Catalog No.
Product Name
Application
Product Information
Citations
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AMPAR PAM
CX 717 is a positive allosteric modulator of the AMPA receptor, enhancing synaptic transmission and activity. It exhibits antidepressant-like effects, making it a valuable tool in the investigation of mood disorders. Additionally, CX 717 is relevant for research into adult attention deficit hyperactivity disorder (ADHD), providing insights into neurotransmission and behavioral modulation. -
AMPA Receptor Modulator
CX614 is a positive allosteric modulator of AMPA receptors that enhances excitatory postsynaptic potentials by inhibiting and prolonging the inactivation of glutamate responses. This compound can evoke excitatory postsynaptic currents in neuronal cultures, making it particularly useful in the investigation of neurophysiological processes. CX614 has potential applications in the study of psychiatric disorders, including depression. -
AMPA receptor Modulator
JNJ-55511118 is a selective modulator of AMPA receptors, specifically targeting TARP γ-8, with an inhibition constant (Ki) of 26 nM. This compound demonstrates significant biological activity by reducing voluntary intake of sweetened alcohol in male murine models. In addition, it disrupts hippocampal neurotransmission, alters specific electroencephalogram frequency bands, induces transient hyperlocomotion, and impairs cognitive functions such as learning and memory, while also exhibiting anticonvulsant properties. JNJ-55511118 is valuable for research focused on alcohol use disorders and seizure mechanisms. -
AMPA-R Potentiator
HBT1 is a selective AMPA receptor (AMPAR) potentiator that enhances receptor activity in the presence of AMPA by binding to its ligand-binding domain. Unlike traditional AMPA-R potentiators, HBT1 exhibits a limited agonistic effect, minimizing the risk of bell-shaped dose-response curves related to brain-derived neurotrophic factor (BDNF) production. This unique profile allows for broader research applications in neurological and psychiatric disorders, including depression and Alzheimer’s disease. -
AMPAR Inhibitor
TAT-GluA2 3Y is an AMPAR inhibitor that interferes with the endocytosis of AMPA receptors, thereby blocking long-term depression (LTD) at glutamatergic synapses. This peptide has been shown to mitigate pentobarbital-induced spatial memory deficits, highlighting its potential in studying synaptic plasticity and memory-related research applications. TAT-GluA2 3Y serves as a valuable tool for exploring the mechanisms underlying synaptic transmission and cognitive function. -
AMPAR Enhancer
CX1739 is an AMPA-glutamate receptor (AMPAR) enhancer that significantly enhances long-term potentiation in a dose-dependent manner in mouse models. This compound effectively mitigates amphetamine-induced locomotor activity and rapidly reverses opioid-induced respiratory depression. Research applications for CX1739 include studies related to dementia, neuropsychiatric disorders, and complications arising from opiate-induced suppression of endogenous inspiratory breathing rhythms. -
AQP2/CFTR Inhibitor
Steviol is a selective inhibitor of the aquaporin-2 (AQP2) and cystic fibrosis transmembrane conductance regulator (CFTR) proteins. This compound impedes renal cyst growth by inhibiting CFTR activity, which leads to decreased AQP2 expression and promotes the degradation of both AQP2 and CFTR. Steviol is relevant for research focused on polycystic kidney disease and mechanisms underlying renal cyst development. -
EHD4 ATPase Inhibitor
ATPase-IN-4 is a selective inhibitor of EHD4 ATPase activity, with an IC50 value of 0.92 μM. This compound also exhibits inhibitory effects on the ATPase activity of EHD2. ATPase-IN-4 is valuable for research applications focused on understanding the role of EHD proteins in cellular processes and membrane trafficking. -
ATPase Inhibitor
ATPase-IN-2 is a potent ATPase inhibitor with an IC50 value of 0.9 μM. It effectively inhibits the glycohydrolase activity of Clostridium difficile toxin B (TcdB) with an AC50 value of 30.91 μM. This compound serves as a valuable tool for studying ATP-related mechanisms and elucidating the role of ATPases in various biological processes. -
CF1 ATPase Inhibitor
