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扎鲁斯特

5-脂氧合酶抑制剂和CysLT1拮抗剂
规格或纯度: ≥99%
有货

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
Z129979-25mg
25mg 现货 Stock Image
Z129979-50mg
50mg 现货 Stock Image
Z129979-100mg
100mg 现货 Stock Image

基本描述

规格或纯度 ≥99%
英文名称 Zafirlukast
别名 扎鲁司特|扎鲁斯特|N-[3-[[2-甲氧基-4-[[[(2-甲苯基)磺酰基]氨基]羰基]苯基]甲基]-1-甲基-1H-吲哚-5-基]氨基甲酸环戊酯|[3-[2-甲氧基-4-[(邻甲苯基磺酰基)氨甲酰基]苯甲基]-1-甲基-1H-吲哚-5-基]氨基甲酸环戊酯
英文别名 zafirlukast|107753-78-6|Accolate|Olmoran|Cyclopentyl (3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methyl-1H-indol-5-yl)carbamate|ICI-204219|Accoleit|Vanticon|ICI 204219|ICI 204,219|Cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-
生化机理 Zafirlukast is a potent subtype specific cysteinyl leukotriene type 1 receptor (CysLT1) antagonist; antiasthmatic. The cysteinyl-leukotrienes (CysLTs), LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, aμgment microvascular permeability, and are vasoconstrictors of coronary arteries.5-lipoxygenase inhibitor and CysLT1 antagonist. Attenuates CNS infiltration of inflammatory cells, shows antiasthmatic and anti-inflammatory effects in vivo. Orally active.
应用 A potent and selective CysLT1 receptor antagonist.
储存温度 -20°C储存,充氩
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Zafirlukast是一种白三烯受体拮抗剂(LTRA),IC50为0.6μM,作用于CYP2C9,IC50为7.0 μM。A potent and selective CysLT1 receptor antagonist.

产品介绍:

Zafirlukast 是一种有效的具有口服活性的白三烯 D4 (LTD4) 受体拮抗剂。Zafirlukast 具有平喘、抗炎和抗菌作用

Zafirlukast is a leukotriene receptor antagonist (LTRA). (IC50=0.6μM, IC50=7.0 μM for CYP2C9).
A potent and selective CysLT1 receptor antagonist.

Product description:

Zafirlukast is a potent leukotriene D4 (LTD4) receptor antagonist with oral activity. Zafirlukast has antiasthmatic, anti-inflammatory and antibacterial effects

Application:

Zafirlukast has been used to stimulate pancreatic β cell line (MIN6) and pancreatic islets for insulin secretion assay. It may be used as an adenosine triphosphate-binding cassette transporter (ABCG2) inhibitor in MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] cytotoxicity assay in human embryonic kidney cells (HEK293) and in Kirby-Bauer disc diffusion assays, bactericidal activity and minimal inhibitory concentration (mIC) assay against M. smegmatis ?

名称和标识符

IUPAC Name cyclopentyl N-[3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methylindol-5-yl]carbamate
INCHI InChI=1S/C31H33N3O6S/c1-20-8-4-7-11-29(20)41(37,38)33-30(35)22-13-12-21(28(17-22)39-3)16-23-19-34(2)27-15-14-24(18-26(23)27)32-31(36)40-25-9-5-6-10-25/h4,7-8,11-15,17-19,25H,5-6,9-10,16H2,1-3H3,(H,32,36)(H,33,35)
InChi Key YEEZWCHGZNKEEK-UHFFFAOYSA-N
Canonical SMILES CC1=CC=CC=C1S(=O)(=O)NC(=O)C2=CC(=C(C=C2)CC3=CN(C4=C3C=C(C=C4)NC(=O)OC5CCCC5)C)OC
WGK Germany 3
PubChem CID 5717
分子量 575.68

化学和物理性质

溶解性 不溶于水,可溶于二甲基甲酰胺,微溶于丙酮,不溶于甲醇, 甲苯
敏感性 对空气敏感;对湿度敏感

安全和危险性(GHS)

危险声明 H413: May cause long lasting harmful effects to aquatic life
WGK Germany 3
Merck Index 10108

关联配体

Ligand ID 3322
名称 zafirlukast
别名 Accolate®
类别 Synthetic organic
学名 cyclopentyl N-{3-[(2-methoxy-4-{[(2-methylbenzene)sulfonyl]carbamoyl}phenyl)methyl]-1-methyl-1H-indol-5-yl}carbamate
生物活性评价 Zafirlukast shows low potency off-target effects on PPARγ and soluble epoxide hydrolase (sEH) .
评价 Zafirlukast is an oral leukotriene receptor antagonist (LTRA), with selectivity for cysteinyl leukotriene receptor 1 (CysLT1 receptor).

产品问答

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参考文献

1. Schierle S, Flauaus C, Heitel P, Willems S, Schmidt J, Kaiser A, Weizel L, Goebel T, Kahnt AS, Geisslinger G et al..  (2018)  Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology..  J Med Chem,  61  (13):  (5758-5764).  [PMID:29878767]

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品牌简介

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