Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H4417 |
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. |
H4416 |
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. |
H4415 |
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. |
H4414 |
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. |
H4413 |
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. |
H4412 |
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. |
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