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531369 RORγt Inverse Agonist II, GSK805 - CAS 1426802-50-7 - Calbiochem

A cell-permeable, potent, non-toxic, inverse agonist of RORγt. Directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: N-(3,5-Dichloro-4-(2-(trifluoromethoxy)phenyl)phenyl)-2-(4-ethylsulfonylphenyl)acetamide, N-(2,6-Dichloro-2ʹ-(trifluoromethoxy)biphenyl-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide, Retinoid-related Orphan Receptor γ t Antagonist II, RORγt Antagonist II; GSK'805

Primary Target: RORγt
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531369
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Tableau de caractéristiques principal

CAS #Empirical Formula
1426802-50-7C₂₃H₁₈Cl₂F₃NO₄S

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      Description
      OverviewA cell-permeable, orally available, non-toxic, conformationally restricted biaryl-amide compound that acts as a potent retinoid-related orphan receptor γt (RORγt) isoform selective inverse agonist and suppresses T helper 17 (Th17) responses, including IL-17 and IFN-γ production (~ 500 nM). Directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects, however, it does not affect RORγt binding to DNA. Induces RORγt binding to Gata3 resulting in increased expression of GATA3. Reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531369
      Brand Family Calbiochem®
      SynonymsN-(3,5-Dichloro-4-(2-(trifluoromethoxy)phenyl)phenyl)-2-(4-ethylsulfonylphenyl)acetamide, N-(2,6-Dichloro-2ʹ-(trifluoromethoxy)biphenyl-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide, Retinoid-related Orphan Receptor γ t Antagonist II, RORγt Antagonist II; GSK'805
      References
      ReferencesXiao, S., et al. 2014. Immunity. 40, 477.
      Product Information
      CAS number1426802-50-7
      FormOff-white powder
      Hill FormulaC₂₃H₁₈Cl₂F₃NO₄S
      Chemical formulaC₂₃H₁₈Cl₂F₃NO₄S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetRORγt
      Purity≥95% 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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5313690001 04055977242713

      Documentation

      RORγt Inverse Agonist II, GSK805 - CAS 1426802-50-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      RORγt Inverse Agonist II, GSK805 - CAS 1426802-50-7 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      531369

      Références bibliographiques

      Aperçu de la référence bibliographique
      Xiao, S., et al. 2014. Immunity. 40, 477.

      Brochure

      Titre
      NPI Flyer- Epigenetics and Nuclear Function Feature
      New Products - Antibodies, Small Molecule, Inhibitors

      Informations techniques

      Titre
      White Paper: Further considerations of antibody validation and usage.
      Fiche technique

      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.

      Revision12-September-2014 JSW
      SynonymsN-(3,5-Dichloro-4-(2-(trifluoromethoxy)phenyl)phenyl)-2-(4-ethylsulfonylphenyl)acetamide, N-(2,6-Dichloro-2ʹ-(trifluoromethoxy)biphenyl-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide, Retinoid-related Orphan Receptor γ t Antagonist II, RORγt Antagonist II; GSK'805
      DescriptionA cell-permeable, orally available, non-toxic, conformationally restricted biaryl-amide compound that acts as a potent retinoid-related orphan receptor γt (RORγt) isoform selective inverse agonist and suppresses T helper 17 (Th17) responses, including IL-17 and IFN-γ production (~ 500 nM). Directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects, however, it does not affect RORγt binding to DNA. Induces RORγt binding to Gata3 resulting in increased expression of GATA3. Reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1426802-50-7
      Chemical formulaC₂₃H₁₈Cl₂F₃NO₄S
      Purity≥95% by HPLC
      SolubilityDMSO (100 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesXiao, S., et al. 2014. Immunity. 40, 477.