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GSK805

Cat. No. M9221
GSK805 Structure
Synonym:

ROR gamma-t-IN-1

Size Price Availability Quantity
5mg USD 198  USD220 In stock
10mg USD 342  USD380 In stock
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Quality Control
Biological Activity

GSK805 is a potent, orally bioavailable RORγγ Inhibitor, with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay. GSK805 suppresses T helper 17 (Th17) responses, including IL-17 and IFN-γ production (~ 500 nM). GSK805 directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects. GSK805 induces RORγt binding to Gata3 resulting in increased expression of GATA3. GSK805 reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models EAE mice
Formulation
Dosages once daily at 3 doses (1, 3, and 10 mg/kg)
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 532.36
Formula C23H18Cl2F3NO4S
CAS Number 1426802-50-7
Purity 98.21%
Solubility DMSO 10 mM
Storage -20°C, protect from light
References

Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors.
Wang Y, et al. ACS Med Chem Lett. 2015 May 26;6(7):787-92. PMID: 26191367.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK805, ROR gamma-t-IN-1 supplier, ROR, inhibitors

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