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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. -
AMPA/kainate receptors agonist
(S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM. -
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. -
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. -
sodium channel blocker
Levobupivacaine hydrochloride is a sodium channel blocker. -
OPRM1/OPRD1 agonist
ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively. -
anticancer agent
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. -
anticancer agent
5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner. -
ATPase activator
Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase. -
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. - Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators.
- Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.
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Calcium channel antagonist
Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.
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potassium currents blocker
Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
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TRPM8 antagonist
M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively). -
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. -
Oct3/4 inducer
Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells. -
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. -
VMAT-2 inhibitor
Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2). -
Potassium Channel inhibitor
Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. -
VDAC Inhibitor
DIDS sodium salt is a potent inhibitor of voltage-dependent anion channels (VDAC1) and also targets the ABCA1 transporter. This compound effectively disrupts RAD51-mediated homologous pairing and strand exchange reactions, making it valuable for studying DNA repair mechanisms. Additionally, DIDS is known to inhibit anion exchange and interfere with caspase-3 and -9 activation, facilitating its application in cancer research and apoptosis studies. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
Serotonergic Receptor Antagonist
Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology. -
K+ Channels Activator
1-EBIO is an activator of Ca2+-sensitive K+ channels, playing a crucial role in the modulation of membrane potential and cellular excitability. This compound is utilized in research to investigate the physiological functions and pathophysiological roles of K+ channels, contributing to a deeper understanding of cellular signaling processes and potential therapeutic targets in various diseases.

