Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Stable Isotope
Tolbutamide-d9 is a deuterated form of Tolbutamide, which primarily targets ATP-sensitive potassium channels. As a first-generation sulfonylurea, it functions as an oral hypoglycemic agent, playing a critical role in glucose regulation. This stable isotope is valuable for metabolic research and isotopic tracing studies, facilitating investigations into pharmacokinetics and the mechanism of action of sulfonylureas. -
CFTR Inhibitor
BPO-27 racemate is a potent cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor, exhibiting an IC50 of 8 nM. This compound has been shown to effectively suppress CFTR activity, making it valuable for research aimed at understanding CFTR-related disorders. BPO-27 racemate can be utilized in studies investigating ion channel regulation and potential therapeutic interventions for cystic fibrosis. -
Stable Isotope
Omeprazole-d3 is a deuterium-labeled variant of Omeprazole, a widely used proton pump inhibitor (PPI) targeting gastric acid secretion. It demonstrates competitive inhibition of CYP2C19 with an inhibition constant (Ki) between 2 to 6 μM, and has been shown to inhibit the growth of both Gram-positive and Gram-negative bacteria. This stable isotope is particularly useful for pharmacokinetic studies, metabolic profiling, and investigations into drug-drug interactions involving Omeprazole. -
Stable Isotope
Omeprazole-13C,d3 is a stable isotope-labeled form of Omeprazole, a proton pump inhibitor (PPI) that targets gastric acid secretion. This compound is utilized in pharmacokinetic studies due to its competitive inhibition of CYP2C19 activity, with an inhibition constant (Ki) ranging from 2 to 6 μM. Additionally, Omeprazole exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria and acts as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome release. It is a valuable reagent for research in gastrointestinal physiology, drug metabolism, and cellular signaling pathways. -
CFTR Corrector
Tezacaftor-d4 is a deuterium-labeled CFTR corrector that targets the F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) protein. By facilitating the proper trafficking of CFTR to the cell surface, Tezacaftor-d4 enhances functional chloride transport in epithelial cells. This compound is primarily utilized in research focused on developing therapeutic strategies for cystic fibrosis by restoring CFTR activity. -
Stable Isotope
Reserpine-d9 is a deuterated form of Reserpine that serves as an inhibitor of the vesicular monoamine transporter 2 (VMAT2). This stable isotope-labeled compound is valuable for studies in neuropharmacology and metabolism, allowing for precise tracking and quantification of Reserpine interactions in various biological systems. It enables researchers to explore its effects on neurotransmitter release and potential applications in psychiatric and neurological disorders. -
Autophagy Inducer
Desethylamiodarone hydrochloride is a significant active metabolite of Amiodarone, primarily functioning as an autophagy inducer. It is produced through the action of CYP3A isoenzymes and plays a critical role in cellular processes affecting autophagy. This compound is utilized in research applications focusing on cardiovascular pharmacology and cellular stress responses, due to its influence on potassium channels and potential therapeutic implications in arrhythmias. -
Stable Isotope
Amiodarone-d4 hydrochloride is a deuterium-labeled derivative of the Class III antiarrhythmic agent, Amiodarone hydrochloride, which primarily targets the human ether-a-go-go-related gene (hERG) potassium channel with an IC50 of approximately 45 nM. This compound influences vital cellular processes, promoting fibroblast proliferation and myofibroblast differentiation through the activation of ERK1/2 and p38 MAPK signaling pathways. Amiodarone-d4 hydrochloride is an essential tool for research into supraventricular and ventricular arrhythmias, providing valuable insights into arrhythmia mechanisms and potential therapeutic strategies. -
Stable Isotope
Amiodarone-d10 hydrochloride is a deuterium-labeled derivative of Amiodarone. This compound acts primarily as an antiarrhythmic agent, exerting its effects through the inhibition of ATP-sensitive potassium channels, with an IC50 value of 19.1 μM. It is utilized in pharmacokinetic studies and research focused on cardiovascular diseases, providing insights into drug metabolism and action mechanisms. -
