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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC73631 ZCAN155
ZCAN155 is a small molecule that prevents AMPA-mediated excitotoxicity (IC50=35 nM) by targeting an allosteric binding site of AMPA glutamate receptor 2 (GluA2), restores neurological function and myelination.
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DC73630 UBP792
UBP792 is a novel negative allosteric modulator (antagonist) of NMDA receptors, displays partial subtype-selectivity by having a varied maximal inhibition of GluN2A-, GluN2B-, GluN2C-, and GluN2D-containing receptors (52%, 70%, 87%, 89%, respectively) wit
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DC73629 UBP791
UBP791 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 80-90 nM, 50-fold selectivity over GluN2A and GluN2B.
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DC73628 UBP1700
UBP1700 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 7-9 nM, 50-fold selectivity over GluN2A and GluN2B.
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DC73627 PTC-174
PTC-174 is a selective, positive allosteric modulator of NMDA receptors containing GluN2C or GluN2D subunits with EC50 of 4.1 uM (GluN1/2C) and 5.7 uM (GluN1/2D).
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DC73626 Org 26576
Org 26576 (MK 8777.
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DC73625 GluN2A PAM (R)-9
GluN2A PAM (R)-9 is a potent, brain penetrant, GluN2A-selective positive allosteric modulator with EC50 of 0.51 uM, Emax 350%.
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DC73623 DQP-997-74
DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 0.35 and 0.13 uM, respectively, exhibits >100-fold over GluN2A- and GluN2B-containing receptors.
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DC73622 (S)-(-)-DQP-997-74
(S)-(-)-DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 69 and 35 nM, respectively, exhibits >100- and >300-fold over GluN2A- and GluN2B-containing receptors.
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DC73621 (R)-OF-NB1
(R)-OF-NB1 is a small molecule splice variant GluN2B-selective NMDAR antagonist with IC50 of 675 nM and 97 nM for F-NB1 for splice variant containing exon 5 and GluN1-1a in X. laevis oocytes.
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DC73620 RO-275
RO-275 is a potent, selective HCN1 ion channel inhibitor with IC50 of 46 nM, displays 311/100/302-fold selectivity over HCN2/HCN3/HCN4.
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DC73618 NUCC-0200590
NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo.
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DC73616 GTS511
GTS511 (GTS-511) is a potent, selective, brain-permeable activator of EAAT2 with EC50 of 3.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.
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DC73615 GTS467
GTS476 (GTS-476) is a potent, selective, orally active activator of EAAT2 with EC50 of 35.1 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.
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DC73614 GT951
GT951 (GT-951) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.
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DC73613 (R)-AS-1
(R)-AS-1 is an orally bioavailable, selective positive allosteric modulator (PAM) of the glutamate transporter EAAT2 with EC50 of 11 nM and Emax of 251%, shows potent antiseizure activity in vivo.
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DC73612 Glutipyran
Glutipyran is a small-molecule glucose transporter inhibitor, inhibits glycolytic activity and cell growth in human pancreatic cancer cells.
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DC73611 SGS742
CGP 36742 (SGS-742) is a BBB-penetrant GABAB receptor antagonist, discretely up-regulates GABAB receptor binding sites.
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DC73610 DS-II-73
DS-II-73 is a selective α2/3/5-containing GABAA receptor (GABAAR) potentiator with IC50 of 320 nM, 381 nM and 435 nM for α2β3γ2 α3β3γ2 α5β3γ2.
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DC73609 ASP8062
ASP8062 is a potent, selective GABA B receptor positive allosteric modulator (PAM), positive allosteric modulating activity for human and rat GABAB receptors, exerts analgesic effects in rat model of fibromyalgia.
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DC73606 VI-116
VI-116 is a potent and selective volume-regulated anion channel (VRAC) inhibitor, fully inhibits VRAC-mediated I- quenching with an IC50 of 1.27 uM in LN215 cells.
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DC73602 DRAinh-A270
DRAinh-A270 is a small-molecule, selective inhibitor of intestinal anion exchanger SLC26A3 (DRA), inhibits SLC26A3-mediated chloride/bicarbonate exchange with IC50 of 35 nM and oxalate/chloride exchange with IC50 of 60 nM.
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DC73601 TTA-Q6
TTA-Q6 is a potent, selective T-type Ca2+ channel antagonist with IC50 of 14 nM and 590 nM in FLIPR depolarized assaay and FLIPR hyperpolarized assay, respectively.
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DC73600 TMDJ-035
TMDJ-035 is the first highly potent and selective ryanodine receptor 2 (RyR2) inhibitor with EC50 of 13 nM, shows no effect on RyR1 and RyR3.
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DC73599 PST3093
PST3093 (PST 3093) is the main Istaroxime metabolite and a selective SERCA2a activator, reduces the SERCA2a KdCa value by about 20% at 100 nM.
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DC73597 Extracellular vesicle enhancer 634
Extracellular vesicle enhancer 634 (Compound 634) is a small molecule enhancer of extracellular vesicle (EV) release with immunostimulatory potency via induction of Ca2+ influx, which is mediated by store-operated Ca2+ entry (SOCE).
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DC73596 Efonidipine hydrochloride
Efonidipine (NZ-105) is a potent, dual T-type and L-type calcium channel blocker, exhibits antihypertensive effect through vasodilatation.
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DC73595 2D216
2D216 is a small molecule calcium channel activator, increases murine antigen-specific antibody responses when used as a co-adjuvant with LPS.
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DC73594 2E151
2E151 is a small molecule calcium channel activator, increases murine antigen-specific antibody responses when used as a co-adjuvant with LPS.
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DC73593 ML753286
ML753286 is a potent, selective BCRP inhibitor with IC50 of 0.6 uM (BCRP efflux transporter), shows no activity against P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP), or major cytochrome P450s (CYPs).
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