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Cat. No. Product Name CAS No. Information
PC-42093

SKF-89976A hydrochloride

85375-15-1

A potent, selective and GABA transporter 1 (GAT1) inhibitor with IC50 of 0.13 uM for hGAT1; shows little to no activity for rGAT-2, hGAT-3 and hBGT-1 (IC50>500 uM); blocks GABA uptake and uncoupled transmitter-gated current with Ki of 7 uM and 0.03 uM, respectively.

PC-62933

CI-966

110283-79-9 CI-966 (PD 126141) is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively; displays >200-fold selectivity over GAT-2 and GAT-3; shows anticonvulsive and neuroprotective activity in vivo.

Epilepsy

Phase 1 Discontinued

PC-62932

CI-966 hydrochloride

110283-66-4 CI-966 is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively; displays >200-fold selectivity over GAT-2 and GAT-3; shows anticonvulsive and neuroprotective activity in vivo.

Epilepsy

Phase 1 Discontinued

PC-62931

NNC-711

145645-62-1 NNC-711 is a potent and selective inhibitor of GABA uptake by GAT-1 with IC50 of 0.04 uM; displays excellent selectivty over rGAT-2, hGAT-3 and hBGT-1, and other other neurotransmitter receptors; inhibits synaptosomal (IC50=47 nM), neuronal (IC50=1238 nM) and glial (IC50=636 nM) GABA uptake in vitro; demonstrates potent anticonvulsant activity against rodent seizures induced by DMCM.
PC-62929

NNC 05-2090 hydrochloride

184845-18-9 NNC 05-2090 is a potent selective GABA transporter inhibitor of mGAT2 with Ki of 1.4 uM; displays >10 fold selectivity over mGAT1, mGAT3 and mGAT4, also has alpha 1- and D2-receptor affinity of 266 and 1632 nM, respectively; inhibits 3HGABA uptake into synaptosomes from cerebral cortex with IC50 of 4.4 uM; significantly reduces generalized seizure severity and afterdischarge duration in rats.
PC-61113

SNAP 5114

157604-55-2 A GABA transport inhibitor with IC50 of 5, 21, 388 and 140 uM for hGAT-3, rGAT-2, hGAT-1 and BGT-1, respectively; increases thalamic GABA levels and is an anticonvulsant following systemic administration in vivo.

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