1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. Apolipoprotein DNA/RNA Synthesis
  3. Pelacarsen sodium

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

目录号: HY-151123A 纯度: 92.70%
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Pelacarsen sodium (ISIS 681257 sodium) 是一种 GalNAc3 偶联的 2′-MOE 修饰的反义寡核苷酸 (antisense oligonucleotide)。Pelacarsen sodium 可减少 apo (a)。

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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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1 mg ¥1480
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5 mg ¥3960
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10 mg ¥5220
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生物活性

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

体外研究
(In Vitro)

Pelacarsen (5-150 μg/mL) sodium 与小鼠血浆蛋白的结合率很高,在 5 μg/mL 和 150 μg/mL 时分别为 96.3% 和 94.1%[2]

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

体内研究
(In Vivo)

Pelacarsen (0.3-10 mg/kg;皮下注射;每周一次;6 周) sodium 可降低人 LPA 转基因小鼠肝脏载脂蛋白 (a) mRNA和血浆载脂蛋白 (a) 蛋白水平,其效力比未结合的 ISIS 494372高出 20 多倍[2]
Pelacarsen (1-12 mg/kg;皮下注射) sodium 在食蟹猴体内吸收迅速[3]

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
分子量

9076.00

Formula

C296H419N71Na20O163P20S13

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

纯度: 92.70%

参考文献
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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产品名称:
Pelacarsen sodium
目录号:
HY-151123A
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