GlyT

Cat. No.

A15021

CAS No.

845614-11-1

Bitopertin

Synonyms: RG1678; RO4917838

RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).

Cat. No.

A15022

CAS No.

845614-12-2

Bitopertin (R enantiomer)

Synonyms: RG1678 (R enantiomer); RO4917838 (R enantiomer)

RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).

Cat. No.

A16692

CAS No.

107-97-1

Sarcosine

Synonyms: N-Methylglycine; Sarcosin

Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.

Cat. No.

A19319

CAS No.

1820934-93-7

GlyT1 Inhibitor 1

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

Cat. No.

A19557

CAS No.

949164-09-4

ALX-1393

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

Cat. No.

A19982

CAS No.

405225-21-0

NFPS

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.

Cat. No.

A20662

CAS No.

1000690-85-6

Tilapertin

Synonyms: AMG747

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

Cat. No.

A21779

CAS No.

1779796-27-8

LY2365109 hydrochloride

Synonyms: LY-2365109

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

Cat. No.

A67012

CAS No.

1421936-85-7

Iclepertin

Synonyms: BI-425809

Iclepertin is a selective and orally active inhibitor of glycine transporter 1 (GlyT1), demonstrating potent inhibition while showing no activity against GlyT2. This compound has significant implications in research related to Alzheimer’s disease and schizophrenia, as it modulates glycine levels in the central nervous system, potentially influencing neurotransmission and cognitive function. Its specificity makes it a valuable tool for investigating the therapeutic potential in various neuropsychiatric disorders.

Cat. No.

A67013

CAS No.

1007109-16-1

TASP0315003

TASP0315003 is a selective inhibitor of the glycine transporter 1 (GlyT1). By inhibiting GlyT1, TASP0315003 enhances NMDA receptor function through elevated synaptic glycine levels. This compound demonstrates potential in addressing cognitive dysfunction and negative symptoms associated with schizophrenia while minimizing adverse central nervous system effects. TASP0315003 is suitable for research applications in neurological diseases.

Cat. No.

A67014

CAS No.

571147-18-7

ALX-5407

Synonyms: (R)-NFPS

ALX-5407 (R)-NFPS is a selective, orally active inhibitor of the glycine transporter GlyT1, exhibiting an IC50 value of 3 nM. This compound plays a crucial role in the study of N-methyl-D-aspartate (NMDA) receptor function and has potential applications in schizophrenia research. Its targeted action on GlyT1 makes ALX-5407 a valuable tool for investigating synaptic transmission and the modulation of glutamatergic signaling pathways.

Cat. No.

A67017

CAS No.

200006-08-2

ALX-5407 hydrochloride

Synonyms: (R)-NFPS hydrochloride

ALX-5407 hydrochloride is a selective inhibitor of the glycine transporter GlyT1, exhibiting a potent IC50 value of 3 nM. This compound is particularly valuable in the study of N-methyl-D-aspartate receptor function and has potential applications in schizophrenia research. Its oral bioavailability allows for convenient administration in vivo, making it an important tool for exploring glycine modulation in neurological studies.

Cat. No.

A67018

CAS No.

495076-64-7

Org 25543 hydrochloride

Org 25543 hydrochloride is a selective and irreversible inhibitor of the glycine transporter 2 (GlyT2), exhibiting an IC50 of 16 nM. This compound demonstrates significant analgesic effects and has been shown to alleviate mechanical allodynia following partial sciatic nerve ligation in murine models. Org 25543 hydrochloride serves as a valuable tool for research focused on pain mechanisms and the modulation of glycinergic signaling.

Cat. No.

A67020

CAS No.

1173239-39-8

PF-03463275

PF-03463275 is a selective and competitive inhibitor of glycine transporter-1 (GlyT1) with a Ki of 11.6 nM. This centrally penetrant and orally available compound demonstrates potential for advancing research in schizophrenia by modulating glycine levels in the central nervous system. Its efficacy in targeting GlyT1 makes it a valuable tool for understanding the mechanisms underlying this neuropsychiatric disorder.

Cat. No.

A67021

CAS No.

615571-23-8

SSR504734

SSR504734 is a selective and reversible inhibitor of the glycine transporter 1 (GlyT1), demonstrating potent activity across human, rat, and mouse models with IC50 values of 18, 15, and 38 nM, respectively. This compound has been shown to exhibit anti-schizophrenia, anti-anxiety, and anti-depression effects, making it a valuable tool for research in neuropsychiatric conditions and related therapeutic studies.

Cat. No.

A67023

CAS No.

