GSK-356278 - CAS 720704-34-7
Catalog number: 720704-34-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H25N7O2S
Molecular Weight:
439.54
COA:
Inquire
Targets:
PDE4
Description:
GSK-356278 is a selective Type 4 cyclic nucleotide phosphodiesterase inhibitor. It shows anxiolytic and cognition-enhancing effects and it has the ability to elevate cAMP in various cell types of the central nervous system. No development was reported for phase-I development in Major depressive disorder and Huntington's-disease.
Purity:
98%
Appearance:
Powder
Synonyms:
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
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Huntington's disease; Major depressive disorder
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
AWDJJMXJUOHGLC-UHFFFAOYSA-N
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)
Canonical SMILES:
CCn1c2c(cn1)c(c(cn2)c3nnc(o3)Cc4c(nc(s4)C)C)NC5CCOCC5
Current Developer:
Originator GlaxoSmithKline
1.GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species.
Rutter AR;Poffe A;Cavallini P;Davis TG;Schneck J;Negri M;Vicentini E;Montanari D;Arban R;Gray FA;Davies CH;Wren PB J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. doi: 10.1124/jpet.114.214155. Epub 2014 Apr 30.
Small molecule phosphodiesterase (PDE) 4 inhibitors have long been known to show therapeutic benefit in various preclinical models of psychiatric and neurologic diseases because of their ability to elevate cAMP in various cell types of the central nervous system. Despite the registration of the first PDE4 inhibitor, roflumilast, for the treatment of chronic obstructive pulmonary disease, the therapeutic potential of PDE4 inhibitors in neurologic diseases has never been fulfilled in the clinic due to severe dose-limiting side effects such as nausea and vomiting. In this study, we describe the detailed pharmacological characterization of GSK356278 [5-(5-((2,4-dimethylthiazol-5-yl)methyl)-1,3,4-oxadiazol-2-yl)-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine], a potent, selective, and brain-penetrant PDE4 inhibitor that shows a superior therapeutic index to both rolipram and roflumilast in various preclinical species and has potential for further development in the clinic for the treatment of psychiatric and neurologic diseases. GSK356278 inhibited PDE4B enzyme activity with a pIC50 of 8.8 and bound to the high-affinity rolipram binding site with a pIC50 of 8.6. In preclinical models, the therapeutic index as defined in a rodent lung inflammation model versus rat pica feeding was >150 compared with 0.
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