[CAS NO. 125961-82-2] Tipelukast
PRODUCTS SPECIFICATIONS [125961-82-2]
DESCRIPTION [125961-82-2]
Overview
| MDL | MFCD00886138 |
|---|---|
| Molecular Weight | 530.67 |
| Molecular Formula | C29H38O7S |
| SMILES | CC(C1=C(O)C(CCC)=C(SCCCOC2=C(CCC)C(OCCCC(O)=O)=C(C(C)=O)C=C2)C=C1)=O |
Summary
Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
IC50 & Target
|
LTD 4 6.41 (pA2, In guinea-pigs) |
LTE 4 6.45 (pA2, In guinea-pigs) |
In Vitro
Tipelukast inhibits the binding of [ 3 H] LTD4 to the LTD4 receptors on pul-monary cell membrane of guinea-pigs (IC 50 = 2.3 μmol) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fiftheen min after an aerosolized antigen challenge, and UNDW inhaled 5 min later into the guinea pigs, Tipelukast significantly alters the UNDW-induced bronchoconstriction [1] . Tipelukast (1 and 5 mg/kg) administered intravenously 15 min after antigen challenge reduces the propranolol-induced bronchoconstriction (PIB) in a dose-dependent manner in guinea-pigs [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02503657 | MediciNova |
Idiopathic Pulmonary Fibrosis|IPF
|
March 9, 2016 | Phase 2 |
| NCT02681055 | MediciNova |
Non-alcoholic Steatohepatitis|Hypertriglyceridemia|Non-alcoholic Fatty Liver Disease|Hypercholesterolemia
|
March 2016 | Phase 2 |
| NCT00295854 | MediciNova |
Interstitial Cystitis
|
May 2005 | Phase 2 |
| NCT05464784 | MediciNova |
Diabetes Mellitus, Type 2|Hypertriglyceridemia|Non-Alcoholic Fatty Liver Disease
|
August 22, 2022 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Ethanol : 1 mg/mL ( 1.88 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8844 mL | 9.4221 mL | 18.8441 mL |
| 5 mM | --- | --- | --- |
| 10 mM | --- | --- | --- |
References
- [1] Fujimura M, et al. No involvement of lipid mediators in a guinea pig model of ultrasonically nebulized distilled water-induced bronchoconstriction. Prostaglandins Other Lipid Mediat. 2000 Jan;60(1-3):49-58.
- [2] Fujimura M, et al. Role of leukotrienes in post-allergic propranolol-induced bronchoconstriction in guinea-pigs. Clin Exp Allergy. 1997 Oct;27(10):1219-26.