LY404187 – 10 mg

Brand:
Cayman
CAS:
211311-95-4
Storage:
-20
UN-No:
Non-Hazardous - /

LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.{46485} It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.{46486,46487} LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA (Item No. 25330) in mouse and rat, respectively, models of Parkinson’s disease when administered at a dose of 0.5 mg/kg per day.{46488}  

 

Available on backorder

SKU: 28741 - 10 mg Category:

Description

A benzothiadiazide positive allosteric modulator of AMPA receptors; increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 µM, respectively, in a calcium influx assay; selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 µM; increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 µM, respectively), but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons; prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA in mouse and rat, respectively, models of Parkinson’s disease at 0.5 mg/kg per day


Formal name: N-[2-(4′-cyano[1,1′-biphenyl]-4-yl)propyl]-2-propanesulfonamide

Synonyms: 

Molecular weight: 342.5

CAS: 211311-95-4

Purity: ≥98%

Formulation: A solid