| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| Z409117-1ml |
1ml |
现货  |
|
| 英文别名 | N-[3-[[2-methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]-carbamic acid cyclopentyl ester |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Zafirlukast (ICI-204219) |
| 生化机理 | 扎非司特（ICI-204219）是一种口服白三烯受体拮抗剂（LTRA），用于预防哮喘症状。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 胱氨酰白三烯受体 1 拮抗剂 |
| 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
Information Zafirlukast (ICI-204219) Zafirlukast (ICI-204219) is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms. Zafirlukast is similar to 3-methylindole because it contains an N-methylindole moiety that has a 3-alkyl substituent on the indole ring. Zafirlukast readily forms (10% conversion in 60 min) a GSH adduct with molecular mass of 880 Da upon incubation with horseradish peroxidase. Zafirlukast produces time-, concentration-, and NADP(H)-dependent inactivation of CYP3A4. Zafirlukast is shown to inhibit CYP3A enzyme activity in vitro (nonpreincubation inhibition) with a Ki of 2 μM in one report, but higher values have been published, and our KI for the inactivation process is 13.4 μM. Zafirlukast has high plasma protein binding (>99%), which would lower the free-drug concentration. Zafirlukast undergoes two successive one-electron oxidations to afford a highly electrophilic α,β-unsaturated iminium species, which reacts spontaneously with GSH to yield the observed adduct. In vivo Zafirlukast is a potent and selective cysteinyl leukotriene receptor antagonist which is used mainly in the prophylaxis of bronchial asthma. Zafirlukast in a dose of 80 mg/kg orally produces a significant decrease in tissue malondialdehyde, myeloperoxidase, and an increase in both reduced glutathione and catalase levels, while there is no significant changes with the rectal route. cell lines：PBMC effector cells Concentrations： Incubation Time： Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=CC(=CC=C1CC2=C[N](C)C3=C2C=C(NC(=O)OC4CCCC4)C=C3)C(=O)N[S](=O)(=O)C5=CC=CC=C5C |
| 分子量 | 575.68 |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| NMR Spectrum 1H | Conforms to structure |
| Record the entire process by video | Conform |
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