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

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

Cat. No.: HY-151123 Purity: 97.75%
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Pelacarsen (ISIS 681257) is a GalNAc3-conjugated 2′-MOE-modified antisense oligonucleotide. Pelacarsen reduces apo (a).

For research use only. We do not sell to patients.

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]

Pelacarsen Chemical Structure

CAS No. : 1637637-70-7

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Pelacarsen:

Pelacarsen Related Antibodies

Top Publications Citing Use of Products

View All Apolipoprotein Isoform Specific Products:

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apoE apoB apoA1 apoA2 apoA4 apoC1 apoC2 apoC3

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

Apolipoprotein(a)[1]
In Vitro

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 Related Antibodies
In Vivo

Pelacarsen (0.3-10 mg/kg; s.c.; once weekly; 6 weeks) reduces liver apo (a) mRNA and plasma apo (a) protein levels in human LPA transgenic mice, with over 20-fold higher potency than the unconjugated ISIS 494372[2].
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.

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.
Molecular Weight

8636.00

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

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]
SMILES

[Pelacarsen]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (11.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.1158 mL 0.5790 mL 1.1579 mL
5 mM 0.0232 mL 0.1158 mL 0.2316 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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Pelacarsen Related Classifications

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:

Pelacarsen1637637-70-7AKCEA-APO(a)-LRx ISIS 681257 TQJ230ISIS681257ISIS 681257ISIS-681257TQJ230TQJ 230TQJ-230ApolipoproteinDNA/RNA Synthesiscardiovascular diseaseslipoprotein disorderschronic kidney diseaseantisense oligonucleotideInhibitorinhibitorinhibit

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