A selective PDE4 inhbitor
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GSK356278

Item No. 30412

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[5-[(2,4-dimethyl-5-thiazolyl)methyl]-1,3,4-oxadiazol-2-yl]-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine
CAS Number
720704-34-7
Molecular Formula
C21H25N7O2S
Formula Weight
439.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 30 mg/ml
λmax
247, 255, 310 nm
SMILES
CC1=C(CC2=NN=C(C3=CN=C4C(C=NN4CC)=C3NC5CCOCC5)O2)SC(C)=N1
InChi Code
InChI=1S/C21H25N7O2S/c1-4-28-20-15(11-23-28)19(25-14-5-7-29-8-6-14)16(10-22-20)21-27-26-18(30-21)9-17-12(2)24-13(3)31-17/h10-11,14H,4-9H2,1-3H3,(H,22,25)
InChi Key
AWDJJMXJUOHGLC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $63

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    10 mg

    $105

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    25 mg

    $229

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    50 mg

    $423

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    Product Description

    GSK356278 is a potent, selective, and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with anxiolytic and cognition-improving effects.1 It is greater than 100-fold selective for PDE4A, -B, and -D (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively) over 10 other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels, and enzymes. It inhibits LPS-induced release of TNF-α in isolated human whole blood (IC50 = 23.1 nM) and reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg). GSK356278 (0.01-1 mg/kg) induces anxiolytic behavior in marmosets, and improves performance of non-human primates in an object retrieval test when administered at a dose of 1 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rutter, A.R., Poffe, A., Cavallini, P., et al. GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species. J. Pharmacol. Exp. Ther. 350(1), 153-163 (2014).