ChemicalBook > Product Catalog >API >Respiratory Drugs >Asthma drugs >Roflumilast

Roflumilast

Roflumilast Suppliers list
Company Name: Henan DaKen Chemical CO.,LTD.
Tel: +86-371-55531817
Email: info@dakenchem.com
Products Intro: Product Name:Roflumilast
CAS:162401-32-3
Purity:99% Package:100g,500g,1KG,10KG,100KG
Company Name: Shanghai Bojing Chemical Co.,Ltd.
Tel: +86-21-37122233
Email: Candy@bj-chem.com
Products Intro: Product Name:Roflumilast
CAS:162401-32-3
Purity:99% Package:1Kg;25kg/ Drum or as customer request
Company Name: Henan Tianfu Chemical Co.,Ltd.
Tel: 0371-55170693
Email: info@tianfuchem.com
Products Intro: CAS:162401-32-3
Purity:99% Package:500G;1KG;5KG;25KG
Company Name: Hangzhou FandaChem Co.,Ltd.
Tel: 0086 158 5814 5714 (Mobile; WhatsApp; Telegram)
Email: fandachem@gmail.com
Products Intro: Product Name:Roflumilast
CAS:162401-32-3
Purity:as in COA Package:as customers' requirements
Company Name: Nanjing ChemLin Chemical Industry Co., Ltd.
Tel: 025-83697070;product@chemlin.com.cn
Email: product@chemlin.com.cn
Products Intro: CAS:162401-32-3
Purity:98% Package:g-Kg

Lastest Price from Roflumilast manufacturers

  • Roflumilast
  • US $1.00 / kg
  • 2019-07-06
  • CAS:162401-32-3
  • Min. Order: 1kg
  • Purity: 99%
  • Supply Ability: Customized
Roflumilast Basic information
Indications and Usage Mechanisms of Action Pharmacokinetics
Product Name:Roflumilast
Synonyms:Roflumilast - Daxas | BY 217 | BYK 20869 | B 9302-107;3-CyclopropylMethoxy-N-(3,5-dichloro-pyridin-4-yl)-4-isopropoxy-benzaMide;APTA 2217;3-Cyclopropylmethoxy-4-difluoromethoxy-N-[3,5-dichloropyrid-4-yl]-benzamide;162401-32-3;Roflumilast intermediates;ROFLUMILAST;3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide
CAS:162401-32-3
MF:C17H14Cl2F2N2O3
MW:403.2074664
EINECS:685-382-2
Product Categories:Roflumilast;Daxas;All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;API;Pharmaceuticals;APIs
Mol File:162401-32-3.mol
Roflumilast Structure
Roflumilast Chemical Properties
Melting point 158°C
Boiling point 430.6±45.0 °C(Predicted)
density 1.471±0.06 g/cm3(Predicted)
storage temp. Refrigerator
solubility DMSO: soluble20mg/mL, clear
form powder
pka9.89±0.70(Predicted)
color white to beige
Merck 14,8249
CAS DataBase Reference162401-32-3(CAS DataBase Reference)
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26
WGK Germany 3
RTECS CV3325600
MSDS Information
Roflumilast Usage And Synthesis
Indications and UsageRoflumilast is a selective oral phosphodiesterase-4 (PDE-4) inhibitor and a benzamide compound. It was developed by the German company Altana in 1993 and is the only oral PDE-4 inhibitor used to treat respiratory tract diseases approved for sale. Roflumilast is the first drug of its kind to target severe chronic obstructive pulmonary disease (COPD), and it is also the first oral anti-inflammation drug specifically developed for COPD patients. Its unique properties can help regulate COPD: when used in combination with bronchodilators to treat extremely severe COPD patients, roflumilast can has the advantage of further reducing symptoms and deterioration rate, thus making it the first drug that targets patients with recurring deteriorating phenotype-specific COPD and severe air flow obstruction related to chronic coughing and excess phlegm. Besides being a treatment for severe COPD, roflumilast can also be used to prevent and treat livestock respiratory tract diseases, excess mucosa bronchitis cough, asthmatic bronchitis, and acute bronchitis and air sacculitis accompanied by abnormal respiratory tract secretion.
Mechanisms of ActionRoflumilast selectively inhibits PDE4 to prevent the signal transduction for inflammatory reactions, and it then inhibits the damage on lung tissue caused by respiratory tract diseases such as COPD and asthma.
PharmacokineticsRoflumilast is taken orally and is metabolized by cytochrome oxidase P45(CYP)3A4 and CYP1A2 enzyme into N-oxide. Roflumilast N-oxide’s activity is only 2-3 times weaker than that of roflumilast, and it also has relatively high PDE-4 selectivity. 90% of PDE-4 inhibition in the body is achieved by roflumilast N-oxide, while the other 10% is achieved by the original drug. A daily 500ng oral dose of roflumilast for a healthy person will produce a free blood concentration of roflumilast N-oxide in 24 hours of about 1-2 nmol•L-1, and its serum protein binding rate is about 97%. Smoking has little impact on roflumilast’s pharmacokinetics. Roflumilast mostly affects inflammation cells related to asthma, including eosinophils, neutrophils, and mast cells. This drug can specifically affect a certain enzyme that participates in smooth muscle contraction, it can prevent cAMP decomposition, thus preventing the signal transduction for inflammatory reactions, and it is anti-inflammatory, giving it relatively good curative effects in clinically treating asthma and COPD. Roflumilast can also significantly extend the deterioration of respiratory symptoms while also dramatically increasing patients’ quality of life.
DescriptionRoflumilast 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.
Chemical PropertiesCrystallin Solid
OriginatorBYK Gulden Lomberg Chemische Fabrik GmbH (Germany)
UsesSelective phosphodiesterase 4(PDE4) inhibitor. Antiasthmatic; in treatment of chronic obstructive pulmonary disease
UsesRoflumilast (Daxas) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.
Usesophthalmic solution
UsesA selective inhibitor of phosphodiesterase 4
DefinitionChEBI: 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 disease
Brand nameDaxas
Roflumilast Preparation Products And Raw materials
Tag:Roflumilast(162401-32-3) Related Product Information
Ezetimibe p-Aminobenzamide Benzamide CHLOANTRANILIPROLE Clopyralid Fleroxacin 2-Chloro-5-chloromethylpyridine CHEMBRDG-BB 5563263 N-[4-(DIFLUOROMETHOXY)BENZYL]-N-METHYLAMINE 4-Difluoromethoxy-3-hydroxybenzaldehyde 4-(DIFLUOROMETHOXY)-3-(CYCLOPROPYLMETHOXY)-BENZALDEHYDE 4-(DIFLUOROMETHOXY)BENZYLAMINE 3-BUTOXY-4-METHOXYBENZAMIDE 4-DIFLUOROMETHOXY-3-METHOXY-BENZALDEHYDE N1-(4-PYRIDYL)BENZAMIDE 3-ISOBUTOXYBENZALDEHYDE BENZYL-PYRIDIN-4-YL-AMINE DIHYDROCHLORIDE (3,5-DICHLORO-PYRIDIN-4-YL)METHYLAMINE