Roflumilast (trade names Daxas, Daliresp) is a novel and selective, long-acting inhibitor of phosphodiesterase 4 (PDE-4) with IC50 of 0.8 nM. It has antiinflammatory effects for the treatment of inflammatory conditions of the lungs such as asthma, and chronic obstructive pulmonary disease (COPD). Roflumilast is a first-in-class antiinflammatory treatment for severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis and a history of frequent exacerbations. Because roflumilast (a phosphodiesterase-4 inhibitor) has a different mode of action to bronchodilators and inhaled corticosteroids, it may provide additional benefits when added to treatments in frequent exacerbators. Roflumilast lowered glucose levels in patients with newly diagnosed DM2 without COPD, suggesting positive effects on glucose homoeostasis.
| Molecular Weight | 403.21 |
| Formula | C17H14Cl2F2N2O3 |
| CAS Number | 162401-32-3 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PDE Products |
|---|
| ME-3183
ME-3183 is an oral selective PDE4 inhibitor with anti-inflammatory activity for studies related to plaque psoriasis. |
| ART-648
ART-648 is a PDE4 inhibitor that may be used in studies related to non-alcoholic steatohepatitis. |
| (E/Z)-HA155
(E/Z)-HA155 is a potent Autotaxin (ATX) type I inhibitor for studies related to cancer, fibrous disorders, inflammation, pain and angiogenesis. |
| Autotaxin-IN-3
Autotaxin-IN-3 is an Autotaxin(ATX) inhibitor with an IC50 value of 2.4 nM. |
| HA155
HA155 is a potent and selective ATX inhibitor with an IC50 value of 5.7 nM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
