GSK-256066

Research use only, not for human use.

A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively.

A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/2/3/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.COPD Phase 2 Discontinued.

——

Animal Model:Male Brown Norway rats (180-200 g)Dosage:10 μg/kg Administration:Intratracheal injection; before (36 hours, 24 hours, 18 hours, 12 hours, 6 hours, and 2 hours) and after (0 hour, 2 hours) LPS challenge Result:Inhibited the LPS-induced pulmonary neutrophilia.

GSK256066 | GSK 256066

Angiogenesis

PDE

PDE4B

Inflammation/Immunology

COPD

801312-28-7

518.5842

C27H26N4O5S

>98% (HPLC)

DMSO: ≥ 5.2 mg/mL

CC1=CC(=CC2=C(C(=CN=C12)C(=O)N)NC3=CC(=CC=C3)OC)S(=O)(=O)C4=CC=CC(=C4)C(=O)N(C)C

3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-

(-20℃)

With Ice Pack

≥ 2 years