| Identification | Back Directory | [Name]
UCPH-101 | [CAS]
1118460-77-7 | [Synonyms]
CS-2757
UCPH-101
UCPH-101; UCPH 101; UCPH101
2-Amino-4-(4-methoxy-phenyl)-7-naphthalen-1-yl-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile
2-Amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-4H-chromene-3-carbonitrile
2-amino-4-(4-methoxyphenyl)-7-(naphthalene-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile
4H-1-Benzopyran-3-carbonitrile, 2-aMino-5,6,7,8-tetrahydro-4-(4-Methoxyphenyl)-7-(1-naphthalenyl)-5-oxo- | [Molecular Formula]
C27H22N2O3 | [MOL File]
1118460-77-7.mol | [Molecular Weight]
422.48 |
| Chemical Properties | Back Directory | [Melting point ]
194.0-197.2 °C | [Boiling point ]
703.5±60.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
Soluble in DMSO (up to 10 mg/ml). | [form ]
solid | [pka]
3.23±0.60(Predicted) | [color ]
Off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system. UCPH-1 is selective for EAAT1 over EAAT2 and EAAT3 with IC50 values of 0.66, >300, and >300 μM, respectively, in a radioligand uptake assay using HEK293 cells transfected with the human transporter. It selectively inhibits anion currents in tsA201 cells expressing human EAAT1 (Kd = 0.34 μM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 μM. UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier. | [Uses]
UCPH 101 is a subtype-selective inhibitor of human excitatory amino acid transporter subtype 1. | [IC 50]
EAAT1 | [storage]
Store at +4°C | [References]
1) Jensen?et al.?(2009),?Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1; J. Med. Chem.,?52?912
2) Erichsen?et al.?(2010),?Structure-Activity Relationship Study of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101); J. Med. Chem.,?53?7180
3) Corbetta?et al.?(2019),?Altered function of the glutamate-aspartate transporter GLAST, a potential therapeutic target in glioblastoma; Int. J. Cancer,?144?2539 |
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