Catalog No.
Product Name
Application
Product Information
Citations
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Parasite Inhibitor
Ep vinyl quinidine, an epi-vinyl stereoisomer of Quinidine, serves as a targeted inhibitor of parasitic activity. This compound exhibits significant potential in malaria research, leveraging its capabilities as a selective cytochrome P450db inhibitor. Additionally, it functions as a potassium channel blocker with an IC50 of 19.9 μM, positioning it as a valuable tool for investigating anti-parasitic mechanisms and therapeutic interventions. -
HCV Inhibitor
Vedroprevir is a potent inhibitor of the HCV NS3/4A protease, demonstrating an IC50 of 3.2 nM. In addition to its antiviral activity, Vedroprevir also inhibits the breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM, as well as P-glycoprotein (P-gp), MRP1, and MRP2 with IC50 values of 34 μM, 14.9 μM, and 12 μM, respectively. These characteristics make Vedroprevir valuable for research in hepatitis C and multidrug resistance cancer studies. Its favorable pharmacokinetic profile has been observed in preclinical models, including rats and dogs. -
V-ATPase/HIV-1 Inhibitor
Diphyllin is a potent inhibitor of vacuolar H+-ATPase (V-ATPase) with an IC50 of 17 nM, and also acts as an HIV-1 inhibitor with an IC50 of 0.38 μM. This compound effectively disrupts the acidification of osteoclast lysosomes, leading to significant inhibition of osteoclast-mediated bone resorption while leaving osteoblastic bone formation unaffected. Diphyllin is valuable for investigating bone metabolism-related diseases and exploring therapeutic avenues for conditions characterized by excessive bone resorption. -
Stable Isotope
Atazanavir-d5 is a deuterium-labeled derivative of Atazanavir, a highly selective inhibitor of HIV-1 protease. This compound serves as a substrate and inhibitor of the cytochrome P450 enzyme CYP3A4, as well as an inhibitor and inducer of P-glycoprotein (P-gp). Additionally, Atazanavir exhibits activity against SARS-CoV 3CLpro with an IC50 of 3.49 μM, making it valuable for research into HIV and coronavirus-related mechanisms. -
AMPAR Modulator
Nooglutil is a positive modulator of AMPA-type glutamate receptors (AMPARs), enhancing synaptic transmission and plasticity. Additionally, it regulates dopamine D2 receptor function, contributing to its anxiolytic effects. This compound is of significant interest for research into neurodegenerative disorders, including Alzheimer's disease, and offers potential insights into therapeutic strategies targeting glutamatergic and dopaminergic systems. -
Dopamine Receptor Inhibitor
Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia. -
Calcium Entry-Blocking
YM-430 is a calcium entry-blocking and beta-adrenoceptor-blocking agent. It effectively inhibits Amifampridine-induced rhythmic contractions with an IC50 value of 59.2 nM and blocks arginine vasopressin-induced ST-segment depression with an IC50 of 36.6 mg/kg. This compound is valuable for research into angina pectoris and related cardiovascular conditions. -
CB1 and TRPV1 agonist
N-Arachidonyldopamine is a selective agonist of the CB1 and TRPV1 receptors, exhibiting a Ki value of 250 nM for the CB1 receptor and an EC50 of approximately 50 nM for TRPV1. This compound plays a significant role in modulating pain and inflammatory responses, making it a valuable tool for research investigating endocannabinoid signaling pathways and their implications in various physiological processes. -
CB1 Agonist
(R)-Methanandamide is a potent CB1 receptor agonist, exhibiting a Ki value of 20 nM. This compound serves as an analytical tool for studying cannabinoid signaling pathways and the endocannabinoid system. Additionally, (R)-Methanandamide can activate vanilloid (TRPV1) receptors, highlighting its potential applications in pain research and modulation of inflammatory processes in cellular assays. -
VR1/CB1 Agonist
OMDM-6 is a hybrid agonist targeting vanilloid receptor type 1 (VR1, TRPV1) with an EC50 of 75 nM and cannabinoid receptor type 1 (CB1) with a Ki of 3.2 μM. This compound also inhibits the cellular uptake of anandamide, demonstrating a Ki of 7.0 μM. Due to its dual mechanism of action, OMDM-6 is valuable for research applications exploring pain modulation and the endocannabinoid system. -
Cannabinoid Receptor
