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Roflumilast

Catalog No.
A4319
PDE-4 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$66.00
In stock
5mg
$55.00
In stock
10mg
$77.00
In stock
25mg
$143.00
In stock
50mg
$253.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Roflumilast is an orally active, selective inhibitor of phophodiesterase-4 (PDE-4) with IC50 value of 0.11nM [1].

Roflumilast is developed for the treatment of the inflammatory component of COPD since PDE-4 is found mainly in inflammatory cells. In vitro studies show that roflumilast inhibits the production of inflammatory mediators in a variety of human immune cells, suggesting a role for reducing COPD-related inflammation. Roflumilast has a rapid absorption with a bioavailability of ~ 80% and the half-life is approximately 17h after repeated dosing of 500 mcg OD. Pharmacokinetic studies show no significant interactions with the drugs used by COPD patients. Roflumilast is also found to decrease glucose levels in patients with newly diagnosed type-2 diabetes since diabetes is an important comorbidity associated with COPD [2].

References:
[1] Z Huang, JA Mancini. Phosphodiesterase 4 Inhibitors for the Treatment of Asthma and COPD. Current Medicinal Chemistry, 2006.
[2] Tashkin DP. Roflumilast : the new orally active, selective phophodiesterase-4 inhibitor, for the treatment of COPD. Expert Opin Pharmacother. 2014 Jan;15(1):85-96.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt403.21
Cas No.162401-32-3
FormulaC17H14Cl2F2N2O3
Solubilityinsoluble in H2O; ≥20.2 mg/mL in DMSO; ≥9.94 mg/mL in EtOH with ultrasonic
Chemical Name3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
SDFDownload SDF
Canonical SMILESC1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control