BiochemProbe — Life Science Research Reagents

GSK805 free base · Synonyms: GSK-805 · GSK 805

GSK805 is an orally active and CNS penetrant RORγt inhibitor.

For research use only. Not for human or veterinary use.

Target ROR
Research area Inflammation/Immunology
Purity >98% Stock Inquire

GSK805 structure

CAS No.: 1426802-50-7

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
100 mg USD 420.00 BP-02142-100mg In stock Get quote
250 mg USD 800.00 BP-02142-250mg In stock Get quote
500 mg USD 1,280.00 BP-02142-500mg In stock Get quote
1 g USD 2,100.00 BP-02142-1g In stock Get quote
2 g USD 3,200.00 BP-02142-2g In stock Get quote
3 g USD 3,980.00 BP-02142-3g In stock Get quote

Need another size or custom synthesis? Request a quote.

Description

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 .

Biological activity

In Vitro GSK805 (0.5 μM; 4 d) inhibits Th17 cell responses. In Vivo GSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE). GSK805 (30 mg/kg) inhibits Th17 cell responses in EAE mice.

Identifiers

SMILES
CCS(=O)(=O)C1=CC=C(CC(=O)NC2=CC(Cl)=C(C(Cl)=C2)C2=CC=CC=C2OC(F)(F)F)C=C1
InChIKey
CEICQMBWAQAIQX-UHFFFAOYSA-N

Specifications

MW (average)
532.3600
Formula
C23H18Cl2F3NO4S
CAS No.
1426802-50-7
Physical state
Solid
Color
White to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 year;

Solubility

Soluble in DMSO

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.
[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.

Same target

Search ROR

Same research area

Search Inflammation/Immunology