CB2 receptor antagonist 1 is a selective competitive antagonist of the cannabinoid receptor CB2, exhibiting strong potency. This hexyl resorcinol derivative not only effectively inhibits CB2 receptor activity but also demonstrates significant antinociceptive properties. Additionally, it has been observed to activate both cannabinoid and TRPV1 receptors, making it a valuable tool for research in pain modulation and cannabinoid signaling pathways. -
CB1 Agonist
CB1/2 agonist 4 serves as a full agonist for the CB1 receptor and a partial agonist for the CB2 receptor, exhibiting EC50 values of 15.09 nM and 1.16 nM, respectively. It demonstrates high affinity for human CB1 and CB2 receptors, with Ki values of 1.1 nM and 4.2 nM. This compound displays notable antinociceptive activity and effectively activates both cannabinoid and TRPV1 receptors, featuring IC50 and EC50 values of 0.8 μM and 0.12 μM, respectively. CB1/2 agonist 4 is valuable for studies exploring cannabinoid receptor functions and their implications in pain modulation. -
CB1/2 Agonist
AB-FUBICA is a potent agonist for CB1 and CB2 receptors, serving as a valuable tool in cannabinoid research. It functions by activating G-protein coupled inwardly rectifying potassium channels (GIRK) through its binding to these receptors, demonstrating significant cannabinoid-like activity. With EC50 values of 21 nM for CB1 and 15 nM for CB2, AB-FUBICA is ideal for investigating pain management, neurodegenerative diseases, and inflammation-related pathways. -
Multi-target modulator
PQM-244 is a multi-target modulator that primarily interacts with TRPV1 and cannabinoid receptors CB1 and CB2. It exhibits noteworthy peripheral antinociceptive properties, effectively addressing both neurogenic and inflammatory pain. Additionally, PQM-244 demonstrates antioxidant activity with an IC50 of 14.15 µM for radical scavenging of DPPH. This compound is suitable for research applications related to chronic pain and inflammatory conditions, including diabetes, atherosclerosis, and Alzheimer's disease. -
Nucleoside Transport Blocker
(S)-Draflazine is a selective nucleoside transport blocker that effectively inhibits nucleoside uptake. This compound demonstrates significant biological activity in modulating nucleoside transport mechanisms. (S)-Draflazine is utilized in research contexts to study nucleoside-related processes and their implications in various biological pathways and diseases. -
Anxiolytic Agent
Succinic acid sodium functions as an effective anxiolytic agent. It has demonstrated inhibitory effects on colonic epithelial cell proliferation in vivo and can down-regulate the expression of key genes such as KCNMB1 and TET1. This compound is particularly useful for research involving gestational hypertension and related physiological studies. -
p97 ATPase Inhibitor
p97-IN-2 is a selective inhibitor of the p97 ATPase, with an IC50 of 0.6 μM. This compound effectively inhibits the proliferation of cancer cell lines, including HCT15 (IC50 = 1.1 μM) and SW403 (IC50 = 0.8 μM). p97-IN-2 serves as a valuable tool for investigating the role of p97 in cancer biology and therapeutic applications. -
ERAD Inhibitor
NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor that functions as a direct binder to VDAC1, VDAC2, and VDAC3. It demonstrates an IC50 of 1.02 μM for inhibiting ERAD and a Kd of 3.13 μM for binding human VDAC1. By disrupting cellular calcium homeostasis and enhancing VDAC1-IP3R coupling, NCATS-SM0225 activates the PERK pathway and selectively induces apoptosis in cancer cells. This reagent is valuable for investigating cancer biology, particularly in melanoma, as well as exploring the underlying mechanisms of ERAD and calcium homeostasis regulation. -
Serotonin And Norepinephrine Reuptake Inhibitor
Milnacipran is an orally active serotonin and norepinephrine reuptake inhibitor that primarily targets the monoamine transporters responsible for neurotransmitter reuptake. It demonstrates high affinity for the norepinephrine transporter and serotonin transporter, with Ki values of 31 nM and 8.5 nM, respectively. Milnacipran exhibits antidepressant, anxiolytic, and analgesic properties, and has been shown to inhibit pERK1/2 activation. This compound is applicable in the study of major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. -
Stable Isotope
