Ossirene

Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.

Product information

CAS Number: 106566-58-9

Molecular Weight: 312.05

Formula: C2H8Cl3NO2Te

Synonym:

AS101

Chemical Name: ammonium 2, 2, 2-trichloro-1, 3, 2-dioxatellurolane

Smiles: [NH4+].[Cl-][Te+4]1([Cl-])([Cl-])[O-]CC[O-]1

InChiKey: AXWLPMGUUAIGJK-UHFFFAOYSA-O

InChi: InChI=1S/C2H4Cl3O2Te.H3N/c3-8(4,5)6-1-2-7-8;/h1-2H2;1H3/q-1;/p+1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Ossirene (AS101; 1 μg/mL; for 24 hours) almost completely abrogates expression of pStat3. Ossirene may reduce expression of Bcl-2 after inhibition of Stat3 activation via IL-10 inhibition. AS101 (0.5, 5 mg/mL; 24 hours) inhibits IL-1β-induced mRNA expression of inflammatory mediators in the RPE in a dose-dependent manner. AS101 inhibits IL-1β-induced mRNA expression and protein production of IL-6 and IL-8 in RPE cells. AS101 (5 mg/mL; 1 hour) inhibits the phosphorylation of the p65 component of the NFκB complex activated by IL-1β. Ossirene (0.1, 0.5, 1, 2.5 μg/mL) significantly decreases B16 melanoma, stomach adenocarcinoma, and human glioblastoma multiforme (GBM) cells proliferation. AS101 (0.5 μg/mL; for 24 hours) sensitizes GBM tumor cells to paclitaxel in an IL-10-dependent manner.

In Vivo:

Ossirene (AS101; 0.5 mg/kg/day; IP; 25 days) sensitizes GBM tumors to paclitaxel via inhibition of IL-10, resulting in increased survival.

References:

1. Diamond Ling, et al. The Tellurium Redox Immunomodulating Compound AS101 Inhibits IL-1β-activated Inflammation in the Human Retinal Pigment Epithelium. Br J Ophthalmol. 2013 Jul;97(7):934-8.
2. Sredni B, et al. Ammonium trichloro(dioxoethylene-o,o')tellurate (AS101) sensitizes tumors to chemotherapy by inhibiting the tumor interleukin 10 autocrine loop. Cancer Res. 2004 Mar 1;64(5):1843-52.
3. Yona Kalechman, et al. Inhibition of interleukin-10 by the Immunomodulator AS101 Reduces Mesangial Cell Proliferation in Experimental Mesangioproliferative Glomerulonephritis: Association With Dephosphorylation of STAT3. J Biol Chem. 2004 Jun 4;279(23):24724-32.
4. Yafit Hachmo, et al. The Small Tellurium Compound AS101 Ameliorates Rat Crescentic Glomerulonephritis: Association With Inhibition of Macrophage Caspase-1 Activity via Very Late Antigen-4 Inactivation. Front Immunol. 2017 Mar 7;8:240.

Products are for research use only. Not for human use.