GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures.

In a dose-dependent manner,GSK2245035 (0.01, 0.1, 1, 10, 100, 1000, 10000 nM;?6 days) reduces levels of the Th2 cytokines IL-5 and IL-13 released in response to Timothy grass or house dust mite in human PBMC cultures derived from individuals allergic to these allergens.

GSK2245035 (3, 30, 300, 3000 ng/kg; 6 hours) treatment can make plasma IP-10 provided the most sensitive biomarker of target engagement with raised levels of this chemokine detected at doses of 30 ng/kg and above in the cynomolgus monkey.?GSK2245035 (i.n.; 0.03-1 mg/kg; 6 hours) makes dose-related increasing in IFNα levels in serum at doses of 0.3 mg/kg and above at the 2 h time point which had subsided at 6 h.

1207629-49-9

C20H34N6O2

390.52

GSK2245035

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years