847950-09-8
847950-09-8 結(jié)構(gòu)式
基本信息
6-(2,6-Dimethylphenyl)-2-[[4-(4-methyl-1-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one
6-(2,6-Dimethylphenyl)-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one
PyriMido[5',4':5,6]pyriMido[1,2-a]benziMidazol-5(6H)-one, 6-(2,6-diMethylphenyl)-2-[[4-(4-Methyl-1-piperazinyl)phenyl]aMino]-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
Lck Inhibitor (compound 25) exhibits good potency in the T-cell receptor-induced IL-2 secretion assay (IL-2, IC 50 =0.46 μM) and also inhibits subsequent T-cell proliferation (T-cell prolif, IC 50 =0.53 μM) in the same human T-cells. Lck Inhibitor also inhibits a human mixed lymphocyte reaction (huMLR) with a 10-fold increase in potency as compared to the other invitro cell assays utilizing purified human cells. Lck Inhibitor also displays inhibition of a mechanism-based biochemical cell assay probing Lck-dependent TCR-chain phosphorylation (TCR-chain). Lck Inhibitor shows a 10-fold reduction in potency when IL-2 is induced in a receptor-independent fashion by stimulating with phorbo lester and calcium ionophore (PMA/iono). Lck Inhibitor exhibits a similar level of potency when tested in a general proliferation assay using the human T-cell line, Jurkat (JKT).
Lck Inhibitor (0-60 mg/kg; p.o.; once daily; from day 9 today 17) shows a dose-dependent inhibition of arthritis.
Lck Inhibitor (p.o.; 5 mg/kg) treatment shows the C
max
, AUC
0-∞
, t
max
and F% are 82 ng/mL, 862 ng h/mL, and 17%, respectively.
| Animal Model: | Male Lewis rat (adjuvant-inducedarthritis model) |
| Dosage: | 0, 30, and 60 mg/kg |
| Administration: | P.o.; once daily; from day 9 today 17 |
| Result: | Showed a dose-dependent inhibition of arthritis, with an ED 50 estimated at 24 mg/kg. |
| Animal Model: | Sprague-Dawley Rats |
| Dosage: | P.o. (Pharmacokinetic Analysis) |
| Administration: | 5 mg/kg |
| Result: | The C max , AUC 0-∞ , t max and F% were 82 ng/mL, 862 ng h/mL, and 17%, respectively. |