Zafirlukast (扎鲁司特) 是口服活性的白三烯受体拮抗剂(LTRA)。
Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Silverman, R.A., Nowak, R.M., Korenblat, P.E., et al. Zafirlukast treatment for acute asthma. Evaluation in a randomized, double-blind, multicenter trail. Chest 126 1480-1489 (2004).
[2] Heise, C.E., O'Dowd, B.F., Figueroa, D.J., et al. Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem 275 30531-30536 (2000).
[3] Johannes Kornhuber et. al. Identification of novel functional inhibitors of acid sphingomyelinase. PLoS ONE, 6(8), e23852 (2011)
[4] Peters-Golden, M., Henderson, W.R. The role of leukotrienes in allergic rhinitis. Ann Allergy Asthma Immunol 94 609-618 (2005).
[5] Muzaffar Iqbal et. al. Rapid determination of canagliflozin in rat plasma by UHPLC-MS/MS using negative ionization mode to avoid adduct-ions formation. Talanta, 132, 29-36 (2015).
分子式 C31H33N3O6S |
分子量 575.68 |
CAS号 107753-78-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 110 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01283061 | Healthy | Drug: Zafirlukast | Dr. Reddy's Laboratories Limited | Phase 1 | 2017-12-07 | 2011-01-25 |
NCT02950480 | Breast Cancer | Drug: zafirlukast|Other: Standard of Care (no intervention) | University of California, San Francisco | Phase 2 | 2017-11-16 | 2016-10-27 |
NCT01125748 | Allergic Asthma | Drug: Omalizumab|Drug: Placebo|Drug: Asthma therapies | Genentech, Inc. | Phase 4 | 2017-05-10 | 2014-10-08 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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