GSK256066 (2,2,2-trifluoroacetic acid)

GSK256066 is a potent and selective PDE4 inhibitor that can be given by inhalation, minimising the potential for side effects. GSK256066 demonstrated a protective effect on the EAR and LAR. GSK256066 is a slow and tight binding inhibitor of PDE4B (apparent IC(50) 3.2 pM; steady-state IC(50) <0.5 pM), which is more potent than any previously documented compound, for example, roflumilast (IC(50) 390 pM), tofimilast (IC(50) 1.6 nM), and cilomilast (IC(50) 74 nM). Consistent with this, GSK256066 inhibited tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC(50). 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.

Product information

CAS Number: 1415560-64-3

Molecular Weight: 632.61

Formula: C29H27F3N4O7S

Chemical Name: 6-[3-(dimethylcarbamoyl)benzenesulfonyl]-4-[(3-methoxyphenyl)amino]-8-methylquinoline-3-carboxamide; trifluoroacetic acid

Smiles: CC1=CC(=CC2=C1N=CC(C(N)=O)=C2NC1=CC(=CC=C1)OC)S(=O)(=O)C1=CC(=CC=C1)C(=O)N(C)C.OC(=O)C(F)(F)F

InChiKey: PTTKEASHQDSBJR-UHFFFAOYSA-N

InChi: InChI=1S/C27H26N4O5S.C2HF3O2/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;3-2(4,5)1(6)7/h5-15H,1-4H3,(H2,28,32)(H,29,30);(H,6,7)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.