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Product info sheet

Chemical structure alt
Chemical name 2-Amino-4-methyl-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile
CAS no  --
MW 330.2
Purity >98% (HPLC)
Solubility Up to 25 mM in DMSO
Pharmacology Ki: 0.42 µM at EAAT1; >300 µM at EAAT2; >300 µM at EAAT3
Bioavailability Half-life of 30 min in serum after oral administration in rat. Penetrates the blood-brain-barrier (BBB)
Litterature references

(1) Jensen, AA; Erichsen, MN; Nielsen, CW; Stensbøl, TB; Kehler, J and Bunch, L ”Discovery of the First Selective Inhibitor of Human Excitatory Amino Acid Transporter Subtype 1” J. Med. Chem. 200952, 912

(2) Erichsen, MN; Huynh, THV; Abrahamsen, B; Bastlund, JF; Bundgaard, C; Monrad, O; Bekker-Jensen, A; Nielsen, CW; Frydenvang, K; Jensen, AA and Bunch, L “Structure-Activity-Relationship Study of 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. 2010, 53, 7180-7191

(3) Bunch, L; Erichsen, MN and Jensen, AA “Excitatory Amino Acid Transporters as Potential Drug Targets“ Exp. Opin. Ther. Targ. 200913, 719-731

(4) Huynh, THV; Shim, I; Bohr, H;Abrahamsen B; Nielsen, B; Jensen, AA and Bunch, L “Structure-Activity-Relationship Study of Selective EAAT1 Inhibitor UCPH-101 and Absolute Configurational Assignment using Infrared (IR) and Vibrational Circular Dichroism (VCD) Spectroscopy in Combination with Ab Initio Hartree-Fock Calculations” J. Med. Chem. 201255, 5403-5412

Patents (IPRs)

WO/2010/066253: SELECTIVE INHIBITORS OF EXCITATORY AMINO ACID TRANSPORTER SUBTYPE 1 (EAAT1/GLAST) by L. Bunch and A. A. Jensen

US Patent 20120035361: SELECTIVE INHIBITORS OF EXCITATORY AMINO ACID TRANSPORTER SUBTYPE 1 (EAAT1/GLAST) by L. Bunch and A. A. Jensen

Price and Availability

    10 mg: EUR 195,-

    50 mg: EUR 795,-

  100 mg: Contact us

  500 mg: Contact us

1000 mg: Contact us

2000 mg: Contact us

 

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The commercial rights to UCPH-102 are covered by patents listed above.

 

All IPRs belong to Hugin NeuroChemicals

 

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