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509225 IFN-α Receptor 2 Agonist, RO8191 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(2,4-bis(Trifluoromethyl)imidazo[1,2-a][1,8]naphthyridin-8-yl)-1,3,4-oxadiazole, 8-(1,3,4-Oxadiazol-2-yl)-2,4-bis(trifluoromethyl)imidazo[1, 2-a][1, 8]naphthyridine, IFN-α R2 Agonist, Interferon-α Receptor 2 Agonist, IFN-α Receptor 2 Agonist, RO4948191

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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₄H₅F₆N₅O
Description
Overview

This product has been discontinued.



A non-cytotoxic imidazonaphthyridine compound that directly binds interferon-α receptor 2 (IFNAR2) extracelluar domain in a 1:1 ratio and activates cellular signaling via IFNAR2 homodimerization in an IFNAR1-independent manner, eliciting similar, but not identical, signaling events as those seen with IFN--α, IFN--β, or IFN--γ stimulation. While being a much stronger stimulant of STAT3 Y705/S727 & JAK1 Y1022/1023 phosphorylations, RO8191 is ineffective in inducing IFNAR1-dependent Tyk2 Y1054/1055 phosphorylations (10 µM for 15 min; in Huh-7 cultures). Effectively boosts host anti-HCV (EC50 = 200 nM in Huh-7-derived HCV replicon cell line) and anti-EMCV (90% viability with 1.23 µM RO8191 in EMCV-infected A549 cultures) by inducing ISG/IFN-stimulated genes expression both in cultures in vitro and in mice (30 mg/kg p.o.) in vivo
Catalogue Number509225
Brand Family Calbiochem®
Synonyms2-(2,4-bis(Trifluoromethyl)imidazo[1,2-a][1,8]naphthyridin-8-yl)-1,3,4-oxadiazole, 8-(1,3,4-Oxadiazol-2-yl)-2,4-bis(trifluoromethyl)imidazo[1, 2-a][1, 8]naphthyridine, IFN-α R2 Agonist, Interferon-α Receptor 2 Agonist, IFN-α Receptor 2 Agonist, RO4948191
References
ReferencesKonishi, H., et al. 2012. Sci. Rep. 2, 259.
Product Information
FormPale yellow powder
Hill FormulaC₁₄H₅F₆N₅O
Chemical formulaC₁₄H₅F₆N₅O
ReversibleY
Quality LevelMQ200
Applications
Biological Information
Primary Targetinterferon-α receptor 2 (IFNAR2)
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
509225 0

Documentation

IFN-α Receptor 2 Agonist, RO8191 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Konishi, H., et al. 2012. Sci. Rep. 2, 259.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision28-April-2014 JSW
Synonyms2-(2,4-bis(Trifluoromethyl)imidazo[1,2-a][1,8]naphthyridin-8-yl)-1,3,4-oxadiazole, 8-(1,3,4-Oxadiazol-2-yl)-2,4-bis(trifluoromethyl)imidazo[1, 2-a][1, 8]naphthyridine, IFN-α R2 Agonist, Interferon-α Receptor 2 Agonist, IFN-α Receptor 2 Agonist, RO4948191
DescriptionA non-cytotoxic (up to 10 µM and 7 d in human hepatocyte Huh-7-derived HCV replicon cultures) imidazonaphthyridine compound that directly binds to the extracelluar domain of interferon-α receptor 2 (IFNAR2) in a 1:1 stoichiometric ratio and activates cellular signaling events in a IFNAR2-dependent and IFNAR1-independent manner distinct from that of interferon-α, which stimulates cellular responses only via IFNAR1/2 heterodimerization. Cellular stimulation by RO8191 via IFNAR2 homodimerization elicits similar, but not identical, signaling events as those seen with IFN-α, IFN-β, or IFN-γ stimulation. While being a much stronger stimulator of STAT3 Y705/S727 & JAK1 Y1022/1023 phosphorylations, RO8191 is ineffective in inducing IFNAR1-dependent Tyk2 Y1054/1055 phosphorylations (1 & 10 µM; 15 min; in Huh-7 cultures). Effectively boosts host anti-HCV (EC50 = 200 nM in Huh-7-derived HCV replicon cell line) and anti-EMCV activity (90% vs. <3% viability with or without 1.23 µM RO8191 in EMCV-infected human A549 lung carcinoma cultures) by inducing ISG/IFN-stimulated genes expression both in cultures in vitro and in mice (30 mg/kg p.o.) in vivo and is efficacious in reducing serum HCV titre when administered to HCV-infected mice harboring humanized liver (30 mg/kg p.o.).
FormPale yellow powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₄H₅F₆N₅O
Purity≥97% by HPLC
SolubilityDMSO (2.5 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesKonishi, H., et al. 2012. Sci. Rep. 2, 259.