Pelacarsen
Based on 1 Customer Validation
Pelacarsen (ISIS 681257) is a GalNAc3-conjugated 2′-MOE-modified antisense oligonucleotide. Pelacarsen reduces apo (a).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 97.75%
- CAS 番号: 1637637-70-7
- 分子量:8636.00
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
Apolipoprotein(a)[1]
Pelacarsen (5-150 μg/mL) has a high binding rate to mouse plasma proteins, 96.3% and 94.1% at 5 μg/mL and 150 μg/mL, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pelacarsen (1-12 mg/kg; s.c.) in cynomolgus monkeys is rapidly absorbed[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human LPA transgenic mice[2]
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Dosage:0.3, 1, 3, 10 mg/kg
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Administration:Subcutaneous injection, once weekly, 6 weeks
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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.
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Animal Model:CD-1 mice[2]
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Dosage:4, 40, 140 mg/kg
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Administration:Subcutaneous injection, loading doses on days 1, 3, 5, 7, then once weekly thereafter, up to 28 days
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Result:Distributed rapidly to liver and kidney.
Showed a tissue elimination half-life of 6-9 days.
化学情報
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CAS 番号 1637637-70-7
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性状 Solid
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分子量 8636.00
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Color White to off-white
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SMILES
[Pelacarsen]
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別名
AKCEA-APO(a)-LRx; ISIS 681257; TQJ230
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配列
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]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
H2O : 100 mg/mL (11.58 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (252 KB)
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- Français - FR (252 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2242 KB)
参考文献
[1]. Yeang C, et al. Effect of Pelacarsen on Lipoprotein(a) Cholesterol and Corrected Low-Density Lipoprotein Cholesterol. J Am Coll Cardiol. 2022 Mar 22;79(11):1035-1046. [Content Brief]
[2]. Yu RZ, Graham MJ, Post N, et al. Disposition and Pharmacology of a GalNAc3-conjugated ASO Targeting Human Lipoprotein (a) in Mice. Mol Ther Nucleic Acids. 2016;5(5):e317. [Content Brief]
[3]. Yu RZ, Gunawan R, Post N, et al. Disposition and Pharmacokinetics of a GalNAc3-Conjugated Antisense Oligonucleotide Targeting Human Lipoprotein (a) in Monkeys. Nucleic Acid Ther. 2016;26(6):372-380. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.1158 mL | 0.5790 mL | 1.1579 mL | 2.8949 mL |
| 5 mM | 0.0232 mL | 0.1158 mL | 0.2316 mL | 0.5790 mL | |
| 10 mM | 0.0116 mL | 0.0579 mL | 0.1158 mL | 0.2895 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Pelacarsen 関連分類
HY-151123 関連分類
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