| Identification | Back Directory | [Name]
ROR gamma-t-IN-1 | [CAS]
1426802-50-7 | [Synonyms]
GSK805
ROR gamma-t-IN-1
GSK805
(GSK-805)
4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1(2H)-one
N-(2,6-dichloro-2'-(trifluoromethoxy)biphenyl-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide
N-[2,6-Dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)benzeneacetamide
Benzeneacetamide, N-[2,6-dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)- | [Molecular Formula]
C23H18Cl2F3NO4S | [MDL Number]
MFCD28902182 | [MOL File]
1426802-50-7.mol | [Molecular Weight]
532.36 |
| Chemical Properties | Back Directory | [Boiling point ]
617.1±55.0 °C(Predicted) | [density ]
1.434±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMF:3.0(Max Conc. mg/mL);5.64(Max Conc. mM)
DMSO:68.33(Max Conc. mg/mL);128.36(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.56(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);93.92(Max Conc. mM) | [form ]
A crystalline solid | [pka]
12.33±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor''s putative ligand binding domain without exerting significant effects on DNA binding.1 It inhibits the expression of IL-17 (at 0.5 μM) in naïve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction. | [Uses]
GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity[1]. | [in vivo]
GSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE)[2].
GSK805 (30 mg/kg; p.o. once) inhibits Th17 cell responses in EAE mice[2]. | Animal Model: | C57BL/6 mice were immunized with MOG35–55 plus CFA[2] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; 10 mg/kg once per day; for 35 days | | Result: | Efficiently ameliorated the severity of EAE in mice. |
| Animal Model: | C57BL/6 mice with EAE[2] | | Dosage: | 30 mg/kg | | Administration: | Oral gavage; 30 mg/kg once | | Result: | Reduced both IFN-γ-IL-17+ and IFN-γ+IL-17+ T cells without altered the frequency of TNF-α+ T cells in EAE mice. |
| [storage]
Store at -20°C | [References]
[1] Wang Y, et al. Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors. ACS Med Chem Lett. 2015 May 26;6(7):787-792. DOI:10.1021/acsmedchemlett.5b00122
[2] Xiao S, et al. Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms. Immunity. 2014 Apr 17;40(4):477-89. DOI:10.1016/j.immuni.2014.04.004 |
|
| Company Name: |
Struchem Co., Ltd.
|
| Tel: |
0512-0512-63009836 15365350169 |
| Website: |
http://www.struchem.com |
|