CAS NO: | 103177-37-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
100mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Pranlukast is a highly potent, selective and competitive antagonist of peptideleukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4bindings to lung membranes withKis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [3H]LTD4binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC4- and LTD4-induced contractions of guinea pig trachea and lung parenchymal strips with a pA2range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC4to LTD4, Pranlukast also antagonizes the LTC4-induced contraction of guinea pig trachea (pA2=7.78). Pranlukast significantly reverses the LTD4-induced prolonged contraction without effect on the KCl- and BaCl2-induced contractions of guinea pig trachea[1]. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT1receptors is inhibited by pretreatment with the CysLT1receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT1receptor 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 CysLT1receptor 6 h after OGD[2]. | ||||||||||||||||
体内研究 (In Vivo) | 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 481.50 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H23N5O4 | ||||||||||||||||
CAS 号 | 103177-37-3 | ||||||||||||||||
中文名称 | 普鲁司特 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(69.22 mM;Need ultrasonic) H2O : 0.67 mg/mL(1.39 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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