Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Proton Pump Inhibitor
Lansoprazole sulfide-d4 is a deuterium-labeled form of Lansoprazole sulfide, a bioactive metabolite of the proton pump inhibitor Lansoprazole. This compound exhibits significant activity against Mycobacterium tuberculosis, demonstrating IC50 values of 0.59 μM intracellularly and 0.46 μM in broth. It is a valuable tool for research into anti-tubercular therapies and the pharmacokinetics of proton pump inhibitors. -
CCR5 Antagonist
AZD-5672 is a potent and selective antagonist of the CCR5 receptor, exhibiting an IC50 of 0.32 nM. This compound demonstrates moderate activity against the hERG ion channel with a binding IC50 of 7.3 μM and acts as a substrate for human P-glycoprotein, inhibiting P-gp-mediated digoxin transport with an IC50 of 32 μM. AZD-5672 is an effective tool for investigating the role of CCR5 in inflammatory diseases, including rheumatoid arthritis. -
CCR8 Antagonist
AZ760 is a potent antagonist of the CCR8 receptor, which plays a significant role in immune response modulation. This compound demonstrates excellent potency and favorable lipophilicity, resulting in a high free fraction in blood. However, it is important to note that AZ760 exhibits unacceptable inhibition of the hERG potassium channel, which may have implications for cardiovascular safety in therapeutic applications. -
CGRP/TRPV1 Inhibitor
Chrysin 6-C-glucoside 8-C-arabinoside is a potent inhibitor of calcitonin gene-related peptide (CGRP) release and the TRPV1 channel activation. This compound exhibits significant biological activity relevant to nociceptive signaling pathways, making it a valuable tool for anti-migraine research. Its mechanism of action offers insights into potential therapeutic strategies for migraine and related pain disorders. -
OCT1 Inhibitor
Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) selectively inhibits the organic cation transporter OCT1, with an IC50 value of 6.6 μM. This compound also acts as a competitive inhibitor of tyrosine hydroxylase, reducing dopamine biosynthesis with an IC50 of 20.7 μM in PC12 cells. Hydrastine is particularly relevant for research into Parkinson's disease, as it may induce neuronal toxicity through mitochondrial dysfunction and has the potential to exacerbate apoptosis when used in conjunction with L-DOPA. -
Fatty Acid Dopamide
N-Palmitoyl dopamine is a long-chain fatty acid dopamide that interacts with endovaniloids, exhibiting 'entourage' effects on N-arachidonoyl-dopamine (NADA) and anandamide. This compound is not active on the TRPV1 receptor, highlighting its selective profile. N-Palmitoyl dopamine is valuable for research applications focused on cannabinoid and pain signaling pathways, particularly in studies examining the interplay between fatty acid derivatives and endocannabinoid activity. -
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. -
TRPV4 Agonist
4α-Phorbol 12,13-didecanoate is a potent agonist of the transient receptor potential vanilloid 4 (TRPV4). It facilitates calcium ion influx and induces ATP release, thereby serving a role as an osmoreceptor. In animal studies, 4α-Phorbol 12,13-didecanoate has been shown to inhibit water intake and elevate maximal micturition pressure in rats. This compound is valuable for research into inflammation, infection, and the biological mechanisms underlying conditions such as chikungunya virus (CHIKV). -
TRPML Agonist
ML-SA1 is a selective agonist of TRPML channels, promoting lysosomal acidification and enhancing protease activity, which leads to the inhibition of Dengue virus 2 (DENV2) and Zika virus (ZIKV). The compound exhibits IC50 values of 8.3 μM for DENV2 RNA and 52.99 μM for ZIKV RNA. Additionally, ML-SA1 stimulates autophagy, making it a valuable tool for research into broad-spectrum antiviral strategies. -
Anti-malarial Agent
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid used primarily as an anti-malarial agent. This compound functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM observed in response to voltage pulses of +100 mV. It is valuable for research applications focused on malaria treatment and investigating ion channel physiology. -
Anti-malaria Agent
Quinine hydrochloride is an alkaloid extracted from the bark of the cinchona tree, primarily functioning as an anti-malarial agent. It acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel and demonstrating inhibitory effects on channel currents evoked by voltage pulses to +100 mV, with an IC50 value of 169 μM. This compound is widely utilized in research applications related to malaria treatment and ion channel studies. -
Anti-malarial Agent
Quinine hemisulfate is an orally active alkaloid derived from cinchona bark, primarily recognized for its anti-malarial properties. This compound acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 value of 169 μM for channel currents induced by voltage pulses to +100 mV. Quinine hemisulfate serves as a valuable reagent for anti-malarial studies and relevant pharmacological investigations.
