Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
TRPM2 Activator
Adenosine 5′-diphosphoribose sodium is a potent activator of the TRPM2 cation channel, which is permeable to Ca2+. This NAD+ metabolite plays a crucial role in cellular signaling and has been shown to enhance autophagy. It serves as a valuable tool for research investigating calcium signaling pathways and the modulation of autophagy in various biological contexts. -
TRPML1/3 Inhibitor
(rel)-ML-SI3 is a selective inhibitor of TRPML1 and TRPML3, exhibiting IC50 values of 3.1 μM and 28.5 μM, respectively. In contrast, it acts as a potent activator of TRPML2 with an EC50 of 3.3 μM. This compound is valuable for research into the roles of TRPML channels in cellular processes and potential therapeutic interventions in related pathologies. Its specificity for multiple isoforms contributes to its utility in exploring calcium signaling pathways and lysosomal function. -
Antidiabetic Agent
4-Hydroxytolbutamide is a metabolite of Tolbutamide and acts primarily as an antidiabetic agent. It is involved in glucose metabolism by functioning as a potassium channel blocker, influencing insulin secretion from pancreatic beta-cells. This compound is particularly relevant in diabetes research, where it is used to study the pharmacodynamics and pharmacokinetics of sulfonylurea derivatives. Additionally, its metabolism by CYP2C8 and CYP2C9 contributes to understanding drug interactions in antidiabetic therapies. -
L-type Calcium Channel Blocker
Fendiline is an L-type calcium channel blocker that exhibits an IC50 of 17 µM. In addition to its role in cardiovascular modulation, Fendiline acts as a selective inhibitor of K-Ras, with an IC50 of 9.64 μM, effectively preventing K-Ras plasma membrane localization and blocking downstream signaling. This compound has demonstrated potential in inhibiting the proliferation of various cancer cell lines such as pancreatic, colon, lung, and endometrial cancers that express oncogenic mutant K-Ras. Furthermore, Fendiline serves as a STING agonist, showing promise in inhibiting the growth of refractory cold tumors, including MC38, CT26, and B16F10. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine dihydrochloride is a potent antimicrobial agent that acts primarily by intercalating into bacterial DNA, disrupting replication and transcription, and leading to bacterial cell lysis. Additionally, it serves as a Kir3.2 potassium channel blocker, making it a valuable tool for investigating neurological conditions such as Down syndrome. Furthermore, due to its ability to penetrate skin layers and accumulate in the cell nucleus, long-term exposure requires careful handling due to potential carcinogenic effects. This reagent is applicable in studies concerning microbial resistance and neurological phenotype exploration. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine sulfate functions primarily as an anti-microbial agent and a Kir3.2 potassium channel blocker. This acridine compound exhibits broad-spectrum antibacterial activity by intercalating into bacterial DNA, disrupting replication and transcription, ultimately leading to cell lysis. Additionally, it is utilized in neurological research, particularly in studying the phenotype associated with Down syndrome. Notably, 3,6-Diaminoacridine sulfate exhibits the capability to penetrate the skin's stratum corneum and accumulate in the cell nucleus, with prolonged exposure possibly linked to carcinogenic effects. -
Aortic Vasodilator
KMUP-4, a xanthine derivative, primarily acts as an aortic vasodilator by enhancing cyclic guanosine monophosphate (cGMP) levels. It promotes aortic relaxation through both endothelium-dependent and independent pathways by inhibiting phosphodiesterases (PDEs) and activating potassium channels, which also increases cyclic adenosine monophosphate (cAMP). KMUP-4 is a valuable reagent for research on cardiovascular diseases, providing insights into vascular relaxation mechanisms and potential therapeutic targets. -
PDE4 Inhibitor
L-869298 is a potent and selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 value of 0.5 nM for the PDE4A isoform. This compound exhibits minimal activity against the hERG potassium channel, making it a valuable tool for studies focused on inflammation, neurodegeneration, and other PDE4-related pathways. Its specificity and efficacy make it a suitable candidate for research applications in therapeutic development targeting PDE4-mediated signaling. -
