普仑司特 - CAS:103177-37-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	普仑司特促销
英文名称:	Pranlukast
别名:	普仑司特 ONO 1078
CAS No:	103177-37-3	分子式:	C₂₇H₂₃N₅O₄	分子量:	481.5
CAS No:	103177-37-3
分子式:	C₂₇H₂₃N₅O₄
分子量:	481.5
MDL:	MFCD24539454	EINEC:	201-616-4
EINEC:	201-616-4

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P10021 普仑司特 ≥99% (psaitong)

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熔点：

236-238°C

包装规格：

100mg 1g 5g in poly bottle

溶解性：

溶于DMSO、甲醇、DMF（~ 20mg/ml）

产品描述：

基本信息

产品编号：	P10021
产品名称：	Pranlukast
CAS:	103177-37-3	储存条件	粉末	2-8℃	四年

分子式：	C27H23N5O4		溶于液体	-80℃	6个月
分子量：	481.50			-20℃	1个月
化学名：	N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-P-(4-phenylbutoxy)benzamide;N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-P-(4-phenylbutoxy)benzamide
Solubility (25°C)：
体外:	DMSO	11mg/mL (22.84mM)
	Ethanol	Insoluble
	Water	Insoluble
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.0768mL	10.3842mL	20.7684mL
5mM	0.4154mL	2.0768mL	4.1537mL
10mM	0.2077mL	1.0384mL	2.0768mL

生物活性

产品描述	半胱氨酰白三烯受体（CYSLTR1）选择性拮抗剂。减轻气道平滑肌收缩。降低支气管哮喘症状的可能性。
靶点	LTE4 0.63nM (Ki)	LTD4 0.99nM (Ki)	LTC4 5640nM (Ki)
体外研究	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±680nM,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 (10μM).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 6h after OGD.
体内研究	Carrageenan (CAR,5mg per mouse) is injected i.p.24h before LPS (50 p,g per mouse) is injected i.v.Various doses of Pranlukast (ONO-1078;40,20,and 10mmol/kg),AA-861 (20,10,and 5mmol/kg),Indomethacin (40mmollkg),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 0.6mmol/mL in 10% DMSO for AA-861 and 1.2mmol/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 (5mg 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 72h after LPS (50 p,g per mouse) administration,s.c.treatment with AA-861 (20mmol/kg) or Pranlukast (40mmol/kg) significantly increases the survival rate after the LPS administration (AA-861,P<0.001;Pranlukast,P<0.01).

推荐实验方法(仅供参考)

细胞实验:

EA.hy926 cells are cultured in Dulbecco's modified Eagle's medium (DMEM),supplemented with 10% heat-inactivated fetal calf serum,Penicillin (100 U/mL) and Streptomycin (100mg/mL).Experiments are conducted 24h after cells are seeded.OGD is performed.Briefly,the original medium is removed;the cells are washed twice with glucose-free Earle's balanced salt solution (EBSS) and placed in fresh glucose-free EBSS.Cultures are then placed in an incubator containing 5% CO2 and 95% N2 at 37℃ for 2 to 8h.Control cultures are maintained in glucose containing EBSS under normal conditions.10μM Pranlukast,10μM Zileuton,a 5-LOX inhibitor or 10μM Pyrrolidine dithiocarbamate (PDTC),is added to the culture 30 min before OGD exposure and maintained during OGD.

动物实验:

Mice

Male ddY mice are used.All mice used are 7 to 8 weeks of age.Endotoxin shock is induced in mice.In brief,CAR (5 mg in 0.5mL of physiological saline) is injected intraperitoneally (i.p.) as a priming agent 24h before LPS challenge. LPS (50 p,g in 0.5mL of physiological saline) is injected intravenously into the tail vein as an inducing agent.The indicated doses of AA-861,Pranlukast (40,20,and 10mmol/kg),saline,DMSO,or ethanol are administrated subcutaneously (s.c.) in a volume of 1mL into the backs of mice 30 min before the LPS provocation. Both drugs are injected s.c.,because CAR i.p.pretreatment caused peritonitis.To examine the role of endogenous TNF in CAR pretreated mice,2×105 U of rabbit anti-TNF-a antibody or normal serum of rabbit in 0.2mL is injected intravenously (i.v.) before the LPS challenge.

保存条件：

2-8℃

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