普鲁司特, 胱氨酰白三烯受体 1 拮抗剂

免疫学与炎症相关拮抗剂
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货号 (SKU) 包装规格 是否现货 价格 数量
P408556-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 ONO-1078 | N-​[4-​oxo-​2-​(2H-​tetrazol-​5-​yl)​-​4H-​1-​benzopyran-​8-​yl]​-​4-​(4-​phenylbutoxy)​-benzamide
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Pranlukast
生化机理 普萘卡斯特(ONO-1078)是一种口服的半胱氨酰白三烯(LT)C(4)、LTD(4)和LTE(4)选择性拮抗剂,用于慢性支气管哮喘的预防性治疗。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 胱氨酰白三烯受体 1 拮抗剂
产品介绍

产品介绍:
普鲁司特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。

Information

Pranlukast Pranlukast (ONO-1078) is an orally administered, and selective antagonist of the cysteinyl leukotrienes (LT) C(4), LTD(4) and LTE(4), used in the prophylactic treatment of chronic bronchial asthma.
In vitro

Pranlukast inhibits NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells by about 40% & 30%, respectively. Pranlukast and MK-571 inhibit NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells in a dose-related manner. Pranlukast and MK-571 inhibits LPS-induced IL-6 production in PBMC by about 65% and 15%, respectively. Pranlukast or zafirlukast significantly inhibits 10 mM LTD4-evoked 35SO4 output in a concentration-dependent fashion, with maximal inhibitions of 83% at 10 mM Pranlukast and 78% at 10 mM Zafirlukast, and IC50 values of 0.3 mM for Pranlukast and 0.6 mM for Zafirlukast. Pranlukast (0.5 microM) causes a parallel rightward shift of the LTD4 concentration-response curve with a pKB of 7. Pranlukast or Zafirlukast (5 microM each) significantly suppresses ovalbumin-induced secretion in tracheae from sensitized guinea-pigs by 70% and 65%, respectively. Pranlukast also inhibits NF-kappaB activation induced by phorbol 12-myristate 13-acetate (PMA). Pranlukast also significantly inhibits LPS-induced MUC2 mRNA expression by reverse transcription-polymerase chain reaction (RT-PCR) analysis in NCI-H292 cells. Pranlukast also inhibits LPS-induced MUC2 gene expression in HM3-MUC2 cells.

In vivo

Pranlukast significantly reduces lesion volume, and increases neuron densities in the cortex and hippocampal CA1 region in the ischemic hemispheres of mice. Pranlukast also remarkably reduces the thickness of a scar wall in the ischemic hemispheres of mice.
Cell Data

cell lines:Oocytes

Concentrations:

Incubation Time:

Powder Purity:≥99%

关联靶点(人)

CYSLTR2 Tchem 半胱氨酰白三烯受体 2(Cysteinyl leukotriene receptor 2) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYSLTR1 Tclin 半胱氨酰白三烯受体 1(Cysteinyl leukotriene receptor 1) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES O=C(NC1=CC2=C(C=C1)C(=O)C=C(O2)C3=NN=N[NH]3)C4=CC=C(OCCCCC5=CC=CC=C5)C=C4
分子量 481.5

安全和危险性(GHS)

技术规格说明书

Concentration(Compounding value) 9.0-11(mmol/L)
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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