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Pranlukast hemihydrate
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。
CAS NO:150821-03-7
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品介绍
Pranlukast hemihydrate (ONO-1078 hemihydrate) 是一种高效的竞争性的选择性leukotriene拮抗剂。Pranlukast 抑制 [3H]LTE4,[3H]LTD4和 [3H]LTC4与肺膜结合,Ki分别为 0.63±0.11,0.99±0.19 和 5640±680 nM。

产品描述

Pranlukast hemihydrate is a highly potent, selective and competitive antagonist of peptide leukotriene s. Pranlukast inhibits [ 3 H]LTE 4, [ 3 H]LTD 4, and [ 3 H]LTC 4 bindings to lung membranes with K i s of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.

体外活性

In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [ 3 H]LTE 4, [ 3 H]LTD 4, and [ 3 H]LTC 4 bindings to lung membranes with K i s of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [ 3 H]LTD 4 binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC 4 - and LTD 4 -induced contractions of guinea pig trachea and lung parenchymal strips with a pA 2 range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC 4 to LTD 4, Pranlukast also antagonizes the LTC 4 -induced contraction of guinea pig trachea (pA 2 =7.78). Pranlukast significantly reverses the LTD 4 -induced prolonged contraction without effect on the KCl- and BaCl 2 -induced contractions of guinea pig trachea [1]. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT 1 receptors is inhibited by pretreatment with the CysLT 1 receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT 1 receptor antagonist Pranlukast and the 5-lipoxygenase inhibitor Zileuton on translocation are also assessed. The results show that Pranlukast, but not Zileuton, inhibits the translocation of the CysLT 1 receptor 6 h after OGD [2].

体内活性

Carrageenan (CAR, 5 mg per mouse) is injected i.p. 24 h before LPS (50 p,g per mouse) is injected i.v. Various doses of Pranlukast (ONO-1078; 40, 20, and 10 mmol/kg), AA-861 (20, 10, and 5 mmol/kg), Indomethacin (40 mmollkg), and the controls are injected s.c. into mice 30 min before they are challenged with 50 p,g of LPS. The maximum soluble doses are 0.6 mmol/mL in 10% DMSO for AA-861 and 1.2 mmol/mL in 10% ethanol for Pranlukast. These solutions are used as the maximum doses for the treatments. The mortality of mice is significantly decreased in AA-861- Pranlukast-treated mice relative to that in the control mice. Pretreatment with CAR (5 mg i.p.) renders the mice more sensitive to the effect of LPS. Although the survival rate of mice treated with each solvent is 20% at 72 h after LPS (50 p,g per mouse) administration, s.c. treatment with AA-861 (20 mmol/kg) or Pranlukast (40 mmol/kg) significantly increases the survival rate after the LPS administration (AA-861, P<0.001; Pranlukast, P<0.01) [3].

Cas No.

150821-03-7

分子式

C54H48N10O9

分子量

981.039

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years