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Product Details

Roflumilast | PDE4 inhibitor

Roflumilast (162401-32-3) is a potent and selective phosphodiesterase (PDE4) inhibitor, IC50=0.7, 0.9, 0.7, 0.2 nM for PDE4A1, PDE4A4, PDE4B1 and PDE4B2 respectively.1 Clinically useful agent for treatment of COPD.2 Improves sensory gating in humans3 and improves memory in rodent models4. Mimics calorie restriction effects via activation of AMPK/SIRT1 and protects against diabetic nephropathy.5 Reduces weight gain by increasing energy expenditure and improves glucose metabolism in mice.6

References/Citations

1) Hatzelmann et al. (2010), The preclinical pharmacology of roflumilast—a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease; Pulm, Pharmacol. Ther., 23 235
2) Rabe et al. (2011), Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease; Br. J. Pharmacol, 163 53
3) Heckman et al. (2018), Acute administration of roflumilast enhances sensory gating in healthy young humans in a randomized trial; Psychopharmacology (Berl.), 235 301
4) Vanmierlo et al. (2016), The PDE4 inhibitor roflumilast improves memory in rodents at non-emetic doses; Behav. Brain Res., 303 26
5) Tikoo et al. (2014), Calorie restriction mimicking effects of roflumilast prevents diabetic nephropathy; Biochem. Biophy. Res. Commun., 450 1581
6) Mollmann et al. (2017), The PDE4 inhibitor roflumilast reduced weight gain by increasing energy expenditure and leads to improved glucose metabolism; Diabetes Obes. Metab., 19 496

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Catalog#  10-2657-0010

$50.00
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CAS:
162401-32-3
Catalog Number:
10-2657
Activity:
PDE4 inhibitor
Chemical Name:
3(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)-benzamide
Alternate Names:
BYK-20869
Molecular Weight:
403.21
Molecular Formula:
C17H14N2Cl2F2O3
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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