Histamine H1 Receptor/TRPV1 Inhibitor
Dexbrompheniramine is a dual inhibitor of the histamine H1 receptor and the TRPV1 receptor, enabling it to effectively cross the blood-brain barrier. It functions by blocking H1 receptor activity and inhibiting TRPV1-mediated calcium responses in a dose-dependent manner, including responses triggered by Capsaicin. Research indicates that Dexbrompheniramine, when combined with Cimetidine, can mitigate drinking behavior induced by histamine and sham feeding, while it alone does not induce thirst. This compound is valuable for investigating the pathophysiology of chronic cough and related disorders. -
Stable Isotope
Uridine 5'-monophosphate-13C9,15N2 dilithium is a stable isotope-labeled form of uridine 5'-monophosphate, incorporating both 13C and 15N isotopes. This compound acts as an orally active mitochondrial ATP-dependent potassium channel activator, demonstrating cardioprotective effects. Additionally, uridine 5'-monophosphate promotes the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, making it valuable for research in gut development and in studies related to gastrointestinal health. -
Stable Isotope
Rabeprazole-d3 sodium is a deuterium-labeled form of the second-generation proton pump inhibitor, Rabeprazole sodium, which irreversibly inhibits the gastric H+/K+-ATPase. This compound has been shown to induce apoptosis and acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 value of 0.3 μM. Rabeprazole-d3 sodium is utilized in research involving gastric ulcerations and gastroesophageal reflux disorders. -
Stable Isotope
Pantoprazole-d8 is a deuterium-labeled form of Pantoprazole, a potent proton pump inhibitor (PPI) that targets H+/K+-ATPase with an IC50 of 6.8 μM. This compound exhibits significant anti-secretory and anti-ulcer activities, enhancing gastric pH stability. Research applications include investigating the pharmacokinetics of Pantoprazole and its potential synergistic effects with other chemotherapeutic agents, such as Doxorubicin, in tumor growth modulation. -
TRPV1 Antagonist
DWP-05195 is a TRPV1 antagonist that inhibits pain signal transduction, providing research applications in pain management studies. Additionally, DWP-05195 induces endoplasmic reticulum (ER) stress-dependent apoptosis in human ovarian cancer cells, mediated by the ROS-p38-CHOP signaling pathway. This compound may be useful for investigating both nociceptive mechanisms and potential therapeutic strategies for ovarian cancer. -
Stable Isotope
Rabeprazole-13C,d3 is a deuterated form of Rabeprazole, a second-generation proton pump inhibitor (PPI) that irreversibly inhibits gastric H+/K+-ATPase. This compound is known to induce apoptosis and has been identified as an inhibitor of uridine nucleoside ribohydrolase (UNH) with an IC50 value of 0.3 μM. Rabeprazole-13C,d3 is utilized in research focused on gastric ulcerations and gastroesophageal reflux disease, facilitating the study of drug metabolism and action in biological systems. -
Stable Isotope
Pantoprazole-d3 is a deuterium-labeled form of Pantoprazole, a potent proton pump inhibitor (PPI) that selectively targets the H+/K+-ATPase enzyme, exhibiting an IC50 of 6.8 μM. This compound enhances gastric pH stability and demonstrates significant anti-secretory and anti-ulcer properties. It is utilized in research to study gastric acid secretion mechanisms and to investigate potential synergistic effects with chemotherapeutic agents, such as Doxorubicin, in cancer treatment. -
Estrogen Receptor Agonist, Voltage-Gated Sodium Channel Blocker, PI3K-AKT/JNK Signaling Modulator,
Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury. -
Antiarrhythmic Agent
Quinidine sulfate is an antiarrhythmic agent that primarily targets cardiac ion channels, particularly potassium channels. It exhibits potent K+ channel blocking activity with an IC50 of 19.9 μM and has been shown to induce apoptosis in various cell types. Additionally, quinidine sulfate is utilized in malaria research, making it valuable for studies related to both cardiovascular and infectious diseases. -
Antiarrhythmic Agent
