oglemilast Chemical Properties

Density 

1.653

storage temp. 

Store at -20°C

solubility 

DMSO : 4 mg/mL (7.75 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)

form 

Powder

pka

7.10±0.30(Predicted)

color 

Light yellow to khaki

oglemilast Usage And Synthesis

Uses

Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases[1][2][3].

target

PDE4

IC 50

PDE4D3: .5 nM (IC₅₀)

References

[1] Giembycz MA. Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking Br J Pharmacol. 2008 Oct;155(3):288-90. DOI:10.1038/bjp.2008.297
[2] Rabe KF, et al. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163(1):53-67. DOI:10.1111/j.1476-5381.2011.01218.x
[3] Wunder F, et al. Characterization of the cellular activity of PDE 4 inhibitors using two novel PDE 4 reporter celllines. Mol Pharm. 2013 Oct 7;10(10):3697-705. DOI:10.1021/mp400206m