Milnacipran-d5 hydrochloride is a deuterated form of Milnacipran hydrochloride, a potent serotonin and norepinephrine reuptake inhibitor. It targets monoamine transporters, exhibiting Ki values of 31 nM for the norepinephrine transporter and 8.5 nM for the serotonin transporter. With notable antidepressant, anxiolytic, and analgesic properties, Milnacipran-d5 hydrochloride is valuable for research on major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. Additionally, it has been shown to affect behavior in preclinical models, providing insights into its pharmacological mechanisms. -
Stable Isotope
Milnacipran-d10 hydrochloride is a deuterium-labeled form of the serotonin and norepinephrine reuptake inhibitor, Milnacipran hydrochloride. It effectively inhibits monoamine transporters, targeting the norepinephrine and serotonin transporters with reported Ki values of 31 nM and 8.5 nM, respectively. This compound exhibits antidepressant, anxiolytic, and analgesic properties, and has demonstrated efficacy in reducing biting behavior in murine models. Milnacipran-d10 hydrochloride is valuable for research applications focused on major depressive disorder, anxiety disorders, and neuropathic pain syndromes, such as fibromyalgia. -
RAD51 Inhibitor
DIDS is a RAD51 inhibitor that disrupts RAD51-mediated homologous pairing and strand exchange reactions, thereby impacting DNA repair processes. In addition to its primary function, DIDS also inhibits ABCA1 and VDAC1, affecting anion exchange and binding to red blood cell membranes. Furthermore, it has been shown to inhibit the activation of caspase-3 and -9, making it a valuable tool for cancer research applications. -
Proton Pump Inhibitor
Ilaprazole sodium hydrate is a potent proton pump inhibitor that irreversibly targets H+/K+-ATPase, exhibiting an IC50 value of 6 μM in rabbit parietal cell preparations. This compound is primarily utilized in research related to gastric ulcers, providing insights into gastric acid secretion and its regulation. In addition, Ilaprazole sodium hydrate demonstrates inhibitory activity against TOPK (T-lymphokine-activated killer cell-originated protein kinase), making it a valuable tool for studies on cellular signaling pathways and cancer research. -
Adrenergic Receptor
FFN270 hydrochloride is a fluorescent tracer that specifically targets adrenergic receptors, functioning as a substrate for norepinephrine and vesicular monoamine transporters. This compound displays distinct absorption and excitation maxima at either 320 nm or 365 nm depending on the solvent pH, with an emission wavelength of 475 nm. FFN270 hydrochloride is valuable in research applications that involve monitoring norepinephrine dynamics and can also serve as a ratiometric pH sensor for various biological studies. -
β2-Adrenergic Receptor Agonist
Protokylol hydrochloride serves as a potent agonist of the β2-adrenergic receptor. This compound demonstrates significant bronchodilator activity, making it valuable in research related to respiratory function and pulmonary pharmacology. Additionally, it interacts with the TRPV1 receptor, further expanding its potential applications in studying pain pathways and sensory responses. -
Stable Isotope
(Rac)-Talinolol-d5 is a stable isotope of Talinolol, a long-acting, cardioselective β1-adrenergic receptor blocker. This compound demonstrates significant cardioprotective and antihypertensive properties. Additionally, Talinolol serves as a valuable probe substrate for investigating P-glycoprotein (P-gp) activity in pharmacokinetic studies. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
TRPV1 Agonist
Protokylol is a TRPV1 agonist that exerts its biological activity through the activation of transient receptor potential vanilloid 1 channels. Its primary application includes functioning as a bronchodilator, which supports airway relaxation and dilation. Research utilizing Protokylol can facilitate investigations into pain modulation, sensory signaling, and respiratory physiology. -
FTO Inhibitor
Meclofenamic acid sodium hydrate is a selective inhibitor of fat mass and obesity-associated enzyme (FTO). Its primary action involves competing with FTO for binding to m(6)A-containing nucleic acids, thereby influencing RNA metabolism. Additionally, it exhibits non-selective gap-junction blocking activity and inhibits potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 μM and 155.9 μM, respectively. This compound is valuable in research focused on obesity, metabolic regulation, and the role of RNA modifications in cellular processes. -
Myosin ATPase Activator
