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Art. -Nr.: HY-112974

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Inotersen

(Synonyms: GSK-2998728; ISIS-420915)

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Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 96.44%
CAS. Nr.: 1492984-65-2
Molecular Weight:7183.08

Speicherung:

-20°C, stored under nitrogen, away from moisture

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

Inotersen Chemical Structure

CAS. Nr.: 1492984-65-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Inotersen inhibits the production of TTR in human hepatocellular carcinoma HepG2 cells in in vitro screening assays^[1].
Inotersen specifically and selectively detects anti-Inotersen antibodies in human plasma, with a sensitivity of 6.28 ng/mL, and exhibits strong drug tolerance. It can still recognize 100 ng/mL of anti-Inotersen antibodies even in the presence of 16.0 μg/mL of circulating Inotersen^[2].
Inotersen (10-1000 nM; 48 h) dose-dependently reduces the mRNA and protein levels of transthyretin (TTR) in the human hepatocellular carcinoma cell line HepG2^[3].

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

Cell Viability Assay^[3]

Cell Line:

HepG2, HepaRG
Concentration:

0 nM, 10 nM, 100 nM, 1000 nM
Incubation Time:

48 h
Result:

Dose-dependent reduced transthyretin (TTR) mRNA and protein levels:
At 10 nM, TTR mRNA decreased by approximately 20%, at 100 nM by approximately 50%, and at 1000 nM by approximately 75%, with protein levels showing a similar decreasing trend.

In Vivo

Inotersen (25 mg/kg) reduces TTR RNA and protein levels by 90% in human TTR^Ile84Ser transgenic mice, and reduces human TTR mRNA and protein levels by up to 80%, with no adverse effects on the overall health or liver function of mice^[1].
Inotersen (>40 mg/kg/week; 3-6 months) causes mild to moderate mononuclear cell infiltration in the hepatic sinusoids, lymph nodes and injection sites of mice after 3 and 6 months of administration, with no adverse effects on the overall health of the mice^[1].
Inotersen (10-80 mg/kg/w; s.c.; once weekly; 26 weeks) induces mild, dose-dependent changes in serum biochemical parameters and typical microscopic effects in Tg.rasH2 mice^[5].
Subcutaneous administration of Inotersen (0.5-6 mg/kg/w; s.c.; once weekly; 2 years) to Sprague-Dawley rats for up to 2 years induces dose-dependent non-neoplastic effects and subcutaneous fibrosarcomas at injection sites^[5].

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

Animal Model:

Macaca fascicularis (male and female)^[1]
Dosage:

3 mg/kg; 6 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

s.c.; days 1, 3, 5, 7 then once weekly; up to 39 weeks
Result:

Reported ADA incidence rates of 28.6% for 3 mg/kg, 50.0% for 6 mg/kg, 42.9% for 10 mg/kg, and 44.4% for 20 mg/kg.
Reported median ADA onset of 140 days for 3 mg/kg, 185 days for 6 mg/kg, 185 days for 10 mg/kg, and 140 days for 20 mg/kg.
Reported median peak titers of 1600 for 3 mg/kg, 800 for 6 mg/kg, 200 for 10 mg/kg, and 300 for 20 mg/kg (all including minimum required dilution of 50).
Observed elevated plasma trough inotersen concentrations in ADA-positive monkeys compared to ADA-negative monkeys, but no consistent differences in liver or kidney inotersen concentrations, liver TTR mRNA levels, or plasma TTR protein levels.
Observed no differences in complement C3 levels or platelet counts between ADA-positive and ADA-negative monkeys across any dose or treatment duration.

Chemical Information

CAS. Nr. 1492984-65-2
Appearance Solid
Molecular Weight 7183.08
Color White to off-white
SMILES

[Inotersen]
Synonyms

GSK-2998728; ISIS-420915
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen, away from moisture

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2242 KB)

Verweise

[1]. Mathew V, et al. Inotersen: new promise for the treatment of hereditary transthyretin amyloidosis. Drug Des Devel Ther. 2019;13:1515-1525. Published 2019 May 6. [Content Brief]

[2]. Yu RZ, et al. Immunogenicity Assessment of Inotersen, a 2'-O-(2-Methoxyethyl) Antisense Oligonucleotide in Animals and Humans: Effect on Pharmacokinetics, Pharmacodynamics, and Safety. Nucleic Acid Ther. 2020;30(5):265-275. [Content Brief]

[3]. Durwin A. The Effect of Cellular Glucose Levels on Inotersen-Mediated Target Reduction in in vitro Cell Models[J]. 2025.

[4]. Kim TW, et al. Carcinogenicity assessment of inotersen in Tg.rasH2 mice and Sprague-Dawley rats: Implications for 2'-MOE antisense oligonucleotides. Regul Toxicol Pharmacol. 2025;155:105743. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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