531369 RORγt Inverse Agonist II, GSK805 - Calbiochem

531369
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₁₈Cl₂F₃NO₄S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31369.0001
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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
          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) 

          References

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

          Brochure

          Title
          NPI Flyer- Epigenetics and Nuclear Function Feature (EMD)
          New Products - Antibodies, Small Molecule, Inhibitors

          Technical Info

          Title
          White Paper: Further considerations of antibody validation and usage. (EMD)
          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 +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesXiao, S., et al. 2014. Immunity. 40, 477.