Chrysosplenol C is a flavonoid compound that functions as a selective activator of cardiac myosin ATPase, with an EC50 value of 45 µM. It enhances intracellular calcium ion release by activating protein kinase C (PKC), resulting in increased contractility of rat ventricular muscle cells. Chrysosplenol C is applicable in research related to heart failure, providing insights into mechanisms that may improve cardiac function. -
Aliostericeffect for Myosin ATPase 13 Inhibitor
Diazobenzenesulfonic acid, also known as 4-Sulfobenzenediazonium, functions as an allosteric inhibitor of myosin ATPase 13. This compound has significant biological activity by modulating the enzyme's function, thereby influencing muscle contraction mechanisms. It is primarily utilized in research applications aimed at understanding myosin-related pathways and exploring potential therapeutic targets for muscle-related diseases. -
Cardiac Myofibrillar ATPase Inhibitor
DN-F01 is a potent inhibitor of cardiac myofibrillar ATPase, exhibiting a strong calcium-dependent activity with an IC50 value of 11 ± 4 nmol/L. This compound serves as a valuable tool in studying cardiac muscle contractility and ATPase regulation. Its ability to selectively inhibit cardiac myofibrillar ATPase makes it suitable for research in cardiovascular physiology and related pathologies. -
Myosin ATPase Inhibitor
Myosin-IN-2 is a potent Myosin ATPase inhibitor, demonstrating an IC50 of 1.06 μM. This compound plays a critical role in research focused on heart diseases, particularly hypertrophic cardiomyopathy (HCM). By selectively inhibiting Myosin ATPase activity, Myosin-IN-2 provides valuable insights into the mechanisms underlying cardiac function and related pathological conditions. -
AMPA/GluR Antagonist
Tezampanel etibutil is an orally active antagonist of AMPA receptors and glutamate receptor (GluR) subtypes. This compound exhibits significant biological activity in modulating excitatory neurotransmission, making it a valuable tool for research into pain management, migraine mechanisms, and a variety of neurological disorders. Its specific targeting of AMPA receptors facilitates investigations into glutamatergic signaling pathways and their implications in neuropharmacology. -
ASK1 Inhibitor
ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications. -
Potassium Channel Opener
Bimakalim is an ATP-sensitive potassium channel opener that induces vasodilation by enhancing potassium ion efflux. This compound has been shown to reduce transmural myeloperoxidase (MPO) activity and mimics ischemic preconditioning effects, leading to decreased infarct size and modulation of adenosine release and neutrophil function. Bimakalim is valuable for research applications focused on cardiovascular physiology and ischemia-reperfusion injury studies. -
8,9-Z-isomer of Abamectin B1a
8,9-Z-Abamectin B1a is the 8,9-Z isomer of Abamectin B1a, a key antiparasitic agent. It effectively paralyzes nematodes by interacting with glutamate-gated chloride channels, leading to increased permeability of cell membranes and subsequent paralysis. This compound is widely utilized in research related to parasitology and therapeutic development for nematode infections. -
Antiparasitic Agent
Avermectin A1a is a potent antiparasitic agent that primarily targets nematodes and arthropods. It binds to glutamate-gated chloride channels, effectively blocking nerve signal transmission, which leads to paralysis of the parasites. Avermectin A1a is valuable for research on parasitic infections and contributes to the understanding of mechanisms involved in parasitic control. -
Insecticide
Avermectin B2a is an insecticide that targets glutamate-gated chloride channels (GluCls). Its primary mechanism induces hyperpolarization in nematode and insect neurons, leading to paralysis and mortality. This compound is relevant for research into the control of agricultural pests and the exploration of neurotoxic mechanisms in pests. -
Antiparasitic Agent
Δ2-Avermectin B1a is an antiparasitic agent that targets glutamate-gated chloride channels (GluCls) in the neuromuscular systems of invertebrates. By enhancing chloride ion influx, it induces hyperpolarization of the neuromuscular cell membrane, which inhibits neural signal transmission and ultimately results in paralysis and death of parasites. This compound is of significant interest for research applications aimed at controlling agricultural pests. -
