Molecular Weight(MW): 312.05
AS101, a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.
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|Description||AS101, a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.|
Treatment of caspase-1 (interleukin-1 [IL-1] converting enzyme [ICE]) with AS101 inhibits its enzymatic activity in a dose-dependent manner. Moreover, AS101 treatment 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 AS101 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. 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 AS101 (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.
|In vivo||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, AS101 also exerted beneficial effects. AS101 treated rats showed a large increase in SIRT1 protein levels in the liver and kidney extracts of rats treated with AS101. AS101 prevents development of insulin resistance in vivo. AS101 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.|
|In vitro||DMSO||62 mg/mL (198.68 mM)|
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03216538||Recruiting||Neovascular Age-related Macular Degeneration||Feramda||September 2018||Phase 1|Phase 2|
|NCT01943630||Recruiting||External Genital Warts||BioMAS Ltd||January 2015||Phase 2|
|NCT01010373||Suspended||Acute Myeloid Leukemia|Myelodysplastic Syndrome||BioMAS Ltd||January 2015||Phase 2|
|NCT01555112||Completed||Wart; External Genital Organs|Condyloma Acuminata||BioMAS Ltd||March 2012||Phase 1|Phase 2|
|NCT00926354||Terminated||Chemotherapy Induced Thrombocytopenia||BioMAS Ltd||August 2009||Phase 2|
|NCT00927212||Terminated||Atopic Dermatitis||BioMAS Ltd||June 2009||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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