gsk256066

Description: GSK256066 (GSK-256066; GSK 256066) is a novel, potent and selective inhibitor of PDE4B (phosphodiesterase 4B) with important biological activity (e.g. inhibiting pulmonary neutrophilia). It inhibits PDE4B with an IC50 of 3.2 pM, and has > 380, 000-fold selectivity for PDE4B over PDE1/2/3/5/6. GSK256066 can be administered by inhalation which can minimize the potential for side effects. It demonstrated a protective effect on the EAR and LAR. GSK256066 has been demonstrated to have exceptional potency in vitro and in vivo and is being clinically investigated as a treatment for chronic obstructive pulmonary disease.

References: J Pharmacol Exp Ther. 2011 Apr; 337(1):145-54; J Pharmacol Exp Ther. 2011 Apr; 337(1):137-44.

Related CAS: 801315-14-0 (HCl salt); 1415560-64-3 (TFA salt); 801312-28-7 (free base);

Chemical Name: 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

InChi Key: JFHROPTYMMSOLG-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H26N4O5S/c1-16-11-21(37(34, 35)20-10-5-7-17(12-20)27(33)31(2)3)14-22-24(16)29-15-23(26(28)32)25(22)30-18-8-6-9-19(13-18)36-4/h5-15H, 1-4H3, (H2, 28, 32)(H, 29, 30)

SMILES Code: O=C(C1=C(NC2=CC=CC(OC)=C2)C3=CC(S(=O)(C4=CC=CC(C(N(C)C)=O)=C4)=O)=CC(C)=C3N=C1)N