Catalog No.
Product Name
Application
Product Information
Citations
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Cardiac Na+ channel blocker
Flecainide is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential. -
Na+,K+-ATPase inhibitor
Istaroxime (PST2744) is a potent inhibitor of Na+,K+-ATPase with IC50 of 0.11 μM. -
CFTR potentiator
Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment. -
CFTR potentiator
Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment. - M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel. Antiviral agents.
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Calcium channel blocker
NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. -
Sodium Channel inhibitor
Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment. -
AMPA antagonist
Tezampanel is an antagonist at the AMPA and kainate families of ionotropic glutamate receptors, with selectivity for the GluR5 subtype of the kainate receptor. -
P-gp inhibitor
Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. -
Potassium channel blocker
Cesium chloride is a potassium channel blocker; inhibits the pacemaker current (If) and the hyperpolarization-activated cationic current (Ih). Prevents activation of caspase-3 and neuronal apoptosis in serum- and potassium-deprived cerebellar granule neurons by inactivating GSK-3β. -
Slows neuronal Na+ channel inactivation
beta-Pompilidotoxin is a peptide with the sequence H2N-Arg. -
glutamate receptors agonist
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
CaCCs Inhibitor
CaCCinh-A01 inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 uM, in TMEM16A-expressing FRT cells). -
TMEM16A Inhibitor
T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells. -
ATPase and GTPase inhibitor
Etidronate Disodium is a bisphosphonate bone resorption inhibitor. -
AMPA antagonist
YM90K hydrochloride is a selective AMPA receptor antagonist that delays neuronal death in a global ischemia model and cerebral infarction in a focal ischemia model following postischemic administration. - Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).
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TRPA1 activatior/TRPM8 blocker
Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility. -
AMPA/kainate receptor antagonist
Talampanel is a non-competitive antagonist of AMPA-receptor. - (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
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5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. -
Sodium Channel Inhibitor
Lamotrigine-13C3 is a stable isotope-labeled derivative of Lamotrigine, a highly effective sodium channel inhibitor. This compound selectively targets voltage-gated Na+ channels, leading to stabilization of presynaptic neuronal membranes and a subsequent reduction in glutamate release. Lamotrigine-13C3 is suitable for research applications related to epilepsy, focal seizures, and other neurological disorders. -
Stable Isotope
Omeprazole-d3-1 is a deuterium-labeled form of Omeprazole, a proton pump inhibitor (PPI) primarily targeting acid-related gastrointestinal disorders. This compound exhibits competitive inhibition of CYP2C19, with a Ki ranging from 2 to 6 μM, and has demonstrated antimicrobial effects against both Gram-positive and Gram-negative bacteria. Additionally, Omeprazole acts as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome production in cell studies. This stable isotope is a valuable tool for pharmacokinetic and metabolic research applications. -
Stable Isotope
Desethyl Amiodarone-d4 hydrochloride is a deuterium-labeled analog of Desethylamiodarone hydrochloride, a significant active metabolite of the antiarrhythmic drug Amiodarone. This compound predominantly arises from the metabolic activity of CYP3A isoenzymes. Desethylamiodarone hydrochloride demonstrates potent inhibition of ATP-sensitive potassium channels, with an IC50 value of 19.1 μM, making it a valuable tool for research in cardiac electrophysiology and drug metabolism studies. -
TRPML Modulator
TRPML modulator 1 is a selective modulator of the TRPML channel, known for its role in promoting autophagy. With an AC50 of less than 2 mM in the TFEB assay, it effectively enhances autophagic flux, making it a valuable tool for research applications focused on cellular degradation processes and lysosomal function. This compound is instrumental in studying the molecular mechanisms underlying autophagy-related diseases. -
