Molecular Formula | C24H21N3OS
|
Molar Mass | 399.51 |
Solubility | DMSO: >15mg/mL |
Appearance | powder |
Color | faint yellow to dark yellow |
Storage Condition | Sealed in dry,2-8°C |
MDL | MFCD17012805 |
Use | TAK-715 |
In vitro study | AK 715 inhibited LPS-stimulated TNF-α release from THP-1 with an IC50 of 48 nM. HK U2OS-EFC (10 μm) inhibited Wnt-3a of the induced phosphorylation of hDvl2 and hDvl2 conversion in cells. The amide NH of TAK715 binds to the main chain carbonyl group of Met109 of p38α by hydrogen bonding. AK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region, and the p38 front pocket, and extends over most of the length of the Gly-rich loop. |
In vivo study | When rats were orally treated with 10 mg/kg of HK 715, LPS-induced TNF-α production was inhibited by 87.6%. Ask 715 treated mice had a moderate bioavailability of 18.4% and treated rats had a slightly higher bioavailability of 21.1%. Rats treated with tae 715 had a Cmax of 0.19 μg/mL and an AUC(0-24 hours) of 1.16 μg-h/mL. The rat model of adjuvant-induced arthritis (AA) was treated orally with 30 mg/kg dose of ask 715, and the volume of the second toe was significantly reduced by 25%. |