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

531369
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1426802-50-7C₂₃H₁₈Cl₂F₃NO₄S

Products

Catalogue NumberPackaging Qty/Pack
5.31369.0001 Glass bottle 10 mg
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
Catalogue Number GTIN
5.31369.0001 04055977242713

Documentation

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

Title

Safety Data Sheet (SDS) 

RORγt Inverse Agonist II, GSK805 - CAS 1426802-50-7 - 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
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.