Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC 50 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.
性状
Solid
IC50 & Target[1][2]
PDE4D3 0.5 nM (IC50)
体外研究(In Vitro)
Oglemilast (GRC 3886) has EC50s of 11.4 nM, 4.4 nM for PDE 4B1 and PDE 4D3 reporter cell lines, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.[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.
溶解度数据
In Vitro: DMSO : 4 mg/mL (7.75 mM; Need ultrasonic)配制储备液