HAMI3379
中文名称 | HAMI3379 |
---|---|
中文同义词 | 化合物 T15463;哈密3379;化合物 (RAC)-HAMI 3379 |
英文名称 | HAMI3379 |
英文同义词 | HAMI3379;HRJWSEPIRZRGCL-UHFFFAOYSA-N;(Rac)-HAMI 3379;(Rac) HAMI 3379,(Rac)HAMI 3379;N-(3-carboxy-cyclo-hexyl-)-5-carboxy-2-(cyclo-hexyl-oxy-butyl-oxy-phenyl-propyl-oxy-)-benz-amide;Benzoic acid, 3-[[(3-carboxycyclohexyl)amino]carbonyl]-4-[3-[4-[4-(cyclohexyloxy)butoxy]phenyl]propoxy]- |
CAS号 | 712313-35-4 |
分子式 | C34H45NO8 |
分子量 | 595.72 |
EINECS号 | |
相关类别 | 小分子 |
Mol文件 | 712313-35-4.mol |
结构式 |
HAMI3379 性质
沸点 | 797.7±60.0 °C(Predicted) |
---|---|
密度 | 1.24±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | 乙醇中≤5mg/ml;DMSO 中≤20mg/ml;二甲基甲酰胺中≤20mg/ml |
形态 | 结晶固体 |
酸度系数(pKa) | 4.20±0.10(Predicted) |
颜色 | 白色至米白色 |
CysLT 2
|
In a CysLT
2
receptor reporter cell line, HAMI 3379 antagonizes leukotriene D
4
- (LTD
4
-) and leukotriene C
4
- (LTC
4
-) induced intracellular calcium mobilization with IC
50
values of 3.8 nM and 4.4 nM, respectively. In contrast, HAMI 3379 exhibits very low potency on a recombinant CysLT
1
receptor cell line (IC
50
>10000 nM).
HAMI 3379 (ip; 0.025-0.4 mg/kg; 24 hours) attenuates the acute brain injury 24 hours after middle cerebral artery occlusion (MCAO) with effective doses of 0.1-0.4 mg/kg and a therapeutic window of ∼1 hour. It attenuates the neurological deficits, and reduces infarct volume, brain edema, and neuronal loss and degeneration 24 and 72 hours after MCAO.
HAMI 3379 (infused into the aortic cannula at a rate of 1% of the total flow rate; 0.01, 0.1, 1 μM; 20 min) concentration-dependently inhibits and reverses the LTC
4
-induced perfusion pressure increase and contractility decrease.
Animal Model: | Male Sprague-Dawley rats (250-300 g) after MCAO |
Dosage: | 0.025, 0.05, 0.1, 0.2, 0.4 mg/kg |
Administration: | IP; 24 hours |
Result: | Attenuated the acute brain injury 24 hours after MCAO with effective doses of 0.1-0.4 mg/kg and a therapeutic window of ∼1 hour. |