2. Oligonucleotides
  3. Antisense Oligonucleotides
  4. Volanesorsen

Volanesorsen (ISIS 304801) is an antisense oligonucleotide inhibitor of apolipoprotein CIII (apo-CIII) mRNA that reduces triglyceride levels and improves insulin resistance. Volanesorsen is being studied in the treatment of hypertriglyceridemia, familial chylosiderosis syndrome, and type 2 diabetes.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Volanesorsen sodium) that retains the same biological activity.

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

DNA, d(P-thio)([2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rU-m5C-T-T-G-T-m5C-m5C-A-G-m5C-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]m5rU)

Volanesorsen Chemical Structure

CAS No. : 915430-78-3

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Description

Volanesorsen (ISIS 304801) is an antisense oligonucleotide inhibitor of apolipoprotein CIII (apo-CIII) mRNA that reduces triglyceride levels and improves insulin resistance. Volanesorsen is being studied in the treatment of hypertriglyceridemia, familial chylosiderosis syndrome, and type 2 diabetes[1][2][3][4][5].

In Vivo

Volanesorsen (1.5-50 mg/kg; i.p.; once a week for 2 weeks) dose-dependently reduces human apolipoprotein CIII (apo-CIII) mRNA, plasma apo-CIII protein and triglyceride (TG) levels in human apo-CIII transgenic mice[1].
Volanesorsen (4-40 mg/kg; s.c.; once a week for 13 weeks) dose-responsively reduces apoC-III mRNA levels in the liver of cynomolgus monkeys[1].
Volanesorsen (10 mg/kg; s.c.; once weekly for 10 weeks) reduces plasma triglyceride levels in hypertriglyceridemic rhesus monkeys[1].

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

Animal Model: Chow-Fed Cynomolgus[1]
Dosage: 4, 8, 12 and 40 mg/kg
Administration: Subcutaneous injection (s.c.) Once a week for 13 weeks
Result: Reduced apoC-III mRNA by 47%, 51%, 80%, and 89% in a dose-responsive manner.
Animal Model: Rhesus monkeys with hypertriglyceridemia after taking high fructose supplements[1]
Dosage: 10 mg/kg
Administration: Subcutaneous injection (s.c.) Once a week for 10 weeks
Result: Reduced plasma triglycerides, very low–density lipoprotein (VLDL)+chylomicron triglyceride, and decreased postprandial triglyceride excursion, while increasing high-density lipoprotein-cholesterol (HDL-C) in hypertriglyceridemic rhesus monkeys.
Clinical Trial
Molecular Weight

7165.00

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

DNA, d(P-thio)([2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]rG-[2′-O-(2-methoxyethyl)]m5rC-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rU-m5C-T-T-G-T-m5C-m5C-A-G-m5C-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]m5rU-[2′-O-(2-methoxyethyl)]rA-[2′-O-(2-methoxyethyl)]m5rU)
SMILES

[Volanesorsen]
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 : 50 mg/mL (6.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.1396 mL 0.6978 mL 1.3957 mL
5 mM 0.0279 mL 0.1396 mL 0.2791 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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 0.1396 mL 0.6978 mL 1.3957 mL 3.4892 mL
5 mM 0.0279 mL 0.1396 mL 0.2791 mL 0.6978 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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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:

Volanesorsen915430-78-3ISIS 304801ISIS304801ISIS-304801OthersInhibitorinhibitorinhibit

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