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Metabolism ROR GSK805

GSK805

Catalog No. T7388   CAS 1426802-50-7
Purity 98.00% Datasheet

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

GSK805, CAS 1426802-50-7
Pack Size Availability Price/USD Quantity
2 mg In stock 113.00
5 mg In stock 162.00
10 mg In stock 286.00
25 mg In stock 572.00
50 mg In stock 858.00
100 mg In stock 1572.00
1 mL * 10 mM (in DMSO) In stock 292.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
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
Targets&IC50 RORγt,  
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

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 100 mg/mL (187.84 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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:-.

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TAK-828F Xylan Vimirogant AZD-0284 RORγt Inverse agonist 8 A-9758 S18-000003 FM26

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