Cilomilast
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Cilomilast 속성
- 녹는점
- 157°C
- 끓는 점
- 549.1±50.0 °C(Predicted)
- 밀도
- 1.21±0.1 g/cm3(Predicted)
- 저장 조건
- -20°C
- 용해도
- DMSO: 용해성15mg/mL, 투명
- 물리적 상태
- 가루
- 산도 계수 (pKa)
- 4.45±0.25(Predicted)
- 색상
- 흰색에서 베이지색
- InChIKey
- CFBUZOUXXHZCFB-OYOVHJISSA-N
안전
| WGK 독일 | 3 |
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Cilomilast C화학적 특성, 용도, 생산
화학적 성질
Cilomilast is White Solid용도
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.Pharmacokinetics
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 준비 용품 및 원자재
원자재
1-Cyclohexene-1-carboxylic acid, 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-, methyl ester
Cyclohexanecarboxylic acid, 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-, methyl ester, cis-
준비 용품
Cilomilast 공급 업체
글로벌( 104)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| Hubei xin bonus chemical co. LTD | 86-13657291602 |
linda@hubeijusheng.com | CHINA | 22968 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 47465 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; |
factory@coreychem.com | China | 29826 | 58 |
| Shaanxi Dideu Medichem Co. Ltd | +86-29-87569265 +86-18612256290 |
1056@dideu.com | China | 3632 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 |
sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 |
1026@dideu.com | China | 29271 | 58 |
| Baoji Guokang Bio-Technology Co., Ltd. | 0917-3909592 13892490616 |
gksales1@gk-bio.com | China | 9339 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 |
shawn@hirisunpharm.com | CHINA | 9923 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 |
sales@sarms4muscle.com | China | 10523 | 58 |
| Nextpeptide Inc | +86-0571-81612335 +8613336028439 |
sales@nextpeptide.com | China | 19915 | 58 |