GSK356278

Additional information:
GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively.{{Omecamtiv mecarbil} MedChemExpress|{Omecamtiv mecarbil} Myosin|{Omecamtiv mecarbil} Biological Activity|{Omecamtiv mecarbil} Formula|{Omecamtiv mecarbil} manufacturer|{Omecamtiv mecarbil} Epigenetics} GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.|Product information|CAS Number: 720704-34-7|Molecular Weight: 439.53|Formula: C21H25N7O2S|Chemical Name: 5-{5-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-1,3,4-oxadiazol-2-yl}-1-ethyl-N-(oxan-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine|Smiles: CCN1N=CC2C(NC3CCOCC3)=C(C=NC1=2)C1=NN=C(CC2SC(C)=NC=2C)O1|InChiKey: AWDJJMXJUOHGLC-UHFFFAOYSA-N|InChi: 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)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 12.5 mg/mL (28.44 mM; ultrasonic and warming and heat to 60°C).{{Pembrolizumab} site|{Pembrolizumab} PD-1/PD-L1|{Pembrolizumab} Biological Activity|{Pembrolizumab} In stock|{Pembrolizumab} supplier|{Pembrolizumab} Cancer} |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.PMID:24059181 |Shelf Life: ≥12 months 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|How to use|In Vitro:|GSK356278 competes with [3H]rolipram for the high affinity rolipram binding site (HARBS) with a pKi of 8.6 in a competitive filtration-binding assay to the recombinant human PDE4B2B enzyme expressed in yeast membranes. GSK356278 bounds to the HARBS in rats, mice, marmosets, and ferrets with pKis of 7.9, 7.8, 8.4, and 8.5, respectively. GSK356278 inhibits LPS-induced release of TNF-α in human whole blood, with a pIC50 of 7.6.|In Vivo:|GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding. GSK356278 (0.1-0.1 mg/kg; p.o.) demonstrates efficacy in a nonhuman primate model of anxiety at exposures that do not induce emesis. GSK356278 (4 doses at 0.03, 0.1, 0.3, and 1.0 mg/kg for 6 weeks; p.o.) enhances performance in a nonhuman primate object retrieval test.GSK356278 exhibits oral bioavailability (rat 91%, monkey 23%) and Cmax (rat 205, monkey 41 nM) following oral administration (rat 1, monkey 0.2 mg/kg). GSK356278 exhibits terminal elimination half-lives (rat 2.2, monkey 1.5 h) due to moderate blood clearance (rat 40, monkey 16 mL/min/kg) combined with volumes of distribution (rat 6.3, monkey 2.1 L/kg) following intravenous administration (rat 1, monkey 0.2 mg/kg).|Products are for research use only. Not for human use.|