2. Neuronal Signaling
  3. Transthyretin (TTR)
  4. Inotersen

Inotersen  (Synonyms: GSK-2998728; ISIS-420915)

Cat. No.: HY-112974 Purity: 96.44%
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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.

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

DNA, d(P-thio)([2'-O-(2-methoxyethyl)]m5rU-[2'-O-(2-methoxyethyl)]m5rC-[2'-O-(2-methoxyethyl)]m5rU-[2'-O-(2-methoxyethyl)]m5rU-[2'-O-(2-methoxyethyl)]rG-G-T-T-A-m5C-A-T-G-A-A-[2'-O-(2-methoxyethyl)]rA-[2'-O-(2-methoxyethyl)]m5rU-[2'-O-(2-methoxyethyl)]m5rC-[2'-O-(2-methoxyethyl)]m5rC-[2'-O-(2-methoxyethyl)]m5rC)

Inotersen Chemical Structure

CAS No. : 1492984-65-2

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3][4].

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.

Inotersen Related Antibodies

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 TTRIle84Ser 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.
Molecular Weight

7183.08

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[Inotersen]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

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

Purity & Documentation

Purity: 96.44%

SDS (252 KB)

COA (247 KB) LCMS (326 KB)

Handling Instructions (2242 KB)
References
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Inotersen Related Classifications

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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:

Inotersen1492984-65-2GSK-2998728 ISIS-420915GSK2998728GSK 2998728ISIS420915ISIS 420915ISIS-420915Transthyretin (TTR)thyroxine-binding prealbuminTg.rasH2 micecynomolgus monkeyshuman TTR Ile84Ser transgenic micetransthyretin (TTR)CD-1 micehuman hepatoma HepG2 cellsSprague Dawley ratshereditary transthyretin amyloidosishuman TTR mRNARNase H1Inhibitorinhibitorinhibit

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