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531369 RORγt Inverse Agonist II, GSK805 - 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.

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

Synonyms: 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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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₃H₁₈Cl₂F₃NO₄S

Pricing & Availability

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      		 Glass bottle 10 mg
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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
      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

      Documentation

      RORγt Inverse Agonist II, GSK805 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      RORγt Inverse Agonist II, GSK805 - Calbiochem Certificates of Analysis

      TitleLot Number
      531369

      References

      Reference overview
      Xiao, S., et al. 2014. Immunity. 40, 477.
      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.

      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
      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.