UCPH-101

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.Formal Name: 2-amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7-(1-naphthalenyl)-5-oxo-4H-1-benzopyran-3-carbonitrile. CAS Number: 1118460-77-7. Molecular Formula: C27H22N2O3. Formula Weight: 422.5. Purity: >98% (mixture of isomers). Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 25 mg/ml. lambdamax: 225, 282 nm. SMILES: COC(C=C1)=CC=C1C2C(C#N)=C(N)OC3=C2C(C[C@@H](C4=C(C=CC=C5)C5=CC=C4)C3)=O. InChi Code: InChI=1S/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,25H,13-14,29H2,1H3/t18-,25?/m1/s1. InChi Key: YBMGNDPBARCLFT-YDONVPIESA-N.