Potassium-competitive Acid Blocker
KFP-H008 is an orally active potassium-competitive acid blocker that targets H+-K+-ATPase to inhibit gastric acid secretion. This compound has shown efficacy in reducing ethanol-induced gastric ulcer index and decreasing malonaldehyde levels, along with the expression of pro-inflammatory cytokines in vivo. KFP-H008 also downregulates p-p38 MAPK and p65 NF-κB expression, demonstrating its potential in mitigating gastric inflammation. This reagent is valuable for research into acid-related diseases, including gastric ulcers and gastric epithelial cell damage. -
Anti-Adipogenesic Agent
Petasin is an anti-adipogenesic agent that effectively inhibits adipogenesis in 3T3-F442A cells with an IC50 of 0.95 μM. It achieves this by suppressing the expression of lipid synthesis factors such as ACC1, FAS, and SCD1 through the inhibition of transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels. Additionally, Petasin inhibits mitochondrial complex I, contributing to reduced tumor growth and metastasis. By activating the AMPK signaling pathway, it plays a significant role in the regulation of glucose and lipid metabolism. Petasin is also noted for its oral bioactivity. -
BRG1/BRM ATPase Inhibitor
BRM/BRG1 ATP Inhibitor-2 is a selective inhibitor of BRG1 and BRM ATPase activity, targeting the SWI/SNF chromatin remodeling complexes. This compound is valuable for investigating the molecular implications of BAF-related disorders, including cancer and developmental syndromes. Its mechanism of action enables researchers to explore the role of ATP-dependent chromatin remodeling in gene expression regulation and cellular differentiation. -
SMARCA2 ATPase Inhibitor
SMARCA2-IN-10 is a selective inhibitor of the SMARCA2 ATPase domain, with an IC50 value of 17.676 μM. This compound has been shown to induce cell death in tumors lacking SMARCA4, making it a valuable tool for investigating SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma. Its targeting of the SMARCA2 ATPase offers significant potential for advancing research in these cancer types. -
Excited-state Intramolecular Proton Transfer Molecules
2-(2′-Hydroxyphenyl)benzimidazole is a well-characterized excited-state intramolecular proton transfer (ESIPT) molecule that demonstrates both normal and tautomer emissions. This compound serves as a valuable fluorescent probe, enabling researchers to explore various biological systems and molecular interactions. Its unique photophysical properties make it an essential tool in studies involving fluorescence spectroscopy and imaging applications. -
Potassium Fluorescent Indicator
Asante potassium green-2 (TMA) is a cell-impermeable potassium-sensitive fluorescent indicator with an excitation/emission spectrum of 525/545 nm. It selectively detects intracellular potassium ion concentrations, making it valuable for studies involving ion channel activity and cellular signaling. This reagent is essential for investigating potassium homeostasis and its implications in various physiological processes and pathologies. -
Potassium Fluorescent Indicator
Asante Potassium Green-1 (TMA) is a cell-impermeable fluorescent indicator designed to selectively detect potassium ions (K+) with an excitation wavelength of 525 nm and emission wavelength of 545 nm. This compound allows researchers to monitor intracellular potassium levels with high sensitivity and specificity, making it invaluable for studies involving ion transport, cellular signaling, and physiology. Its utility in real-time fluorescence imaging facilitates investigations into potassium's role in various biological processes and disease states. -
Potassium Fluorescent Indicator
Asante potassium green-1 AM is a cell-permeable potassium (K+) sensitive fluorescent indicator with an excitation/emission wavelength of 525/545 nm. This reagent enables the visualization and quantification of potassium ion fluctuations within live cells, making it suitable for studies in neurobiology, cardiac research, and cellular signaling. Its high sensitivity to K+ concentrations facilitates investigations into ion channel activity and cellular excitability, enhancing understanding of various physiological processes.
