Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.
| Molecular Weight | 601.68 |
| Formula | C36H37F2NO5 |
| CAS Number | 1232861-58-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 250 mg/mL (ultrasonic) |
| 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.
| 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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