5.38256

IDO Inhibitor

• Synonyme(s) : IDO Inhibitor, 4-Amino-N-(3-chloro-4-fluorophenyl)-Nʹ-hydroxy-1,2,5-oxadiazole-3-carboximidamide, IDOi, Indoleamine 2,3-Dioxygenase Inhibitor
• Formule empirique (notation de Hill): C₉H₇ClFN₅O₂
• Numéro CAS: 914471-09-3
• Poids moléculaire : 271.64
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

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 (t_1/2<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 (t_1/2<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.

Actions biochimiques/physiologiques

Cell permeable: no

Primary Target
IDO

Reversible: yes

Target IC₅₀: 67 nM for hIDO

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Yue, E.W., et al. 2009. J. Med. Chem.52, 7364.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable