gat-2

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.

BPDBA is an effective, selective, and non-competitive inhibitor of the betaine/GABA transporter (BGT-1), displaying inhibitory activity against human BGT-1 and mouse GAT2, with IC50 values of 20 μM and 35 μM, respectively.

Xanthohumol, also known as 2', 4, 4'-trihydroxy-6'-methoxy-3'-prenylchalcone or desmethylxanthohumol, is a member of the class of compounds known as 3-prenylated chalcones. It inhibits COX-1 and COX-2 activity and shows chemopreventive effects.

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.

MGAT2-IN-1 is an orally active monoacylglycerol acyltransferase (MGAT2)inhibitor (human and mouse MGAT2 with IC50 of 7.8 and 2.4 nM , respectively).

MGAT2-IN-2 is a potent inhibitor of acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) with an IC50 of 3.4 nM.

PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inhibition. It operates in a noncompetitive manner relative to the acyl-CoA substrate, marking its efficacy in targeting DGAT2.

PF-06424439 is an oral and selective inhibitor of imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) (IC50 of 14 nM).

DGAT2-IN-3 (compound 9) is an inhibitor of DGAT2 with an IC50 value of 0.4 nM. It is utilized in research related to fatty liver disease, diabetes, and cardiovascular diseases.

GAT2711 is a full agonist of α9nAChR, with an EC50 of 230 nM. It exhibits 340 times greater selectivity for α9 over α7nAChR. In THP-1 cells, GAT2711 inhibits ATP-induced IL-1β release. Additionally, GAT2711 retains full analgesic activity in α7nAChR knockout mice.

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

JNJ-DGAT2-A, a specific inhibitor of DGAT2(IC50 = 0.14 μM), can be used in studies about the synthesis of triglycerides.

JNJ-DGAT2-B is a selective inhibitor of Diacylglycerol acyltransferase 2.

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

BMS-963272 is a selective and potent MGAT2 inhibitor with an IC50 value of 7.1 nM used in the study of metabolic disorders and obesity.

GAT228, an allosteric ligand for the cannabinoid receptor 1 (CB1), functions as the enantiomer of GAT211 [1].

A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor of human and mouse DGAT-1 with IC50 values of 7 nM and 24 nM, respectively, demonstrating good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

PF-07202954 is a DGAT2 inhibitor with a long half-life. Its IC50 values for human DGAT2 and rat DGAT2 are 10 nM and 9.1-33 nM respectively. It can reduce the triglyceride content in the liver of rats fed with a Western diet and can be used for the study of non-alcoholic fatty liver disease (NASH).

MGAT2-IN-4 (compound 33) is a monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with liver metabolic stability, applicable in obesity, diabetes, and non-alcoholic steatohepatitis (NASH) research [1].

Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor. Ervogastat reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).

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.