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Catalog No.
Product Name
Application
Product Information
Product Citation
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TRPV4 antagonist
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4. -
serotonin-norepinephrine reuptake inhibitor
Nitroxazepine is a tricyclic antidepressant (TCA) for the treatment of depression. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor. -
Kv7 (KCNQ) channels blocker
XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 ?M, 0.71 ?M, 0.6 μM, and 0.98 ?M, respectively. -
SOCE inhibitor
SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM. -
Pgp modulator
P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR). -
potassium channel blocker
Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K+ current. -
AMPAR negative modulator
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. -
TRPV4 ion channel blocker
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. -
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. -
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. -
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. -
AMPA receptor positive allosteric modulator
PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models. -
Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.
- Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
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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. -
AMPA receptors potentiator
Mibampator (LY451395) is a potent and highly selective potentiator of the AMPA receptors. -
L-type calcium antagonist
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors. -
Na+ channel blocker
Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain. -
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. -
CRAC inhibitor
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. -
TRPV1 antagonist and TNF-alpha production inhibitor
LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor. -
blocker of fast Na+-dependent action potentials and voltage-dependent
Lidocaine N-ethyl bromide is a non-membrane-permeable blocker of fast Na+-dependent action potentials and voltage-dependent, non-inactivating Na+ conductance. -
CRM1-selective inhibitor
Selinexor trans-isomer is a trans-isomer of Selinexor or KPT-330, which is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells.