Stable Isotope
Flufenamic acid-d4 is a deuterium-labeled derivative of Flufenamic acid, a non-steroidal anti-inflammatory drug. It primarily functions as a cyclooxygenase (COX) inhibitor while also activating AMP-activated protein kinase (AMPK) and modulating various ion channels, including chloride channels and L-type Ca2+ channels. This compound inhibits TEAD2 YBD functionality, affecting YAP-dependent processes such as cell migration and proliferation. Flufenamic acid-d4 is thus a valuable tool for studies in inflammation, cell signaling, and cancer research. -
Parasite
Doramectin monosaccharide, an acid degradation product of Doramectin, targets glutamate- and GABA-gated chloride channels in nematodes, enhancing their opening and resulting in effective anthelminthic activity. This compound is useful for studying the pharmacodynamics of anthelmintics and exploring mechanisms of resistance in parasitic infection research. Its significance lies in its role in understanding the biochemical pathways involved in nematode neuromuscular function and development. -
hERG Inhibitor
GSK369796 is a selective inhibitor of the hERG potassium ion channel, demonstrating an IC50 value of 7.5 μM. This compound exhibits significant antimalarial activity, making it a valuable tool for research in both cardiac function and malaria therapeutics. Its potential implications in pharmacology and drug development provide a basis for further exploration in ion channel regulation and associated biological pathways. -
Parasiticide
Sisapronil is a phenylpyrazole compound that functions as an ectoparasiticide by inhibiting the GABA-gated chloride channels in parasites, leading to paralysis and death. It exhibits potent activity against a variety of ectoparasites, making it valuable in veterinary medicine for controlling infestations. This compound is utilized in research to investigate mechanisms of action against parasitic infections. -
Stable Isotope
Atazanavir-d6 is a deuterium-labeled form of Atazanavir, a selective inhibitor of HIV-1 protease. Recognized for its capability as a CYP3A4 substrate and inhibitor, it also exerts dual effects as both an inhibitor and inducer of P-glycoprotein (P-gp). In addition, Atazanavir demonstrates antiviral activity by inhibiting the SARS-CoV 3CLpro with an IC50 of 3.49 μM, making it a valuable tool for research in HIV and coronavirus-related studies. -
ATPase Inhibitor
ATPase-IN-6 is a H+/K+-ATPase inhibitor and a prazole derivative. It exhibits significant antiviral activity against a range of viruses, including HIV-1 and SARS-CoV-2. This compound is useful for research investigating antiviral mechanisms and potential therapeutic strategies for viral infections. -
P-glycoprotein Inhibits
NIK250 is a potent inhibitor of P-glycoprotein, a key mediator of multidrug resistance (MDR) in cancer cells. By disrupting the efflux activity of P-glycoprotein, NIK250 enhances the cellular retention of chemotherapeutic agents, thereby increasing their efficacy. This compound can be utilized in research aimed at overcoming drug resistance in cancer therapies and elucidating the mechanisms of MDR in various pathological contexts. -
TrpAB Inhibitor
BRD-4592 is an allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase (TrpAB), specifically targeting the α-β-subunit interface. It demonstrates potent inhibitory activity, with an IC50 of 70.9 nM for the α-subunit and 22.6 nM for the β-subunit. This compound is valuable for research applications aimed at elucidating the role of tryptophan metabolism in tuberculosis and exploring novel therapeutic strategies against Mycobacterium tuberculosis. -
Proton Pump Inhibitor
AHR-9294 is a potent inhibitor of the H+ pump enzyme, specifically targeting H, K-ATPase. This compound effectively inhibits gastric acid secretion in vivo, making it valuable for research related to gastrointestinal physiology and the treatment of acid-related disorders. Its mechanism of action supports studies exploring proton pump inhibition and related therapeutic applications. -
ATPase Inhibitor
Apicularen A is a macrolide that selectively inhibits vesicular ATPases, targeting ATPase activity in cellular processes. This compound has been isolated from the mucoid bacterium Chondrosporium spp. Its potent inhibitory effects make it a valuable tool for research applications focused on cellular transport mechanisms and metabolic regulation.
