化合物 T24524
中文名称 | 化合物 T24524 |
---|---|
中文同义词 | 化合物 T24524;N,N-双(1,3-苯并二恶唑-5-甲基)-1-丁基-2,4-二苯基-1H-咪唑-5-甲胺;无损检测9513727 |
英文名称 | NDT 9513727 |
英文同义词 | NDT 9513727;N,N-Bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-Imidazole-5-methanamine;1H-Imidazole-5-methanamine, N,N-bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl- |
CAS号 | 439571-48-9 |
分子式 | C36H35N3O4 |
分子量 | 573.68 |
EINECS号 | |
相关类别 | 小分子;Agonist, Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals |
Mol文件 | 439571-48-9.mol |
结构式 |
化合物 T24524 性质
沸点 | 723.1±62.0 °C(Predicted) |
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密度 | 1.23±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | 二甲基亚砜:100mM;乙醇:100 mM |
形态 | 固体 |
酸度系数(pKa) | 6.69±0.50(Predicted) |
颜色 | 白色至黄色 |
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). |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-110060 | NDT 9513727 | 5 mg | 800元 | |
2024/04/30 | HY-110060 | 化合物 T24524 NDT 9513727 | 439571-48-9 | 10mg | 1360元 |