gat-3

6,7-Dimethylisatin (6,7-dimethyl-1H-indole-2,3-dione) inhibits hGAT3 with IC50 of 108 μM. 6,7-Dimethylisatin also inhibits hBGT1, hGAT2.

SKF89976A hydrochloride (d,l-SKF89976A hydrochloride) is a selective inhibitor GABA transporter such as GAT-1 (IC50s = 0.28 μM), GAT-2 (IC50s = 137.34 μM) and GAT-3(IC50s = 202.8 μM) in CHO cells.

(S)-SNAP5114 is a selective inhibitor of GABA transport, exhibiting IC50 values of 5 μM for hGAT-3 and 21 μM for rGAT-2, and possesses anticonvulsant properties.

Guvacine hydrobromide is an alkaloid discovered in Areca catechu and a GABA uptake inhibitor with IC50 values of 39 μM/58 μM/378 μM for rat GAT-1/GAT-2/GAT-3.

Guvacine is a natural alkaloid and selective GAT (GABA transporter) inhibitor, serving as a lead structure for GAT inhibitors with psychoactive properties.

PF-06471553 is an effective and selective inhibitor of monoacylglycerol acyltransferase 3 (IC50: 92 nM).

T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

mGAT3/4-IN-2 are potent inhibitors of mGAT3/mGAT4 with their pIC50 values of 5.44 and 5.25, respectively.

mGAT3/4-IN-1 is a potent inhibitor of mGAT3/mGAT4, and their pIC50 values were 5.31 and 5.24, respectively. mGAT3/4-IN-1 significantly inhibited tactile abnormal pain in diabetic neuropathic mice.

N-Acetylglucosaminyltransferase III [EC:2.4.1.144, MGAT3] transfers a GlcNAc residue to the β-linked mannose of an N-linked oligosaccharide's trimannosyl core, resulting in the formation of bisected GlcNAc.

SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo.