MW: 518.6 Da CAS Registry #: 801312-28-7 Formula: C
27H
26N
4O
5S Target: PDE4 Description:GSK256066 is a selective PDE4 inhibitor with an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 vs. other PDE isoforms. Often used clinically by inhalation in chronic obstructive pulmonary disease and asthma. Synonym(s): 6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide Biological Activity: IC50 =3.2 pM for PDE4B, with >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. GSK256066 inhibits PDE4 isoforms A-D with equal affinity. Solubility: Soluble in DMSO (>4.6 mg/mL). Minimal solubility in water (< 1.2 mg/mL) Storage / Stability:
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Reference(s): 1. Tralau-Stewart CJ, et al. J Pharmacol Exp Ther, 2011, 337(1), 145-154.2. Woodrow MD, et al. Bioorg Med Chem Lett, 2009, 19(17), 5261-5265. Scientific Category: PDE Inhibitor Product Type: Inhibitor Data shown is lot-specific. Contact us for specific information on other lots.
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