Ovothiol A disulfide is a specific inhibitor of CF1 ATPase, targeting its light-activated function. This compound has been shown to effectively inhibit ATP synthesis in photophosphorylation processes, making it a valuable tool for studying energy transduction in photosynthetic organisms. Its role in modulating ATPase activity provides insights into the regulation of bioenergetics and enzyme kinetics in various biological systems. -
Mitochondrial F0F1-ATPase Inhibitor
Isoapoptolidin is an inhibitor of the mitochondrial F0F1-ATPase, exhibiting a Ki greater than 100 μM and selective action towards mitochondrial complex V. This compound is valuable for investigating mitochondrial energy metabolism-related disorders, including cancer and neurodegenerative diseases. Its inhibitory properties facilitate studies on the role of ATP synthase in cellular energy regulation. -
Dual MDR1/BCRP Inhibitor
CP-100356 hydrochloride is a potent dual inhibitor of MDR1 (P-glycoprotein) and BCRP, featuring IC50 values of 0.5 µM and 1.5 µM for the inhibition of MDR1-mediated transport of Calcein-AM and BCRP-mediated transport of Prazosin, respectively. It also exhibits off-target activity as a weak inhibitor of OATP1B1 with an IC50 of approximately 66 µM, while showing no significant inhibition against MRP2 or major human P450 enzymes (IC50 > 15 µM). This compound is useful in studying drug transport dynamics and enhancing the bioavailability of therapeutic agents in pharmacological research. -
BCRP Inhibitor
Ac32Az19 is a selective inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating a potent inhibitory effect with an EC50 value of 13 nM in BCRP-overexpressing HEK293/R2 cells. This high affinity and nontoxic profile make Ac32Az19 a valuable tool for research applications focused on drug transport mechanisms and multidrug resistance in cancer studies. Its specificity for BCRP allows for detailed investigations into therapeutic strategies and the modulation of drug pharmacokinetics. -
ABCG2/BCRP Inhibitor
Efflux inhibitor-1 is a pyrazolo[1,5-a]pyrimidine compound that selectively inhibits the ABCG2/BCRP transporter. With IC50 values of 0.45 μM for ABCG2/BCRP and 2.17 μM for ABCB1, this inhibitor is a valuable tool for studying drug efflux mechanisms and multidrug resistance. It is useful in research applications focused on cancer pharmacology and the modulation of drug absorption and resistance pathways. -
BCRP Inhibitor
ML753286 is a selective inhibitor of the Breast Cancer Resistance Protein (BCRP), exhibiting an IC50 of 0.6 μM. This compound demonstrates high permeability and moderate clearance in liver S9 fractions from both rodent and human sources. Additionally, ML753286 remains stable across species in plasma, making it a valuable tool for studies investigating drug resistance mechanisms and pharmacokinetics in cancer research. -
BCRP Inhibitor
Ac22(Az8)2 is a selective inhibitor of the Breast Cancer Resistance Protein (BCRP), exhibiting an EC50 value of 1-2 nM. This compound effectively restores drug sensitivity in BCRP-overexpressing cells by inhibiting BCRP-ATPase activity, thereby blocking drug efflux and enhancing intracellular drug accumulation. Ac22(Az8)2 is a valuable tool for investigating BCRP-mediated mechanisms in multidrug-resistant cancers. -
BCRP Inhibitor
Pentamethoxymorin is a selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2), demonstrating significant potency with IC50 values of 5.98 μM and 5.94 μM in the Hoechst 33342 and Pheophorbide A assays, respectively. This compound showcases a preference for BCRP over other efflux transporters such as P-glycoprotein and MRP1. Pentamethoxymorin is valuable for research focusing on cancer resistance mechanisms and potential therapeutic interventions in breast cancer. -
MDR1/BCRP Inhibitor
CP-100356 is a dual inhibitor of MDR1 (P-glycoprotein) and BCRP, exhibiting IC50 values of 0.5 µM and 1.5 µM, respectively, for the inhibition of MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport. Additionally, CP-100356 shows weak inhibition of the OATP1B1 transporter, with an IC50 of approximately 66 µM, while demonstrating minimal inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM). This compound is valuable for research applications targeting drug resistance mechanisms and transport protein interactions in pharmacology and toxicology studies. -
BCRP/ABCG2 Inhibitor