Quinidine polygalacturonate is an antiarrhythmic agent that primarily targets potassium channels, exhibiting an IC50 of 19.9 μM. It also functions as a selective inhibitor of cytochrome P450db and has the capability to induce apoptosis. This compound is particularly useful in research focused on cardiac arrhythmias and malaria studies, making it a valuable reagent for pharmacological investigations. -
Vasodilator
KMUP-1 is a xanthine derivative that acts as a vasodilator through the inhibition of phosphodiesterase (PDE) and activation of soluble guanylyl cyclase (sGC). It stimulates the nitric oxide/sGC/cyclic GMP signaling pathway and facilitates the opening of potassium channels. Additionally, KMUP-1 has been shown to reduce ischemia-induced cardiomyocyte apoptosis. This compound is relevant for studies in cardiovascular health and anti-inflammatory research. -
P-glycoprotein Inhibitor
P-gp inhibitor 22 is a potent inhibitor of P-glycoprotein (P-gp), effectively blocking its efflux function. This compound has been shown to induce apoptosis and promote the accumulation of MCF-7/ADR cells in the S phase of the cell cycle. Its ability to inhibit P-gp makes it relevant in studies focused on multidrug resistance and cancer therapeutics. -
Potassium Channel Inhibitor
DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation. -
Sodium Channel Inhibitor
Articaine is a selective inhibitor of voltage-gated sodium channels, including rNav1.4, hNav1.7, and rNav1.8, demonstrating an IC50 of 15.8 μM for open-state Na+ channels. It effectively blocks Na+ influx, leading to local anesthetic effects and interruption of nerve impulse conduction. Additionally, Articaine exhibits anti-inflammatory properties by inhibiting NF-κB activation and the NLRP3 inflammasome pathway. This compound is valuable for research in dental anesthesia and inflammatory-related conditions, such as acute kidney injury. -
CO Donor
Tricarbonyldichlororuthenium(II) dimer serves as a carbon monoxide (CO) donor, facilitating various biological processes. This compound demonstrates notable anti-inflammatory and antioxidant properties, in addition to its protective effects on gastric mucosa. Furthermore, Tricarbonyldichlororuthenium(II) dimer exhibits CO-independent effects on several potassium channels, highlighting its significance in cellular physiology and potential therapeutic applications. -
NAAA Inhibitor
AM9053 is a selective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) with an IC50 of 30 nM. It shows limited impact on FAAH activity (IC50 > 100 nM). AM9053 demonstrates significant anti-proliferative effects on colorectal cancer cells through the activation of PPAR-α and TRPV1-dependent pathways, leading to S-phase cell cycle arrest. Additionally, it alleviates intestinal fibrosis by modulating macrophage activity and inhibiting the IL-23 signaling pathway, resulting in increased levels of N-acylethanolamines, particularly palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). AM9053 is valuable for research into colorectal cancer and intestinal fibrosis. -
ABCG2/BCRP Inhibitor
Triclabendazole sulfoxide is an ABCG2/BCRP inhibitor that serves as the primary plasma metabolite of Triclabendazole. This compound demonstrates significant anti-parasitic activity and is useful in research applications focusing on the modulation of drug transport mechanisms in cellular assays. It contributes to studies investigating the role of ABCG2/BCRP in drug resistance and pharmacokinetics. -
Mycotoxin
Roquefortine C is a mycotoxin derived from Penicillium species, exhibiting multiple biological activities. As an agonist of P-glycoprotein (P-gp), it inhibits cytochrome P450 enzymes, specifically P450 3A and P450 1A. This compound demonstrates antimicrobial effects against Gram-positive bacteria and possesses neurotoxic properties, along with potential antitumor activity. Roquefortine C serves as a valuable tool in research exploring microbial interactions and pharmacological mechanisms. -
HSP70 ATPase Inhibitor
Displurigen (NSC375009) is an HSP70 ATPase inhibitor that specifically targets HSPA8, disrupting the pluripotency of human embryonic stem cells. This compound effectively inhibits the ATPase activity of HSP70 with an IC50 of 225 μM, making it a valuable tool for research in stem cell biology and differentiation processes. Its mechanism of action provides insights into cellular signaling pathways related to stem cell maintenance and development. -
ASH ATPase Activity Inhibitor
