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Catalog No.
Product Name
Application
Product Information
Citations
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Proton Pump inhibitor
Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition. -
BCRP inhibitor
(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter. -
TRPC3 inhibitor
Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.- Keisuke Obara, .et al. , Biol Pharm Bull, 2025, 48(6):932-940 PMID: 40582844
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KCC2 inhibitor
VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). -
gastric H+/K+-ATPase inhibitor
Tegoprazan, a potassium-competitive acid blocker, is a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro. -
Calcium Channel Inhibitor
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. -
IBAT inhibitor
Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ?? 0.17 nM, 0.13 ?? 0.03 nM, and 5.8 ?? 1.6 nM for human IBAT, mouse IBAT, and canine IBAT. -
nuclear export receptor CRM1 inhibitor
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle. -
dual NE/DA transporter inhibitor
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively. -
calcium channel inhibitor
Bay-K-8644 (R)-(+)- is a calcium channel inhibitor. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM). -
P-glycoprotein inhibitor
Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. -
Serotonin reuptake inhibitor (SSRI)
Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM. -
H+/K+-ATPase inhibitor
Picoprazole is a specific inhibitor of H+/K+-ATPase with IC50 of 3.1??0.4 μM. -
HCN channels inhibitor
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 ?M. -
TRPP3 channel inhibitor
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis. -
P-glycoprotein inhibitor
Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor. -
BCRP inhibitor
YHO-13351 (free base) is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP. -
SGLT2 inhibitor
Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6. -
triple reuptake inhibitor
Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively. -
Nav1.7 sodium channel inhibitor
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor. -
HCN channels inhibitor
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 ?M. -
triple reuptake inhibitor
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively. -
CRM1 inhibitor
Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor. -
Na+/H+ exchange inhibitor
Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Na+/H+ exchange inhibitor. -
sphingomyelin synthase inhibitor
Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors. -
SGLT1 inhibitor
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. -
CRAC inhibitor
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. -
inhibitor of Kv2.1 and Kv2.2
RY785 (Kv2-IN-A1) is an inhibitor of Kv2.1 and Kv2.2. -
glutamine transporter ASCT2 inhibitor
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor.
