General description
A cell-permeable, bioactive, non-toxic oxadiazolohydroxyamidine based compound that acts as a potent, selective and competitive inhibitor of indoleamine 2,3-dioxygenase (IDO; IC50 = 67 nM for hIDO). Reversibly binds to the catalytically active heme iron (Fe2+) and is inactive towards closely related tryptophan 2,3-dioxygenase (TDO; IC50 >10 µM). Shown to dose-dependently decrease kynurenine levels (IC50 = 19 & 46 nM in HeLa treated with IFN-γ & B16-GM-CSF melanoma cells, respectively) and suppress B16-GM-CSF xenograft tumor growth in C57BL/6 mice (75 mg/kg, s.c., b.i.d.). Though orally bioavailable, but undergoes a rapid clearance (t1/2<0.5 h).
A cell-permeable, bioactive, non-toxic oxadiazolohydroxyamidine based compound that acts as a potent, selective and competitive inhibitor of indoleamine 2,3-dioxygenase (IDO; IC50 = 67 nM for hIDO). Reversibly binds to the catalytically active heme iron (Fe2+) and is inactive towards closely related tryptophan 2,3-dioxygenase (TDO; IC50 >10 µM). Shown to dose-dependently decrease kynurenine levels (IC50 = 19 & 46 nM in HeLa treated with IFN-γ & B16-GM-CSF melanoma cells, respectively) and suppress B16-GM-CSF xenograft tumor growth in C57BL/6 mice (75 mg/kg, s.c., b.i.d.). Though orally bioavailable, but undergoes a rapid clearance (t1/2<0.5 h).
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: no
Primary Target
IDO
Reversible: yes
Target IC50: 67 nM for hIDO
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Yue, E.W., et al. 2009. J. Med. Chem.52, 7364.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 271.64. Empirical Formula: C9H7ClFN5O2. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 50 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51112024
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5382560001