Pranlukast hemihydrate
(Synonyms: 普鲁司特半水合物; ONO-1078 hemihydrate) 目录号 : GC36956
A CysLT1 receptor antagonist
Cas No.:150821-03-7
Sample solution is provided at 25 µL, 10mM.
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Pranlukast is an orally bioavailable cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50s = 4.3-7.2 nM in radioligand binding assays).1 It is selective for the CysLT1 receptor over the CysLT2 receptor (IC50 = 3,620 nM for the human receptor).2 Pranlukast inhibits mucus secretion induced by leukotriene D4 in isolated guinea pig trachea with an IC50 value of 0.3 ?M.3 It inhibits TNF-α-induced NF-?B p65 nuclear localization in U937 and Jurkat cells when used at concentrations of 10 and 100 ?M.4 Pranlukast inhibits bronchoconstriction induced by LTC4 , LTD4, and LTE4 , but not LTB4 , in guinea pigs (ID50s = 0.8, 1, 0.7, and >500 ?g/kg, respectively).5 It reduces cortical infarct volume by 81.6% and decreases neuronal death in the cortex, hippocampus, and striatum in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 0.03 mg/kg.6
1.Lynch, K.R., O'Neill, G.P., Liu, Q., et al.Characterization of the human cysteinyl leukotriene CysLT1 receptorNature399(6738)789-793(1999) 2.Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al.Characterization of the human cysteinyl leukotriene 2 receptorJ. Biol. Chem.275(39)30531-30536(2000) 3.Liu, Y.-C., Khawaja, A.M., and Rogers, D.F.Effects of the cysteinyl leukotriene receptor antagonists pranlukast and zafirlukast on tracheal mucus secretion in ovalbumin-sensitized guinea-pigs in vitroBr. J. Pharmacol.124(3)563-571(1998) 4.Ichiyama, T., Hasegawa, S., Umeda, M., et al.Pranlukast inhibits NF-KB activation in human monocytes/macrophages and T cellsClin. Exp. Allergy33(6)802-807(2003) 5.Nakai, H., Konno, M., Kosuge, S., et al.New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationshipsJ. Med. Chem.31(1)84-91(1988) 6.Zhang, W.-P., Wei, E.-Q., Mei, R.-H., et al.Neuroprotective effect of ONO-1078, a leukotriene receptor antagonist, on focal cerebral ischemia in ratsActa Pharmacol. Sin.23(10)871-877(2002)
Cell experiment: | 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 (100 mg/mL). Experiments are conducted 24 h 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°C for 2 to 8 h. Control cultures are maintained in glucose-containing EBSS under normal conditions. 10 μM Pranlukast, 10 μM Zileuton, a 5-LOX inhibitor or 10 μM Pyrrolidine dithiocarbamate (PDTC), is added to the culture 30 min before OGD exposure and maintained during OGD[2]. |
Animal experiment: | Mice[3]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 0.5 mL of physiological saline) is injected intraperitoneally (i.p.) as a priming agent 24 h before LPS challenge. LPS (50 p,g in 0.5 mL of physiological saline) is injected intravenously into the tail vein as an inducing agent. The indicated doses of AA-861, Pranlukast (40, 20, and 10 mmol/kg), saline, DMSO, or ethanol are administrated subcutaneously (s.c.) in a volume of 1 mL 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 0.2 mL is injected intravenously (i.v.) before the LPS challenge[3]. |
References: [1]. Obata T, et al. In vitro antagonism of ONO-1078, a newly developed anti-asthma agent, against peptide leukotrienes in isolated guinea pig tissues. Jpn J Pharmacol. 1992 Nov;60(3):227-37. | |
| Cas No. | 150821-03-7 | SDF | |
| 别名 | 普鲁司特半水合物; ONO-1078 hemihydrate | ||
| Canonical SMILES | O=C(C1=CC=C(OCCCCC2=CC=CC=C2)C=C1)NC3=C4C(C(C=C(C5=NN=NN5)O4)=O)=CC=C3.[1/2].O | ||
| 分子式 | C27H23N5O4.1/2H2O | 分子量 | 490.51 |
| 溶解度 | DMSO: 25 mg/mL (50.97 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0387 mL | 10.1935 mL | 20.3869 mL |
| 5 mM | 0.4077 mL | 2.0387 mL | 4.0774 mL |
| 10 mM | 0.2039 mL | 1.0193 mL | 2.0387 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet