2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
PI3Kγ:29 nM (IC50)
Akt:294 nM (IC50)
In Vivo
TASP0415914 (compound 8j; 10-100 mg/kg; orally administration; twice daily; for 14 days) treatment suppressed the progression of the disease in a dose-dependent manner in a mouse collagen-induced arthritis (CIA) model[1]. Animal Model: Collagen-primed DBA/1 mice[1] Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg Administration: Orally administration; twice daily; for 14 days Result: Suppressed the progression of the disease in a dose-dependent manner.
In Vitro
TASP0415914 (compound 8j) shows high metabolic stability in rat/human liver microsomes. TASP0415914 has no CYP inhibition up to 10 μM for CYP1A2, 2C9, 2C19, 2D6 and 3A4[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Yusuke Oka, et al. Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases. Bioorg Med Chem. 2013 Dec 15;21(24):7578-83.
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