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Cilomilast

Cilomilast Struktur
153259-65-5
CAS-Nr.
153259-65-5
Englisch Name:
Cilomilast
Synonyma:
Ariflo;CS-515;ArifloR;SB 207499;Clomilast;Cilomelast;CILOMILAST;Cilomilast-d5;Cilomilast USP/EP/BP;Sb207499 Cilomilast
CBNumber:
CB4841029
Summenformel:
C20H25NO4
Molgewicht:
343.42
MOL-Datei:
153259-65-5.mol

Cilomilast Eigenschaften

Schmelzpunkt:
157°C
Siedepunkt:
549.1±50.0 °C(Predicted)
Dichte
1.21±0.1 g/cm3(Predicted)
storage temp. 
-20°C
L?slichkeit
DMSO: soluble15mg/mL, clear
Aggregatzustand
powder
pka
4.45±0.25(Predicted)
Farbe
white to beige
InChIKey
CFBUZOUXXHZCFB-OYOVHJISSA-N

Sicherheit

WGK Germany  3

Cilomilast Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften

Cilomilast is White Solid

Verwenden

Cilomilast is a selective phosphodiesterase 4 (PDE4) inhibitor and can be used in treatment of chronic obstructive pulmonary disease.

Mechanism of action

Cilomilast 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.

Pharmakokinetik

Cilomilast 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.

Cilomilast Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Cilomilast Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 108)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hubei xin bonus chemical co. LTD
86-13657291602
linda@hubeijusheng.com CHINA 22963 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49374 58
career henan chemical co
+86-0371-86658258 +8613203830695
factory@coreychem.com China 29811 58
Shaanxi Dideu Medichem Co. Ltd
+86-29-87569262 +86-15319487004
1015@dideu.com China 3209 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32161 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226
sales@hzclap.com CHINA 6312 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 22784 58
Baoji Guokang Bio-Technology Co., Ltd.
0917-3909592 13892490616
gksales1@gk-bio.com China 9312 58
Hefei Hirisun Pharmatech Co., Ltd
+8615056975894
shawn@hirisunpharm.com CHINA 9911 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471
sales@sarms4muscle.com China 10473 58

153259-65-5()Verwandte Suche:


  • 4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)cyclohexane-1-carboxylic acid
  • Cilomilast, SB 207499, Ariflo
  • "(cilomilast) 4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexane-1-carboxylic acid"
  • CILOMILAST
  • Clomilast
  • Cilomelast
  • Ariflo
  • cis-4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-4-cyanocyclohexane-1-carboxylic Acid
  • cis-4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-cyclohexanecarboxylic Acid
  • SB 207499
  • ArifloR
  • Sb207499 Cilomilast
  • CiloMilast(SB-207499)
  • 4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
  • cis-4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexane-1-carboxylic acid
  • (1r,4r)-4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
  • CS-515
  • SB 207499 - Cilomilast | Ariflo
  • 4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)-1-cyclohexanecarboxylic acid
  • Cyclohexanecarboxylic acid, 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-, cis-
  • Cilomilast USP/EP/BP
  • Cilomilast-d5
  • 153259-65-5
  • Inhibitor
  • Aromatics
  • Inhibitors
  • 13C & 2H Sugars
  • Carbohydrates & Derivatives
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
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