Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
DPP8/9 Inhibitor
DPP8/9-IN-2 is a selective inhibitor of dipeptidyl peptidase 8 and 9 (DPP8/DPP9) with potent inhibitory activity, exhibiting IC50 values of 0.22 nM and 3 nM, respectively. This compound has been implicated in research related to tumor biology and other pathological conditions. Notably, DPP8/9-IN-2 demonstrates certain cardiotoxicity, indicated by its IC50 values of 0.7 μM for the hERG potassium channel, 29.0 μM for the Nav1.5 sodium channel, and 27.7 μM for the Cav1.2 calcium channel. -
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. -
TRPA1 Inhibitor
Aurothiomalate disodium acts as a TRPA1 inhibitor, effectively blocking NF-κB activation and inhibiting iNOS expression. This compound fosters the M2 transformation of macrophages and enhances the expression of TREM-2 and arginase-1. Aurothiomalate disodium is applicable in research concerning liver fibrosis, cirrhosis, and arthritis, providing insights into inflammation and tissue repair mechanisms. -
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. -
TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM. - Selamectin is a topical parasiticide and antihelminthic used on dogs and cats to treat and prevent infections of heartworms, fleas, ear mites, sarcoptic mange, and certain types of ticks in dogs as well as prevent heartworms, fleas, ear mites, hookworms, and roundworms in cats.
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non-ionic emulsifying agent
Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent. -
Calcium channel blocker
Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively. -
Calcium channel blocker
Mibefradil 2Hcl is calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 uM and 18.6 uM for T-type and L-type channels respectively. - N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.
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T-type Ca2+ channel blocker
ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker. -
CNT2 Inhibitor
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2. - Pinaverium Bromide is a spasmolytic agent with low incidence of anticholinergic effects. Pinaverium Bromide is also an antispasmodic.
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SGLT2 inhibitor
Tofogliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. -
TRPV1 antagonist
NJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1. -
SGLT1/SGLT2 inhibitor
Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor. -
Na+/H+-exchange inhibitor
FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively. -
K+ channel blocker?€?
E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). -
Na+/H+ exchange inhibitor
Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor. -
glutamate release inhibitor
Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke.
