439571-48-9
439571-48-9 結(jié)構(gòu)式
基本信息
無損檢測9513727
N,N-雙(1,3-苯并二惡唑-5-甲基)-1-丁基-2,4-二苯基-1H-咪唑-5-甲胺
N,N-Bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-Imidazole-5-methanamine
物理化學(xué)性質(zhì)
常見問題列表
IC50: 11.6 nM (human C5aR)
NDT 9513727 inhibits C5a-stimulated responses, including guanosine 5'-3-O-(thio)triphosphate binding, Ca
2+
mobilization, oxidative burst, degranulation, cell surface CD11b expression and chemotaxis in various cell types with IC
50
s from 1.1 to 9.2 nM, respectively.
NDT 9513727 (3-30 mg/kg; p.o.) exhibits a dose-dependent inhibition of hC5a-induced neutropenia.
NDT 9513727 exhibits moderate oral bioavailability (rat 73%, monkey 26%) and C
max
(rat 5.98 μM, monkey 830 nM) following oral administration (rat 50, monkey 25.2 mg/kg).
NDT 9513727 exhibits moderate plasma elimination half-lives (rat 4.8, monkey 7.9 h) due to low plasma clearance (1.4 L/h/kg and 3.8 l/h/kg respectively) following oral administration (rat 50, monkey 25.2 mg/kg).
| Animal Model: | Six-week-old Mongolian gerbils |
| Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral administration |
| Result: | Significantly inhibited hC5a-induced neutropenia at 3 mg/kg, 10 mg/kg, 30 mg/kg. |
| Animal Model: | Rat |
| Dosage: | 50 mg/kg |
| Administration: | Oral administration |
| Result: | Oral bioavailability (73%), C max (5.98 μM), T 1/2 (4.8 h). |
| Animal Model: | Monkey |
| Dosage: | 25.2 mg/kg |
| Administration: | Oral administration |
| Result: | Oral bioavailability (26%), C max (830 nM), T 1/2 (7.9 h). |