Oglemilast

Short Summary : Potent PDE4 inhibitor

Category : Metabolism|PDE

Purity : 0.98

CAS Number : 778576-62-8

Formula : C20H13Cl2F2N3O5S

Molecular Weight : 516.3

SMILE : CS(=O)(=O)NC1=CC2=C(C=C1)OC3=C(C=CC(=C23)C(=O)NC4=C(C=NC=C4Cl)Cl)OC(F)F

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : Oglemilast Description:IC50: 2.5 nM (PDE4B) and 1.7 nM (PDE4D) [1]Among the emerging agents to treat COPD or asthma, phosphodiesterase 4 (PDE4) inhibitors have attracted particular attention. PDE4 inhibitors have been in development as a novel anti-inflammatory therapy since the 1980s with asthma and chronic obstructive pulmonary disease (COPD) being primary indications. Oglemilast is an orally administered inhibitor drug which is touted as an important and novel therapeutic target for asthma and chronic obstructive pulmonary disease (COPD), also known as smoker’s cough.In vitro: Oglemilast (GRC-3886), a potent PDE4 inhibitor, inhibited PDE4 enzyme with an IC50 value of 1.4 nM and exhibited > 7,000-fold selectivity over other PDE (PDE1–11) families. In human whole blood assays, oglemilast inhibited LPS-induced TNF? production with an IC50 value of 190 nM and [2]. In vivo: Oglemilast oral treatment of rats blocked Lipopolysaccharide (LPS)-induced pulmonary neu-trophilia with an ID50 of 1.45 mg/kg. In ferrets, oglemilast neither induced emesis nor caused any behavioral changes associated with emesis at 100 mg/kg. Hence, oglemilast could represent a new generation of potent selective PDE4 inhibitor with significantly improved emetic side-effect profile [2]. Clinical trial: Glenmark Pharmaceuticals’ licensing partner, Forest Laboratories, announced that the Phase IIb results on Oglemilast did not show a statistically meaningful increase from the baseline compared to the placebo (dummy drug). The markets took to this badly and the stock was pummeled on the bourses.Reference:[1] Gorja DR, Mukherjee S, Meda CL, Deora GS, Kumar KL, Jain A, Chaudhari GH, Chennubhotla KS, Banote RK, Kulkarni P, Parsa KV, Mukkanti K, Pal M. Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitors. Org Biomol Chem. 2013;11(13):2075-9.[2] Vakkalanka SKVS, Balasubramaniam LA, Gharat LA, et al. The pharmacological and safety profile of a novel selective phosphodiesterase-4 (PDE4) inhibitor:GRC-3886. Eur Respir J 2004;24:1391

Download datasheet