Stable Isotope
Diazoxide-d3 is a deuterium-labeled derivative of Diazoxide, an ATP-sensitive potassium channel activator. This compound is primarily utilized in research to investigate insulin regulation and has potential applications in the treatment of hyperinsulinism. Its unique isotopic labeling allows for enhanced tracking and analysis in various biochemical studies. -
Stable Isotope
Omeprazole-d6 is a deuterium-labeled form of Omeprazole, a proton pump inhibitor (PPI) primarily targeting gastric acid secretion. It demonstrates competitive inhibition of CYP2C19 with an inhibition constant (Ki) ranging from 2 to 6 μM, making it a valuable tool in drug metabolism studies. In addition to its role in gastrointestinal health, Omeprazole exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria and serves as a potent inhibitor of neutral sphingomyelinase (N-SMase), thereby impacting exosome production and release. This stable isotope variant is useful for pharmacokinetic studies and tracing in biological research applications. -
ATX Inhibitor/PPARγ Agonist
EL244 is a dual inhibitor of Autotaxin (ATX), with an IC50 of 50 nM, and a selective agonist of PPARγ, exhibiting an IC50 of 1.3 μM. This compound shows low cytotoxicity in human HepG2 cells, with an EC50 of 81.2 μM, and minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 effectively reduces pulmonary Lysophosphatidic Acid (LPA) levels, mitigates fibrosis, and enhances respiratory function in vivo, making it a valuable tool for the study of idiopathic pulmonary fibrosis and interstitial lung disease (ILD). -
PPARγ/TRPA1 Receptor Partial Agonist
Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics. -
PPAR Agonist
20-HEPE is a metabolite of eicosapentaenoic acid that functions primarily as a peroxisome proliferator-activated receptor α (PPARα) agonist. At a concentration of 10 μM, it effectively activates PPARα in COS-7 cells that express a luciferase reporter gene. Additionally, 20-HEPE activates the mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro, although it does not exhibit analgesic effects in rat models. This compound has potential applications in the study of metabolic processes and receptor signaling pathways. -
Piezo1 Agonist
Piezo1 agonist 1-d2 is a selective agonist for the Piezo1 ion channel, exhibiting an EC50 of 2.21 μM. This compound activates Ca2+-dependent ERK signaling pathways, thereby facilitating the osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs). Additionally, Piezo1 agonist 1-d2 has demonstrated efficacy in ameliorating disuse osteoporosis in hindlimb-unloading rat models, making it a valuable tool for research in bone health and regenerative medicine. -
Inflammation Inhibitor
Resolvin D5 is an anti-inflammatory agent primarily targeting the GPR32 receptor, effectively modulating inflammation responses. It alleviates Paclitaxel-induced mechanical allodynia and inflammatory pain in male mice through mechanisms that do not involve TRPV1 or TRPA1 channels. Resolvin D5 reduces LPS-induced ERK phosphorylation and NF-κB nuclear translocation while downregulating pro-inflammatory mediators, inhibiting Th17 differentiation, and promoting regulatory T cell differentiation. This compound is particularly relevant for research on chemotherapy-induced peripheral neuropathy, inflammatory pain, and rheumatoid arthritis. -
Stable Isotope
Hydrochlorothiazid-d2 is the deuterated form of Hydrochlorothiazide, a thiazide diuretic known for its role in inhibiting the transforming growth factor-beta (TGF-β)/Smad signaling pathway. This compound exhibits direct vascular relaxation by activating calcium-activated potassium channels, contributing to its antihypertensive properties. Hydrochlorothiazid-d2 is valuable in research applications involving the study of cardiovascular function, fibrosis reduction, and the overall effects of diuretics on systemic blood pressure regulation. -
Stable Isotope
Hydrochlorothiazid-13C,d2 is a stable isotope-labeled form of Hydrochlorothiazide (HCTZ), a thiazide diuretic that functions by inhibiting the TGF-β/Smad signaling pathway. This compound exhibits direct vascular relaxant effects through the activation of calcium-activated potassium channels. Hydrochlorothiazide is primarily utilized in research to improve cardiac function, reduce fibrosis, and exhibit antihypertensive properties, making it a valuable tool for studies on cardiovascular health and hypertension management. -