SEW84 is a potent inhibitor of Aha1-stimulated Hsp90 (ASH) ATPase activity, demonstrating an IC50 of 0.3 μM. This compound is valuable for investigating the role of Hsp90 in protein deposition disorders and offers insights into the underlying mechanisms of these diseases. Additionally, SEW84 may serve as a tool for studying Hsp90's involvement in cellular stress responses and protein folding pathways. -
CFTR
H2-Gamendazole, a derivative of Lonidamine, targets the cystic fibrosis transmembrane conductance regulator (CFTR). It demonstrates significant efficacy in reducing cyst formation in polycystic kidney disease models. This compound is primarily used in research related to autosomal dominant polycystic kidney disease, contributing to a better understanding of therapeutic strategies for this condition. -
Calcium Channel Antagonist
Benidipine is a potent orally active calcium channel antagonist. It exhibits anti-apoptotic effects in ischemic/reperfused myocardial cells and enhances the activity of endothelial cell-type nitric oxide synthase. Additionally, Benidipine has been shown to improve coronary circulation in hypertensive rat models, making it valuable for research on cardiovascular health and related disorders. -
P-gp Inhibitor
RMS3 is a tetrandrine analogue that functions as a potent inhibitor of P-glycoprotein (P-gp). This compound exhibits significant antiproliferative and cytotoxic effects on various cancer cell lines. Notably, RMS3 induces PARP cleavage, which is indicative of cells undergoing apoptosis. Its strong anticancer properties make RMS3 a valuable tool for cancer research and therapeutic studies. -
P-gp Inhibitor
RMS5 is a potent P-glycoprotein (P-gp) inhibitor, derived from a tetrandrine analogue. It exhibits significant antiproliferative and cytotoxic effects on cancer cells, contributing to its strong anticancer properties. Additionally, RMS5 has been observed to reduce the expression of anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1 while inducing PARP cleavage, a hallmark of apoptosis. This compound is valuable for research applications focusing on cancer therapeutics and the modulation of multidrug resistance. -
Stable Isotope
Capsaicin-d3 is a deuterated form of Capsaicin, a well-known TRPV1 agonist derived from chili peppers. This stable isotope allows for precise tracking and analysis in various research applications. Capsaicin-d3 has been implicated in studies exploring analgesic effects for neurological disorders, as well as its potential antioxidant, anti-inflammatory, and anti-cancer properties. Its use in research facilitates a better understanding of pain pathways and the therapeutic potential of capsaicin-related compounds. -
Stable Isotope
Pantoprazole-d6 is a deuterated form of Pantoprazole, a potent proton pump inhibitor (PPI) targeting H+/K+-ATPase with an IC50 of 6.8 μM. This stable isotope is primarily utilized in pharmacokinetic studies and metabolic investigations. Pantoprazole exhibits significant anti-secretory and anti-ulcer activities, enhancing pH stability while demonstrating the potential to improve tumor growth delay when combined with Doxorubicin. -
Antiarrhythmic Agent
Quinidine gluconic acid is an antiarrhythmic agent primarily targeting potassium channels, exhibiting an IC50 of 19.9 μM. This compound is a potent, orally active inhibitor of cytochrome P450 enzymes and has been shown to induce apoptosis in certain cell types. Quinidine gluconic acid is utilized in research related to cardiac arrhythmias as well as malaria studies, providing valuable insights into these complex biological processes. -
P-gp Inhibitor
(R)-OY-101 is an orally active and selective inhibitor of P-glycoprotein (P-gp). This compound enhances the sensitivity of tumors to anticancer agents by reversing drug resistance and promoting apoptosis. It has valuable applications in cancer research, particularly in studies focused on overcoming multidrug resistance and improving therapeutic efficacy. -
Na+/K+ ATPase Activator
Oleic acid sodium, also known as sodium oleate, is a sodium salt of the monounsaturated fatty acid oleic acid. It functions as an activator of Na+/K+ ATPase, which is essential for maintaining ion gradients across cell membranes. This compound has significant implications in various biological research applications, particularly in studies involving membrane function and cellular signaling pathways.
