Home Immunology & Inflammation Interleukins inhibitor - Immunology & Inflammation related modulator Ossirene (AS101)

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Ossirene (AS101) Interleukins inhibitor

Cat.No.S8301

A potent in vitro and in vivo immunomodulator, Ossirene (AS101) is a novel inhibitor of IL-1beta converting enzyme.
Ossirene (AS101) Interleukins inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 312.05

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Chemical Information, Storage & Stability

Molecular Weight 312.05 Formula

C2H4Cl3O2Te.H4N

 Storage (From the date of receipt)
CAS No. 106566-58-9 Download SDF Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (198.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
IL-1β converting enzyme [1]
In vitro
Treatment of caspase-1 (interleukin-1 [IL-1] converting enzyme [ICE]) with Ossirene (AS101) inhibits its enzymatic activity in a dose-dependent manner. Moreover, it causes a significant reduction in the active form of IL-18 and IL-1 in peripheral blood mononuclear cells (PBMC) and in human HaCat keratinocytes. The inhibitory effect of this compound does not involve nitric oxide (NO) or interferon- (IFN- ), two possible regulators of IL-18 production, and does not occur at the mRNA level. It may exert effects through a posttranscriptional mechanism[1]. AS101 induced SIRT1 expression in a dose dependent manner in three different cell lines, HEK293, HL-60 and Rin-5f. Incubation of HEK293 and HL-60 cell lines with it (0.1-2.5μg/ml) resulted in a dose dependent reduction in PPARγ protein expression relative to the control cells, and the reduction of PPARγ expression is in parallel to increased SIRT1 expression[2].
In vivo
Ossirene (AS101) downregulates IL-18 and IL-1 serum levels in a mouse model of lipopolysaccharide (LPS)-induced sepsis, resulting in increased survival. It has also been shown to be protective against lethal and sublethal effects of irradiation and chemotherapy. In a model of cecal ligation and puncture (CLP)-induced sepsis in mice, this compound also exerted beneficial effects[1]. Treated rats showed a large increase in SIRT1 protein levels in the liver and kidney extracts. It prevents development of insulin resistance in vivo and affects SIRT1 related metabolic pathways by changing the insulin levels. AS101 treatment prevents hyperglycemia associated with T2D(type 2 diabetes) and some of the symptoms of the disease in the HFD(high fat diet)+STZ(Streptozotocin) rat model[2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01943630 Unknown status
External Genital Warts
BioMAS Ltd
 January 2015 Phase 2
NCT01010373 Suspended
Acute Myeloid Leukemia|Myelodysplastic Syndrome
BioMAS Ltd
 January 2015 Phase 2

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