| Cat. No. |
Product Name |
CAS No. |
Information |
| H9477 |
Iclepertin
|
1421936-85-7 |
Iclepertin(BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor;BI-425809 is inactive against GlyT2. BI 425809 inhibits GlyT1 with the IC50 values of 5.2 nM in rat primary neurons and 5.0 nM in human SK-N-MC cells. |
| H4448 |
TASP0315003
|
1007109-16-1 |
A potent, selective, orally available GlyT1 inhibitor with IC50 of 1.6 nM, weakly inhibits rat GlyT2 (IC50=138 nM); shows no activities at 107 other receptors, transporters, and ion channels, including NMDA, dopamine, serotonin and opioid receptors; significantly improves MK-801 impaired cognition, and also enhanced social memory in rats, reduces social interaction induced by repeated phencyclidine (PCP) in mice; also exhibits an antidepressant effect in rats, does not cause sedation or motor dysfunction. |
| H4447 |
PF0346275
|
1173239-39-8 |
A potent, selective, orally available GlyT1 inhibitor with Ki of 11.6 nM, without activity against GlyT2 (IC50>10 uM); demonstrates potent activity in elevating CSF levels of glycine in vivo (ED200, 3.5 mg/kg). |
| H4446 |
PF-03463275
|
1173177-11-1 |
PF-03463275 (PF 3463275) ia an orally bioavailable, centrally penetrant, potent, reversible, selective, and competitive inhibitor of the human GlyT1 transporter with Ki of 13 nM; shows no significant affinity for GlyT2 (Ki >1 mM); is under investigation for the treatment of schizophrenia. |
| H4445 |
Org 25935
|
949588-40-3 |
A potent, selective glycine transporter 1 (GlyT1) inhibitor with IC50 of 100 nM; shows negligible action on GlyT2; produces a robust and dose-dependent decrease in EtOH consumption in rats, reduces compulsive relapse-like drinking without the development of tolerance. |
| H4444 |
Org 25543
|
495076-64-7 |
A potent, highly selective glycine transporter 1 (GlyT2) inhibitor with IC50 of 16 nM with negligible affinity for GlyT1. |
| H4443 |
Opiranserin
|
1441000-45-8 |
Opiranserin (VVZ-149, VVZ-000149) is a?potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM); demonstrates analgesic efficacy for postoperative pain. |
| H4442 |
NFPS
|
405225-21-0 |
NFPS (ALX-5407) is a potent, selective GlyT1 inhibitor with IC50 of 2.8 and 9.8 nM for hGlyT1 and rGlyT1 respectively, >5,000-fold selectivity over rGlyT2; inhibits glycine transport by the GlyT1a, b and c subtypes of glycine transporters, but has no effect on the GLYT2a subtype of transporter; reverses PCP-induced changes in EEG power spectra in conscious rats (1-10 mg/kg i.p.), significantly enhances long-term potentiation in the hippocampal dentate gyrus in vivo. |
| H4441 |
LY-2365109 hydrochloride
|
1779796-27-8 |
A potent and selective GlyT1 inhibitor with IC50 of 15.8 nM, displays no activity for GlyT2 (IC50>30 uM); increases cerebrospinal fluid levels of glycine and potentiates NMDA-induced increases in dialysate levels of neurotransmitters in the prefrontal cortex (PFC) and the striatum. |
| H4440 |
GSK 494581A
|
909416-67-7 |
A potent, specific and mixed glycine transporter subtype 1 (GlyT1) inhibitor (pIC50=7.7) and GPR55 agonist (pEC50=6.5); shows no activity across a set of more than 200 validated molecular target assays from diverse classes, including kinases, proteases and other enzymes, GPCRs. |
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