当前位置: 易推广 > 生物试剂/抗体/细胞 > 生化试剂 > 其他 > MedChemExpress > 产品展示 > MCE信号通路 > 蛋白偶联受体/G 蛋白 > Pranlukast hemihydrate
Pranlukast hemihydrate
企业档案
会员类型:会员
已获得易推广信誉 等级评定
(0 -40)基础信誉积累,可浏览访问
(41-90)良好信誉积累,可接洽商谈
(91+ )优质信誉积累,可持续信赖
易推广会员:8年
最后认证时间:
注册号: 【已认证】
法人代表: 【已认证】
企业类型:生产商 【已认证】
注册资金:人民币万 【已认证】
产品数:91228
参观次数:11349402
联系我们
MedChemExpress
电话:021-58955995
联系人:客服部 (请说明是在易推广看到的!谢谢)
手机:13611715263
邮编:201203
邮箱:sales@medchemexpress.cn
地址:上海上海
详细内容
MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
Pranlukast hemihydrate
CAS No. : 150821-03-7
MCE 站:Pranlukast hemihydrate
产品活性: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。
研究领域:GPCR/G Protein
作用靶点:Leukotriene Receptor
In Vitro: In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings 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]LTD4 binding 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 pA2 range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC4 to 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. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT1 receptors is inhibited by pretreatment with the CysLT1 receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT1 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 CysLT1 receptor 6 h after OGD.
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).
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | MK-571 sodium salt | Montelukast sodium | MK-886 | Zafirlukast | Pranlukast | Nedocromil | LY223982 | CP-105696 | HAMI 3379 | Leukotriene B4 | LY255283 | (S)-Verapamil hydrochloride | 5-O-Demethylnobiletin | BIIL-260 hydrochloride | Etalocib | 11-?Keto-?beta-?boswellic acid | 12S-HHT | AS-35 | Darbufelone | KP496 | RG-12525 | Veliflapon | CP-96021 hydrochloride | LM-1484 | Quinotolast sodium | RS-601
品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物;
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果;
• 专业团队跟踪*新的制药及生命科学研究进展,为您提供全球*新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。
热门标签:Ultair