Zafirlukast is in a class of medications called leukotriene receptor antagonists (LTRAs). It works by blocking the action of certain natural substances that cause swelling and tightening of the airways. In a study, pranlukast or zafirlukast significantly inhibited 10 μM LTD4-evoked 35SO4 output in a concentration- dependent fashion, with maximal inhibitions of 83% at 10 μM pranlukast and 78% at 10 μM zafirlukast, and IC50 values of 0.3 μM for pranlukast and 0.6 μM for zafirlukast. Both pranlukast and zafirlukast showed moderate inhibition of CYP2C9-catalysed tolbutamide 4-methylhydroxylation, competitively inhibiting tolbutamide 4-methylhydroxylation with estimated mean Ki values of 3.82 ± 0.50 and 5.86 ± 0.08 μM, respectively.Zafirlukast inhibited the hydroxylation of tolbutamide (CYP2C9; mean IC50=7.0 µM).
| Molecular Weight | 575.68 |
| Formula | C31H33N3O6S |
| CAS Number | 107753-78-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Qiang Song, et al. Zafirlukast prevented ox-LDL-induced formation of foam cells
[2] Amareen Dhaliwal, et al. Zafirlukast
[3] No authors listed. Zafirlukast
| Related Leukotriene Receptor Products |
|---|
| Piriprost potassium
Piriprost (U-60,257B) potassium is an inhibitor of leukotriene synthesis. |
| LTB4 antagonist 3
LTB4 antagonist 3 is a leukotriene B4 (LTB4) antagonist with an IC50 value of 477 nM. |
| LTB4 antagonist 1
LTB4 antagonist 1, a carboxamide-acid compound, is a potent Leukotriene B4 (LTB4) antagonist with an IC50 of 288 nM. |
| LTB4 antagonist 2
LTB4 antagonist 2, a carboxamide-acid compound, is an antagonist of leukotriene B4 (LTB4) with potentially anti-inflammatory activity. |
| Tipelukast
Tipelukast is an orally bioavailable leukotriene receptor antagonist with anti-inflammatory activity for studies related to asthma and non-alcoholic steatohepatitis (NASH). |
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