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LY171883
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY171883图片
CAS NO:88107-10-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
leukotriene D4 receptor antagonist, orally active
Cas No.88107-10-2
别名油酸三乙醇胺
化学名1-[2-hydroxy-3-propyl-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]-ethanone
Canonical SMILESCCCc1c(OCCCCc2nnn[nH]2)ccc(C(=O)C)c1O
分子式C16H22N4O3
分子量318.4
溶解度≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide
储存条件Room temperature
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

LY171883 is a leukotriene D4 receptor antagonist.

Leukotriene D4 is one of the leukotrienes, whose major function is to induce the smooth muscle contraction, leading to vasoconstriction and bronchoconstriction. Leukotriene D4 can also increase vascular permeability.

In vitro: In GH(3) cells, LY-171883 was able to reversibly increase the amplitude of Ca(2+)-activated K(+) current concentration-dependently with an EC(50) value of 15 μM. Moreover, the treatment of LY-171883 to cytosolic face did not affect single channel conductance of large-conductance Ca(2+)-activated K(+) channels in excised inside-out patches recorded from GH(3) cells, however, LY-171883 did increase the channel activity. In addition, the LY-171883-stimulated activity of BK(Ca) channels was dependent on membrane potential [1].

In vivo: The effect of LY-171883 on the respiratory and cardiovascular changes in endotoxemia was studied in unanesthetized sheep. In group one, LY-171883 at 4 mg/kg was i.v. injected. In group two, Escherichia coli endotoxin (1 μg/kg) was infused, and in group three, LY-171883 at 4 mg/kg was administered before and after the same dose of endotoxin. Results showed that infusion of LY-171883 in group one did not alter baseline ventilatory and cardiovascular measurements. In group two, a two-phase pulmonary response was found. An early pulmonary hypertension phase with a fall in cardiac index was observed in group three [2].

Clinical trial: Up to now, no clinical data have been released.

References:
[1] PC Li et al.  Enhanced Activity of Ca2+-Activated K+ Channels by 1-[2-Hydroxy-3-Propyl-4-[(1h-Tetrazol-5-Yl)butoxyl]phenyl] Ethanone (LY-171883) in Neuroendocrine and Neuroblastoma Cell Lines. J Cell Physiol 192 (2), 188-199. 8 2002.
[2] Gross D, Ben Dahan J, Landau EH, Krausz MM.  Effect of leukotriene inhibitor LY-171883 on the pulmonary response to Escherichia coli endotoxemia. Crit Care Med. 1990 Feb;18(2):190-7.