3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
Roflumilast, B 9302-107, BYK 20869
API & Intermediates
KAPI2F03
162401-32-3
MFCD00938270
449193
9802592
image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide
C17H14Cl2F2N2O3
403.21
≥98%(HPLC)
Colorless to White Solid
157-158°C
500mg,1g,5g,10g,50g,100g,500g and 1kg
-20°C Freezer
Roflumilast(also known as B 9302-107, BYK 20869) is a highly potent, orally active, and selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 0.8 nM. It has anti-inflammatory properties and is used clinically for the treatment of the chronic obstructive pulmonary disease (COPD).
Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. [1]
The phosphodiesterase 4 inhibitor roflumilast is effective in the treatment of allergic rhinitis. [2]
Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease. [3]
PDE4 inhibitors: Current status. [4]
The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. [5]
Sensitive quantification of roflumilast and roflumilast N-oxide in human plasma by LC-MS/MS employing parallel chromatography and electrospray ionisation. [6]
Isolation, synthesis and structure confirmation of the impurity in crude roflumilast product. [7]
References:
[1] A.Hatzelmann, et al, J. Pharmacol. Exp. Ther., 2001, 297(1), pp 267-279.
[2] B.M.W.Schmidt, et al, J. Allergy Clin. Immunol., 2001, 108(4), pp 530-536.
[3] B.J.Lipworth, et al, Lancet, 2005, 365(9454), pp 167-175.
[4] D.Spina, Br. J. Pharmacol., 2008, 155(3), pp 308-315.
[5] A.Hatzelmann, et al, Pulm. Pharmacol. Ther., 2010, 23(4), pp 235-256.
[6] H.G.Knebel, et al, J. Chromatogr. B Analyt. Technol. Biomed. Life Sci., 2012, 82(91), pp 893-894.
[7] Y.Lin, et al, Res. Chem. Intermed., 2013, 39(7), pp 3111-3115.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Warning
H315,H319,H335
P261,P305+P351+P338

NONH for all modes of transport
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