Stable Isotope
Hydrochlorothiazide-15N2,13C,d2 is a stable isotope-labeled derivative of hydrochlorothiazide, incorporating 15N and deuterium for enhanced tracking in metabolic studies. As a thiazide diuretic, hydrochlorothiazide inhibits the TGF-β/Smad signaling pathway, which plays a crucial role in cardiovascular remodeling. This compound exhibits direct vascular relaxation by activating calcium-activated potassium channels, thereby improving cardiac function, reducing fibrosis, and delivering antihypertensive effects. It is ideal for research applications focusing on cardiovascular health and the mechanisms of diuretic therapy. -
Kir2.1 Agonist
Tetramisole acts as a selective agonist for the inward rectifier potassium channel Kir2.1, displaying an EC50 of approximately 30 μM. This compound enhances the forward transport of Kir2.1 channels, hyperpolarizing the resting potential and shortening action potential duration, while also inhibiting intracellular calcium overload and PKA signaling. Additionally, Tetramisole exhibits anti-arrhythmic and anti-myocardial remodeling properties. It is valuable in cardiac electrophysiology studies and investigations focused on myocardial ischemia and heart failure. -
NF-κB Inhibitor/TRP Modulator
Cannabitwinol is a selective NF-κB inhibitor and thermosensitive TRP modulator. It effectively inhibits TNFα-induced NF-κB-driven transcription and IL-8 release, exhibiting notable anti-inflammatory and antioxidant properties. Cannabitwinol selectively activates cold-activated TRP channels, such as TRPA1 (EC50 = 3.0 μM), while antagonizing TRPM8 (IC50 = 3.9 μM), with minimal interaction with heat-activated TRP channels like TRPV1 and TRPV2. This compound is applicable in research focused on inflammatory skin diseases, cold allodynia, and hyperalgesia. -
TRPA1 Agonist
Methyl syringate is a selective agonist of the TRPA1 receptor, playing a crucial role in the regulation of food intake and gastric emptying through TRPA1-mediated pathways. Additionally, this compound functions as an effective phenolic mediator for bacterial and fungal laccases, enhancing their catalytic activities. Methyl syringate serves as a chemical marker in Asphodel monofloral honey and is associated with its antibacterial properties. Furthermore, it has been shown to inhibit aflatoxin production and may contribute to weight suppression, as well as being applicable in research focused on cancer prevention, hypoxia-induced inflammatory response, and tumorigenesis. -
ecto-ATPase Inhibitor
ARL67156 is an inhibitor of ecto-ATPase, specifically targeting NTPDase1 (CD39), NTPDase3, and NPP1. It exhibits weak competitive inhibition with Ki values of 11 µM, 18 µM, and 12 µM for these enzymes, respectively. This compound is useful for studies investigating purinergic signaling and ATP metabolism in various biological contexts, including cell signaling and immune response research. -
Piezo1 Agonist
MCB-22-174 is a deuterated agonist of the Piezo1 mechanosensitive ion channel, exhibiting an EC50 of 6.28 μM. This compound effectively activates the CaMKII/ERK signaling pathway and promotes calcium influx in rat mesenchymal stem cells (rMSCs). MCB-22-174 reduces the expression of chondrogenic markers, such as Comp and Acan, alongside adipogenic markers including Lpl and Fabp4. This reagent has potential applications in enhancing bone quality in models of disuse osteoporosis, making it a valuable tool for research in skeletal health and regenerative medicine. -
NMDAR/TRPM4 Inhibitor
Brophenexin free base is a potent inhibitor targeting the N-methyl-D-aspartate receptor (NMDAR) and the transient receptor potential melastatin 4 (TRPM4). This compound exhibits significant neuroprotective activity, preventing NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Furthermore, Brophenexin free base has demonstrated protective effects in vivo, safeguarding against brain damage induced by middle cerebral artery occlusion (MCAO) and preserving retinal ganglion cells from NMDA-induced loss. -
CFTR Modulator
Olacaftor is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator that enhances the function of the defective CFTR protein. It has been shown to improve chloride ion transport, leading to increased hydration of airway surfaces and improved pulmonary function. Olacaftor is primarily utilized in research focused on cystic fibrosis and the development of therapies aimed at restoring CFTR activity.
