| Identification | Back Directory | [Name]
N-((3S,4S)-4-(4-(5-cyanothiophen-2-yl)phenoxy)tetrahydrofuran-3-yl)propane-2-sulfonamide | [CAS]
1258963-59-5 | [Synonyms]
EOS-62062
PF-4958242
PF-4958242 1258963-59-5
N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide
N-((3S,4S)-4-(4-(5-cyanothiophen-2-yl)phenoxy)tetrahydrofuran-3-yl)methanesulfonamide
2-Propanesulfonamide, N-[(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydro-3-furanyl]-
N-((3S,4S)-4-(4-(5-cyanothiophen-2-yl)phenoxy)tetrahydrofuran-3-yl)propane-2-sulfonamide | [Molecular Formula]
C18H20N2O4S2 | [MOL File]
1258963-59-5.mol | [Molecular Weight]
392.49 |
| Chemical Properties | Back Directory | [Boiling point ]
577.5±60.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
9.75±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator of AMPA receptor (an AMPA potentiator) with an EC50 of 310 nM and a Ki of 170 nM[1]. | [in vivo]
Pesampator (0.1-1 mg/kg; SC) dose-dependently increases CD-1 mouse cerebellum cGMP and Pesampator (0.1-0.32 mg/kg; SC) decreases fall latency in C57BL/6J mice traversing an accelerating rotarod[1].
Pesampator (0.001-0.01 mg/kg; male Sprague-Dawley rats) reverses the MK-801-mediated (0.05 mg/kg; IV) reduction in paired-pulse facilitation (PPF) after cumulative or a single (0.01 mg/kg) intravenous dose[1].
Pesampator (0.0032–0.032 mg/kg; SC) attenuates ketamine-induced working memory disruptions in rats as determined by mean errors in a radial arm maze[1].
In rats, Pesampator (0.027, 0.08, and 0.60 mg/kg; SC) dose-dependently affectes the regional brain uptake of 2-deoxy-2-[18F]fluoro-d-glucose (FDG)[1]. | [storage]
Store at -20°C | [References]
[1] Shaffer CL, et al. The discovery and characterization of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor potentiator N-{(3S,4S)-4-[4-(5-cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242). J Med Chem. 2015;58(10):4291-4308. DOI:10.1021/acs.jmedchem.5b00300 |
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