Zafirlukast
Cat.No:IZ0230 Solarbio
CAS:107753-78-6
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Solid
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ZafirlukastCAS:107753-78-6
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Solid
Qty:
Size:
CAS | 107753-78-6 |
Name | Zafirlukast |
Molecular Formula | C31H33N3O6S |
Molecular Weight | 575.68 |
Solubility | Soluble in DMSO ≥10mg/mL |
Purity | ≥98% |
Appearance | Solid |
Storage | Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD00864775 |
SMILES | O=C(OC1CCCC1)NC2=CC3=C(N(C)C=C3CC4=CC=C(C(NS(=O)(C5=CC=CC=C5C)=O)=O)C=C4OC)C=C2 |
InChIKey | YEEZWCHGZNKEEK-UHFFFAOYSA-N |
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) |
PubChem CID | 5717 |
Target Point | Leukotriene Receptor |
Passage | GPCR & G Protein |
Background | Zafirlukast is a potent leukotriene D4 (LTD4) receptor antagonist |
Biological Activity | Zafirlukast 是一种有效的具有口服活性的白三烯 D4 (LTD4) 受体拮抗剂[1-2] |
In Vivo | 扎鲁司特是肽基白三烯拮抗剂和LTD4的抑制剂。暴露13周后,Zafirlukast(270和540 mg / kg),高剂量Zileuton(1200 mg / kg)和含有600 mg / kg Zileuton的组合的剂量水平显著降低了肺肿瘤的产量与Zafirlukast或MK-866。含有Zileuton和Zafirlukast的组合预防肺肿瘤的功效与单独给予抑制剂的功效没有显著差异。虽然在组合中单独给予剂量水平时,Zileuton或MK-886都不能预防肺部肿瘤;含有它们的组合确实可以显著预防肿瘤。相反,含有扎鲁司特和MK-886的组合不会降低肿瘤的产量,而单独使用扎鲁司特确实会显著降低肿瘤的产量[2]。 |
Animal Experiment | 小鼠[2]使用雌性A / J小鼠(5-6周龄)。当小鼠7-8周龄时,给予它们两次腹膜内注射氨基甲酸乙酯的第一次,每次注射16mg / kg,间隔7天。在第二剂乙烯基氨基甲酸酯后两周,小鼠在其饮食中接受白三烯抑制剂。在饮食中以指定的mg / kg浓度提供扎鲁司特(270或540mg / kg),齐留通(600或1200mg / kg)和MK-886(30mg / kg)。在暴露于白三烯抑制剂的前6周每周称重小鼠。之后,每2-4周对它们称重直至处死。在暴露于药物13和43周后,通过二氧化碳窒息处死小鼠。收获肺,在福尔马林中固定过夜,转移至70%酒精,并在嵌入石蜡进行组织学评估之前评估肿瘤[1]。 |
Data Literature Source | [1]. Finnerty JP,et al. Role of leukotrienes in exercise-induced asthma. Inhibitory effect of ICI 204219,a potent leukotriene D4 receptor antagonist. Am Rev Respir Dis. 1992 Apr;145(4 Pt 1):746-9. [2]. Gunning WT,et al. Chemoprevention by lipoxygenase and leukotriene pathway inhibitors of vinyl carbamate-induced lung tumors in mice. Cancer Res. 2002 Aug 1;62(15):4199-201 |
Unit | Bottle |
Specification | 10mg 10mM*1mL in DMSO 25mg 50mg 100mg |
Zafirlukast 是一种有效的白三烯 D4 (LTD4) 受体拮抗剂
Remark:These protocols are for reference only. Solarbio does not independently validate these methods.
Note:
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