可有效降低大鼠肝组织和血清中的 ALAS1 mRNA 水平，且具有快速起效和持久抑制作用[2]。
Givosiran (3 mg/kg，皮下，每周两次，共 3 周) 在大鼠急性间歇性卟啉症 (AIP) 模型中表现出完全预防作用[2]。
Givosiran (20 mg/kg，皮下，单剂量) 在小鼠中起效更快，抑制作用更强，优于标准血红蛋白 (HY-P2995) 治疗[2]。
Givosiran (1-10 mg/kg，皮下，单剂量或每日一次，共 8 周) 可降低食蟹猴血清和尿液中 ALAS1 的水平，重复给药可产生持续抑制，且停药后可逆[2]。

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

Animal Model: AIP model induced by Phenobarbital established in SD rats[2]
Dosage: 3 mg/kg
Administration: Subcutaneous injection (s.c.), twice weekly for 3 weeks
Result: Completely prevented inducible ALAS1 elevation and associated metabolite accumulation.
Animal Model: AIP model induced by Phenobarbital established in T1/T2 AIP mice[2]
Dosage: 20 mg/kg
Administration: Subcutaneous injection (s.c.), single dose
Result: Inhibited ALAS1 faster and stronger than Hemoglobin.
Animal Model: AIP model induced by Phenobarbital established in cynomolgus monkey (M. fascicularis)[2]
Dosage: 1 and 10 mg/kg (single dose); 5 mg/kg (8 weeks)
Administration: Subcutaneous injection (s.c.), single dose or once daily for 8 weeks
Result: Dose-dependently and reversibly inhibited ALAS1 levels and repeated dosing achieved sustained suppression.
Clinical Trial
分子量

16300.60

CAS 号
性状

固体

颜色

White to off-white

Sequence

RNA, (Cm-sp-Am-sp-Gm-Am-Am-Am-(2'-deoxy-2'-fluoro)G-Am-(2'-deoxy-2'-fluoro)G-Um-(2'-deoxy-2'-fluoro)G-Um-(2'-deoxy-2'-fluoro)C-Um-(2'-deoxy-2'-fluoro)C-Am-Um-Cm-Um-Um-Am), 3'-[[(2S,4R)-1-[29-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]- 14,14-bis[[3-[[3-[[5-[[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl]oxy]-1-oxopentyl]amino]propyl]amino]-3-oxopropoxy]methyl]-1,12,19,25-tetraoxo-16-oxa13,20,24-triazanonacos-1-yl]-4-hydroxy-2-pyrrolidinyl]methyl hydrogen phosphate], complex with RNA (Um-sp-(2'-deoxy-2'-fluoro)A-sp-(2'-deoxy-2'-fluoro)A-(2'-deoxy-2'-fluoro)G-Am-(2'-deoxy-2'-fluoro)U-Gm-(2'-deoxy-2'-fluoro)A-Gm-(2'-deoxy-2'-fluoro)A-Cm-(2'-deoxy-2'-fluoro)A-Cm-(2'-deoxy-2'-fluoro)U-Cm-(2'-deoxy-2'-fluoro)U-Um-(2'-deoxy-2'-fluoro)U-Cm-(2'-deoxy-2'-fluoro)U-Gm-sp-Gm-sp-Um) (1:1)
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

纯度: 98.51%

COA (294 KB) RP-HPLC (220 KB) MS (474 KB)

产品使用指南 (1538 KB)
参考文献

Givosiran 相关分类

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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:

Givosiran1639325-43-1ALN-AS1Small Interfering RNA (siRNA)siRNAaminolevulinateALAS1mRNAδ-aminolevulinicacidporphobilinogenacuteintermittentporphyriaInhibitorinhibitorinhibit

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