Roflumilast manufacturers and suppliers in india

Roflumilast

Properties

Melting point:: 158°C

Boiling point:: 430.6±45.0 °C(Predicted)

Density: 1.471±0.06 g/cm3(Predicted)

storage temp.: -20°C

solubility: DMSO: soluble20mg/mL, clear

pka: 9.89±0.70(Predicted)

form: powder

color: white to beige

Merck: 14,8249

Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

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

Safety Information

Symbol(GHS): GHS07

Signal word: Warning

Hazard statements: H315-H319-H335

Precautionary statements: P261-P264-P271-P280-P302+P352-P305+P351+P338

Hazard Codes: Xi

Risk Statements: 36/37/38

Safety Statements: 26

WGK Germany: 3

RTECS: CV3325600

HS Code: 2933.39.4100

Use

Roflumilast is taken orally and is metabolized by cytochrome oxidase P45(CYP)3A4 and CYP1A2 enzyme into N-oxide. Roflumilast N-oxides 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 nmolL-1, and its serum protein binding rate is about 97%. Smoking has little impact on roflumilasts 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.