LY255283

LY255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂,抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。

CAS号

117690-79-6

分子式

C19H28N4O3

主要靶点

Leukotriene Receptor

仅限科研使用

Cat No : CM05004

Print datasheet

Synonyms

LY 255283



产品信息

LY255283 is a specific antagonit of leukotriene B4 (LTB4) receptor. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.

CAS号 117690-79-6
分子式 C19H28N4O3
主要靶点 Leukotriene Receptor
主要通路 G蛋白偶联受体
分子量 360.46
纯度 99.45%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 LY 255283

靶点活性

LTB 4:100 nM (IC50, LTB4binds to guinea pig lung membranes)

体内活性

All seven rats given only the vehicle died within 2 h of reperfusion, whereas rats treated with LY-255283 (3 or 10 mg/kg iv), a leukotriene B4 (LTB4) receptor antagonist given 10 min before reperfusion, exhibited significantly higher survival rates of 57% (4 out of 7) and 75% (6 out of 8), respectively, 2 h after reperfusion.?Rats given 1 mg/kg of LY-255283 showed no significant improvement in survival.?Splanchnic artery occlusion (SAO)-shock rats treated with LY-255283 (3 or 10 mg/kg) exhibited significantly attenuated accumulation of plasma free amino-nitrogenous compounds and of a myocardial depressant factor.?Treatment with LY-255283 (10 mg/kg) markedly (P less than 0.01) ameliorated the deficits of endothelium-dependent relaxation of isolated superior mesenteric artery (SMA) rings in untreated SAO-shock rats.?LY-255283 at 10 mg/kg significantly attenuated the increased myeloperoxidase activity in the intestinal tissue of SAO-shock rats[1].

溶解度

DMSO:25 mg/mL (69.36 mM)

参考文献

1.Karasawa A , Guo J P , Ma X L , et al. Protective actions of a leukotriene B4 antagonist in splanchnic ischemia and reperfusion in rats.[J]. Am J Physiol, 1991, 261(2):191-8.
2.M Uğur, M Melli.Inhibitory effect of LY 255283 on the synthesis of leukotriene B(4) and thromboxane A(2) in human peripheral blood polymorphonuclear leukocytes and monocytes.Mediators Inflamm. 1993;2(6):407-9.

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