GlyT Inhibitor

Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.

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.

N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC₅₀ = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC₅₀ = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.
The product specifications provided below refer solely to the active content of N-Arachidonylglycine.

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

Stearoyl-L-carnitine chloride is an endogenous long-chain acylcarnitine. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2. Stearoyl-L-carnitine chloride inhibits glycine responses by 16.8% at concentrations up 3 μM.

Org 25935 is a potent and selective glycine transporter 1 protein (GlyT1) inhibitor with an IC₅₀ value of 100 nM. Org 25935 can decrease ethanol (EtOH) intake and EtOH preference in rats, whereas water intake is unaffected. Org 25935 can be used for researching alcohol dependence or abuse.

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.

Sarcosine-d₃ is the deuterium 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.

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

Sarcosine (Standard) is the analytical standard of Sarcosine. This product is intended for research and analytical applications. 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.

Org 25543 hydrochloride is a selective and irreversible GlyT2 inhibitor (IC₅₀: 16 nM). Org 25543 hydrochloride has analgesia effect. Org 25543 hydrochloride ameliorates mechanical allodynia after partial sciatic nerve ligation injury in mice.

Stearoyl-L-carnitine-d₃ (chloride) is the deuterium labeled Stearoyl-L-carnitine chloride. Stearoyl-L-carnitine chloride is an endogenous long-chain acylcarnitine. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2. Stearoyl-L-carnitine chloride inhibits glycine responses by 16.8% at concentrations up 3 μM.

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

PF-03463275 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 has the potential for Schizophrenia research.

GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC₅₀ of 38 nM for rGlyT1. Antipsychotic activity.

SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC₅₀=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.

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

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.