374886-51-8

ASP2535

ASP2535 is a selective inhibitor of the glycine transporter-1 (GlyT1), demonstrating potent activity and oral bioavailability. This compound effectively crosses the blood-brain barrier and has been shown to improve cognitive impairment in preclinical models of schizophrenia and Alzheimer's disease, making it valuable for neurological research and potential therapeutic development.

Cat. No.

A67024

CAS No.

868265-28-5

LY2365109

LY2365109 is a selective glycine transporter 1 (GlyT1) inhibitor, exhibiting an IC50 of 15.8 nM for glycine uptake in cells over-expressing human GlyT1a. This compound plays a critical role in modulating glycine signaling pathways, making it valuable for research in neuropharmacology and the study of psychiatric disorders. Its specificity and potency facilitate investigations into the therapeutic potential of GlyT1 inhibition in various neurological conditions.

Cat. No.

A67025

CAS No.

363628-88-0

Org 25543

Org 25543 is a selective inhibitor of glycine transporter 2 (GlyT2), known for its analgesic effects. This compound demonstrates potential efficacy in alleviating chronic pain in preclinical models, making it a valuable tool for exploring pain modulation mechanisms. Its specificity for GlyT2 positions it as an important reagent for research in neurobiology and pain management applications.

Cat. No.

A67027

CAS No.

722456-08-8

Org-24598 lithium

Org-24598 lithium is a selective inhibitor of glycine transporter 1 (GlyT-1), demonstrating significant binding affinity with a Ki value of 16.9 nM for [3H] CHIBIA-3007 in rat brain membranes. This compound is valuable for research focused on neurotransmission, synaptic modulation, and neuropharmacology, particularly in the context of disorders associated with aberrant glycine signaling. Org-24598 lithium can aid in the exploration of GlyT-1's role in various neurological conditions and potential therapeutic strategies.

Cat. No.

A67028

CAS No.

1236046-15-3

DCCCyB

DCCCyB is a selective GlyT1 inhibitor known for its oral bioavailability and potent action. This compound exhibits significant in vivo occupancy of GlyT1 transporters in rhesus monkeys, making it a valuable tool for studying the roles of GlyT1 in neurological processes. DCCCyB is applicable in research related to schizophrenia, depression, and other neuropsychiatric disorders, facilitating investigations into neurotransmitter transport mechanisms.

Cat. No.

A67030

CAS No.

372198-97-5

Org-24598

Org-24598 is a potent inhibitor of glycine transporter 1 (GlyT-1). It effectively inhibits the binding of [3H] CHIBIA-3007 to rat brain membranes, demonstrating a Ki value of 16.9 nM. This compound is valuable for investigating the role of GlyT-1 in neurological disorders and could aid in the development of therapeutics targeting glycine transport.

Cat. No.

A67033

CAS No.

742693-38-5

SSR504734 free base

SSR504734 free base is a selective and reversible inhibitor of the GlyT1 transporter, with high potency across human, rat, and mouse models (IC50 values of 18, 15, and 38 nM, respectively). This compound demonstrates significant anti-schizophrenia, anti-anxiety, and anti-depression effects, making it a valuable tool for research in psychiatric disorders. Its oral bioavailability allows for versatile applications in behavioral studies and pharmacological investigations.

Cat. No.

A67034

CAS No.

1173177-11-1

PF-03463275 hydrochloride

PF-03463275 hydrochloride is a selective and competitive inhibitor of GlyT1 (glycine transporter-1), exhibiting a Ki of 11.6 nM. This compound is centrally penetrant and orally available, making it a valuable tool for research on synaptic transmission and neuropharmacology. PF-03463275 hydrochloride holds potential for advancing studies related to schizophrenia and other psychiatric disorders.

Cat. No.

A67035

CAS No.

949588-40-3

Org 25935

Org 25935 is a potent and selective inhibitor of glycine transporter 1 (GlyT1), exhibiting an IC50 value of 100 nM. This compound has been shown to significantly reduce ethanol intake and preference in rat models without affecting water consumption. Org 25935 serves as a valuable tool for investigating the mechanisms underlying alcohol dependence and abuse.

Cat. No.

A67414

CAS No.

2240164-55-8

Oleoyl-D-lysine

Oleoyl-D-lysine is a lipid-based selective inhibitor of Glycine Transporter-2 (GlyT2). This compound demonstrates significant potential in reversing neuropathic pain in murine models, while also exhibiting antidrowsiness effects in chronic neuropathic pain conditions. Additionally, Oleoyl-D-lysine has been identified as a safe and effective treatment option, showing no signs of respiratory depression.