GlyT Inhibitor

NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC₅₀s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.

ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model.

ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.

MPDC is a potent and competitive inhibitor of the Na⁺-dependent high-affinity glutamate transporter in forebrain synaptosomes.

Sarcosine-¹⁵N is the ¹⁵N-labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia.

Bitopertin R enantiomer (RG1678 R enantiomer; RO4917838 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.

LY2365109 is a potent and selective GlyT1 inhibitor, with an IC₅₀ of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.

Org 25543 is a selective inhibitor of the glycine transporter 2, exhibiting analgesic properties in a rat model of chronic pain.

Org-24598 lithium is an inhibitor of glycine transporter 1 GlyT-1 . Org-24598 lithium can inhibit the specific binding of [³H] CHIBIA-3007 to the rat brain membranes with a Ki value of 16.9 nM.

DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey.

Org-24598 is an inhibitor of glycine transporter 1 GlyT-1 . Org-24598 can inhibit the specific binding of [³H] CHIBIA-3007 to the rat brain membranes with a Ki value of 16.9 nM.

Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).

8-Hydroxyamoxapine is an orally active antidepressant, which inhibits the reuptake of norepinephrine and serotonin at synapses.

TASP0315003 is a glycine transporter 1 (GlyT1) inhibitor. TASP0315003 potentiates NMDA receptor function by increasing synaptic glycine levels. TASP0315003 can improve cognitive dysfunction and the negative symptoms of schizophrenia without having undesirable central nervous system side effects. TASP0315003 can be used for the research of neurological disease.

PF-03463275 hydrochloride is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a K_i of 11.6 nM. PF-03463275 hydrochloride has the potential for Schizophrenia research.

ALX-5407 ((R)-NFPS) is a selective and orally active glycine transporter GlyT1 inhibitor with an IC₅₀ value of 3 nM. ALX-5407 can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia.

Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [³H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia.

LY2365109 (hydrochloride) (Standard) is the analytical standard of LY2365109 (hydrochloride) (HY-100416A). This product is intended for research and analytical applications. LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.

Stearoyl-L-carnitine-d9 chloride is the deuterium labeled Stearoyl-L-carnitine chloride. Stearoyl-L-carnitine chloride, a fatty ester lipid molecule, is an endogenous metabolite. Stearoyl-L-carnitine chloride can be used as PKC inhibitor. Stearoyl-L-carnitine chloride accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoyl-L-carnitine chloride inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoyl-L-carnitine chloride acts as a metabolomics biomarker for Parkinson’s disease. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2.

Bitopertin (Standard) is the analytical standard of Bitopertin. This product is intended for research and analytical applications. Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.