Roflumilast
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Roflumilast 속성
- 녹는점
- 158°C
- 끓는 점
- 430.6±45.0 °C(Predicted)
- 밀도
- 1.471±0.06 g/cm3(Predicted)
- 저장 조건
- -20°C
- 용해도
- DMSO: 용해성20mg/mL, 투명
- 산도 계수 (pKa)
- 9.89±0.70(Predicted)
- 물리적 상태
- 가루
- 색상
- 흰색에서 베이지색
- Merck
- 14,8249
- 안정성
- 제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
- InChI
- InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24)
- InChIKey
- MNDBXUUTURYVHR-UHFFFAOYSA-N
- SMILES
- C(NC1C(Cl)=CN=CC=1Cl)(=O)C1=CC=C(OC(F)F)C(OCC2CC2)=C1
- CAS 데이터베이스
- 162401-32-3(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
Roflumilast C화학적 특성, 용도, 생산
개요
Roflumilast is a selective, orally active PDE4 inhibitor thatwas approved in Germany in July 2010 as an add-on to bronchodilator treatment for maintenance therapy of severe chronic obstructive pulmonary disorder (COPD) associated with chronic bronchitis in adult patients with a history of frequent exacerbations .Roflumilast and its primary metabolite roflumilast N-oxide are potent and competitive inhibitors of PDE4 and are equipotent against PDE4A, B, andD but inactive against PDE4C and the other ten members of the PDE family (PDEs 1–3, 5–11). Despite its inhibition of PDE4D (IC50=0.80 nM, N-oxide IC50=2.0 nM), roflumilast shows the lowest incidence of nausea (3–5%) among the PDE4 inhibitors investigated in clinical trials.Anti-inflammatory effects of roflumilast have been demonstrated in preclinical cellular and animal models. Roflumilast is synthesized in four steps from 3-(cyclopropylmethoxy)-4-hydroxybenzaldehyde. The difluoromethyl ether is introduced by alkylation of the free phenolic group with chlorodifluoromethane and base. The aldehyde moiety is oxidized to the benzoic acid, which is then converted to an acid chloride and coupled with 3,5-dichloro-4-aminopyridine. Roflumilast is rapidly absorbed and metabolized to its active metabolite, roflumilast N-oxide. Metabolism is mediated by CYP3A4 and CYP1A2.
화학적 성질
Crystallin Solid용도
Roflumilast (Daxas) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.정의
ChEBI: A benzamide obtained by formal condensation of the carboxy group of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid with the amino group of 3,5-dichloropyridin-4-amine. Used for treatment of bronchial asthma and chronic obstructive pulmonary diseaseMechanism of action
Roflumilast is the more potent of the two drugs, and along with its active metabolite, roflumilast-N-oxide, it is nonselective in its inhibitory action on PDE4B and PDE4D. The PDE4B appears to be the most closely linked to anti-inflammatory effects, whereas the PDE4D receptor subtype is thought to be linked to nausea, possibly through a central effect. Roflumilast exhibits 80% oral bioavailability and has an elimination half-life of 10 hours, whereas the N-oxide has an elimination half-life of 20 hours and has shown no drug interactions. Clinical trials in patients with asthma or COPD are quite promising.Pharmacokinetics
Roflumilast is well absorbed on oral administration and has a half-life of 10 hours. Roflumilast is metabolized in the liver to its N-oxide derivative, which also is a PDE4 inhibitor, and it has a plasma half-life of 20 hours.Clinical Use
Roflumilast is currently undergoing clinical trials in Europe for use in the treatment of both asthma and COPD.부작용
Common side effects of Roflumilast include: diarrhoea, nausea, dizziness, headache, back pain, muscle cramps, loss of appetite and weight loss. Severe can lead to persistent diarrhoea, acute pancreatitis, significant weight loss and psychiatric symptoms (such as anxiety, depression, insomnia and suicidal tendencies). In addition, the incidence of prostate, lung and colorectal cancer is significantly higher.Roflumilast 준비 용품 및 원자재
원자재
준비 용품
Roflumilast 공급 업체
글로벌( 494)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hefei TianRui Pharmaceutical Chemical Co., Ltd. | +86-0551-68665055 +86-+86-18616906106 |
sales@trywchem.com | China | 129 | 58 |
Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 |
sales@hbmojin.com | China | 12446 | 58 |
Hebei Chuanghai Biotechnology Co,.LTD | +86-13131129325 |
sales1@chuanghaibio.com | China | 5866 | 58 |
Henan Bao Enluo International TradeCo.,LTD | +86-17331933971 +86-17331933971 |
deasea125996@gmail.com | China | 2503 | 58 |
Anhui Ruihan Technology Co., Ltd | +8617756083858 |
daisy@anhuiruihan.com | China | 994 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21667 | 55 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9355 | 55 |
Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 |
product@chemlin.com.cn | CHINA | 3012 | 60 |
Shanghai Yingrui Biopharma Co., Ltd. | +86-21-33585366 - 03@ |
sales03@shyrchem.com | CHINA | 738 | 60 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32836 | 60 |
Roflumilast 관련 검색:
P-아미노벤즈아마이드 벤즈아마이드 클로피랄리드 2-클로로-5-클로로메틸피리딘 폴리테트라플루오르에틸렌
Montelukast
Montelukast sodium
Chlorantraniliprole
Fleroxacin
Ezetimibe
4-(DIFLUOROMETHOXY)-3-(CYCLOPROPYLMETHOXY)-BENZALDEHYDE
3-Cyclopropylmethoxy-4-difluoromethoxy-benzoic acid
benzaMide, N-(3,5-dichloro-4-pyridinyl)-4-(difluoroMethoxy)-3-hydroxy-
4-Amino-3,5-dichloropyridine
4-(Cyclopropylmethoxy)-3-(difluoromethoxy) Roflumilast
RofluMilast related substance
Roflumilast
RofluMilast N-Oxide