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509225 IFN-α Receptor 2 Agonist, RO8191 - Calbiochem

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Synonyme: 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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      Übersicht

      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
      Bestellnummer GTIN
      509225 0

      Documentation

      IFN-α Receptor 2 Agonist, RO8191 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Konishi, H., et al. 2012. Sci. Rep. 2, 259.
      Datenblatt

      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.