1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. GlyT

GlyT

Glycine transporters

Glycine transporters (GlyTs) are members of the Na+/Cl--dependent transporter family, whose activities and subcellular distributions are regulated by phosphorylation and interactions with other proteins. GlyTs comprise glycine transporter type 1 (SLC6A9; GlyT1) and glycine transporter type 2 (SLC6A5; Glyt2). Both GlyTs exist in multiple splice variants. GlyTs that regulate levels of brain glycine, an inhibitory neurotransmitter with co-agonist activity for NMDA receptors (NMDARs), have been considered to be important targets for the treatment of brain disorders with suppressed NMDAR function such as schizophrenia.

GlyT1 and GlyT2 are expressed on both astrocytes and neurons, but their expression pattern in brain tissue is foremost related to neurotransmission. GlyT2 is markedly expressed in brainstem, spinal cord and cerebellum, where it is responsible for glycine uptake into glycinergic and GABAergic terminals. GlyT1 is abundant in neocortex, thalamus and hippocampus, where it is expressed in astrocytes, and involved in glutamatergic neurotransmission. GlyT1 and GlyT2, which are located in glial cells and neurons, respectively play important roles by clearing synaptically released glycine or supplying glycine to glycinergic neurons to regulate glycinergic neurotransmission. Thus, inhibition of GlyTs could be used to modify pain signal transmission in the spinal cord.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103332
    N-Arachidonylglycine
    Inhibitor 98.82%
    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.
    N-Arachidonylglycine
  • HY-10809
    Bitopertin
    Inhibitor 99.59%
    Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
    Bitopertin
  • HY-101037
    Sarcosine
    Inhibitor ≥98.0%
    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.
    Sarcosine
  • HY-138935
    Iclepertin
    Inhibitor 99.65%
    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.
    Iclepertin
  • HY-10716A
    PF-03463275
    Inhibitor 98.40%
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
    PF-03463275
  • HY-10712
    Org-24598
    Inhibitor
    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.
    Org-24598
  • HY-12389
    8-Hydroxyamoxapine
    Inhibitor
    8-Hydroxyamoxapine is an orally active antidepressant, which inhibits the reuptake of norepinephrine and serotonin at synapses.
    8-Hydroxyamoxapine
  • HY-107527
    Org 25543 hydrochloride
    Inhibitor
    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.
    Org 25543 hydrochloride
  • HY-130466
    Stearoyl-L-carnitine chloride
    Inhibitor ≥99.0%
    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.
    Stearoyl-L-carnitine chloride
  • HY-109067A
    Opiranserin hydrochloride
    Antagonist 99.44%
    Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain.
    Opiranserin hydrochloride
  • HY-10711A
    ALX-5407 hydrochloride
    Inhibitor ≥98.0%
    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.
    ALX-5407 hydrochloride
  • HY-100416A
    LY2365109 hydrochloride
    Inhibitor 98.69%
    LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.
    LY2365109 hydrochloride
  • HY-110176
    ASP2535
    Inhibitor 99.44%
    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.
    ASP2535
  • HY-112432
    GlyT1 Inhibitor 1
    Inhibitor 98.35%
    GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC50 of 38 nM for rGlyT1. Antipsychotic activity.
    GlyT1 Inhibitor 1
  • HY-101037S1
    Sarcosine-d3
    Inhibitor ≥98.0%
    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[1][2].
    Sarcosine-d<sub>3</sub>
  • HY-10715
    SSR504734
    Inhibitor 99.82%
    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.
    SSR504734
  • HY-107526
    (Rac)-ALX 5407
    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.
    (Rac)-ALX 5407
  • HY-111029
    ALX-1393
    Inhibitor ≥99.0%
    ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model.
    ALX-1393
  • HY-101334
    MPDC
    Inhibitor
    MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes.
    MPDC
  • HY-101037S
    Sarcosine-15N
    Inhibitor ≥99.0%
    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[1][2].
    Sarcosine-<sup>15</sup>N

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