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GSK805

Catalog No. T7388 CAS 1426802-50-7

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

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GSK805, CAS 1426802-50-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
2 mg	In stock	$ 72.00
5 mg	In stock	$ 123.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 397.00
50 mg	In stock	$ 486.00
100 mg	In stock	$ 697.00
200 mg	In stock	$ 997.00
1 mL * 10 mM (in DMSO)	In stock	$ 146.00

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Purity: 98.23%

Purity: 98%

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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
In vitro	GSK805 inhibits the expression of IL-17 (at 0.5 μM) in na?ve 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[1].
In vivo	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[1].
Cell Research	CD4+CD62LhighCD25? naive CD4+ T cells were purified by FACS sorting following a MACS bead isolation of CD4+ cells. Naive CD4+ cells were activated with plate-bound anti-CD3 (2 μg/ml) and anti-CD28 (2 μg/ml). For Th17 cell differentiation, cultures were supplemented with IL-6 (20 ng/ml) plus TGF-β1 (1 ng/ml), and IL-23 (10 ng/ml) was added after 48 h. RORγt inhibitors or vehicle control DMSO was also included in the cultures. After 96 h, cells were collected for further experiments[1].

Molecular Weight	532.36
Formula	C23H18Cl2F3NO4S
CAS No.	1426802-50-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (187.84 mM)

References and Literature

1. Xiao S , Yosef N , Yang J , et al. Small-Molecule RORγt Antagonists Inhibit T Helper 17 Cell Transcriptional Network by Divergent Mechanisms[J]. Immunity, 2014, 40(4):477-489. 2. Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors[J]. ACS Medicinal Chemistry Letters:-.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library Immunology/Inflammation Compound Library Nuclear Receptor Compound Library Bioactive Compounds Library Max Lipid Metabolism Compound Library Orally Active Compound Library NO PAINS Compound Library CNS-Penetrant Compound Library

Related Products

Related compounds with same targets

S18-000003 RORγt inverse agonist 14 SR1001 RORγt Inverse agonist 8 T0901317 ML 209 Neoruscogenin RORγt inverse agonist 31

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Keywords

GSK805 1426802-50-7 Metabolism ROR GSK 805 immunity RAR-related orphan receptor Inhibitor inhibit oral CNS penetrant Th17 cell GSK-805 inhibitor

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