HAMI3379

生物活性靶点体外研究体内研究 HAMI3379 试剂级价格

HAMI3379

CAS号:712313-35-4
英文名:HAMI3379
中文名:HAMI3379
CBNumber:CB62591197
分子式:C34H45NO8
分子量:595.72
MOL File:712313-35-4.mol

HAMI3379化学性质

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 :≤5mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
形态 :crystalline solid
酸度系数(pKa) :4.20±0.10(Predicted)
颜色 :White to off-white

HAMI3379性质、用途与生产工艺

生物活性 HAMI 3379 是一种有效的，选择性的半胱氨酸白三烯 (CysLT2) 受体拮抗剂。HAMI 3379 对急性和亚急性缺血性脑损伤具有保护作用，并减轻小胶质细胞相关的炎症。
靶点

CysLT ₂
体外研究

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).

体内研究

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.