ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > Metabolism > PDE inhibitors > Cilomilast
Cilomilast Chemical Properties
- Melting point:157°C
- Boiling point:549.1±50.0 °C(Predicted)
- Density 1.21±0.1 g/cm3(Predicted)
- storage temp. -20°C
- solubility DMSO: soluble15mg/mL, clear
- form powder
- color white to beige
- WGK Germany 3
Cilomilast Usage And Synthesis
- Chemical PropertiesCilomilast is White Solid
- UsesCilomilast is a selective phosphodiesterase 4 (PDE4) inhibitor and can be used in treatment of chronic obstructive pulmonary disease.
- Mechanism of actionCilomilast contains the dialkoxyphenyl ring characteristic of selective PDE4 inhibitors. The ether oxygens hydrogen bond to a glutamine in the binding pocket, and the cyclopentyl ring adds additional hydrophobic interactions. The oxygen atoms of the carboxyl group form hydrogen bonds with water that is coordinated with Mg2+ located in the distal end of the binding pocket. Orally administered cilomilast is 96% bioavailable. Food does not interfere with the overall absorption; however, food does slow down the rate. Cilomilast is 99% bound to albumin in the plasma and is metabolized in the liver by CYP2C8. The metabolism is extensive and results in oxidation, carboxyl group glucuronidation, and dealkylation of the cyclopentyl group, followed by glucuronidation or sulfation.
- PharmacokineticsCilomilast is rapidly absorbed following oral administration (96% bioavailability), has an elimination half-life of 7 hours, and is extensively metabolized, but not by cytochrom P450 enzymes. The drug shows considerably more selectivity than roflumilast toward PDE4D, and this might account for the common side effects of nausea and emesis. Studies regarding the benefits of cilomilast versus placebo in the treatment of asthma have not been very encouraging, but significant improvement was seen in clinical trials of cilomilast in the treatment of COPD. The side effects of diarrhea and nausea have been considerably higher with cilomilast versus placebo, but these effects generally are tolerable and self limiting.
- 2-PHENYL-5-(TRIFLUOROMETHYL)-OXAZOLE-4-CARBOXYLIC ACID, ETHYL ESTER ETHYL 5-METHYLOXAZOLE-4-CARBOXYLATE Ethyl 5-(4-chlorophenyl)oxazole-4-carboxylate 2-PHENYL-5-(TRIFLUOROMETHYL)-OXAZOLE-4-CARBOXYLICACID 5-PHENYL-OXAZOLE-4-CARBOXYLIC ACID ETHYL ESTER Cilomilast Montelukast Phenyl salicylate Montelukast sodium (Trifluoromethoxy)benzene Zafirlukast Cyano Methoxy 4-Methoxyphenol PHENYL VALERATE CARBOXYLIC ACID Tranilast 4-Methoxybenzyl cyanide
- Company Name:DKMbiochem.Co. Ltd Gold
- Tel:15901859516 15901864159
- Company Name:Chembest Research Laboratories Limited
- Company Name:LGM Pharma
- Company Name:Chemsky（shanghai）International Co.,Ltd.
- Company Name:BOC Sciences