Butein tetramethyl ether is a selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2) that demonstrates potent biological activity. It has been shown to inhibit BCRP in MCF-7 MX and MDCK cell lines, with IC50 values of 2.2 μM and 1.03 μM, respectively. This compound is a valuable tool for research investigating the mechanisms of cancer resistance and could provide insights into therapeutic strategies for overcoming drug resistance in cancer treatments. -
ABCG2 (BCRP) Inhibitor
UR-MB108 is a selective inhibitor of ABCG2 (BCRP) with an IC50 value of 79 nM. This compound demonstrates high potency in inhibiting the efflux activity of the ABCG2 transporter. UR-MB108's stability in blood plasma enhances its potential for various biological applications, including studies on drug absorption and resistance in cancer research. -
P-gp/BCRP Inhibitor
P-gp/BCRP-IN-1 is a potent inhibitor targeting P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). This compound is designed to reverse drug resistance by inhibiting the efflux activities of these pivotal transporters. P-gp/BCRP-IN-1 enhances the oral bioavailability of chemotherapeutic agents, such as Paclitaxel (PTX), making it a valuable tool in cancer research and therapeutic development. Its efficacy and oral activity suggest a promising utility in overcoming drug resistance in various cancer models. -
BCRP
2,4-Dibromoestradiol primarily targets the ABCG2 transporter, a member of the ATP-binding cassette (ABC) family. This compound exhibits significant influence on the function of the breast cancer resistance protein (BCRP), which is pivotal in drug efflux and resistance mechanisms. It is utilized in research focused on drug transport, pharmacokinetics, and cancer biology. -
Substrate for BCRP
INCB-056868 is a metabolite of Epacadostat (M11) that acts as a substrate for the Breast Cancer Resistance Protein (BCRP). This compound is valuable for investigating the mechanisms underlying metabolic diseases and the transport processes mediated by BCRP. Its role in examining drug metabolism and resistance mechanisms makes it a significant reagent for biochemical research. -
BCRP Inhibitor
BCRP-IN-2 is a potent inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating enhanced inhibitory activity upon ultraviolet light activation. This compound serves as an effective probe for investigating the interactions of quinazolinamine derivatives with BCRP, facilitating ATP hydrolysis of the transport protein. BCRP-IN-2 significantly increases the accumulation of mitoxantrone in H460/MX20 cells, which exhibit BCRP overexpression, making it valuable for studies on multidrug resistance mechanisms in cancer research. -
BCRP/ABCG2 Inhibitor
3,7,2',4'-Tetramethoxy-5-hydroxyflavone is a potent inhibitor of the breast cancer resistance protein (BCRP/ABCG2), exhibiting an IC50 value of 5.98 μM. This compound is significant for research into multidrug resistance mechanisms in breast cancer, providing insights into potential therapeutic strategies to overcome treatment resistance. Its ability to modulate BCRP activity makes it a valuable tool in cancer pharmacology studies. -
BCRP Inhibitor
BCRP-IN-1 is a potent inhibitor of breast cancer resistance protein (BCRP), exhibiting IC50 values of 2.92 μM in the Hoechst 33342 assay and 2.46 μM in the Pheophorbide A assay. This compound is valuable for research applications targeting multidrug resistance in cancer cells, facilitating the study of therapeutic efficacy and drug transport mechanisms. Its selective inhibition of BCRP makes it an essential tool for understanding resistance pathways in oncology. -
Dihydropyridine Calcium Antagonist
(S)-Nimodipine is a potent dihydropyridine calcium antagonist known for its selective effect on calcium channels. It exhibits significant biological activity, primarily in the management of cerebrovascular disorders by improving cerebral blood flow. This compound is especially valuable in research focusing on neurological conditions and the effects of calcium modulation in neuronal tissue. -
Calcium Channel Blocker
Verapamil hydrochloride is a calcium channel blocker primarily targeting L-type calcium channels. It exhibits potent inhibitory activity on P-glycoprotein and CYP3A4, contributing to its pharmacological profile. This compound is widely utilized in research related to hypertension, cardiac arrhythmias, and angina, facilitating studies on cardiovascular function and drug metabolism. -
L-type Calcium Chanel Inhibitor
Diltiazem is an orally active L-type calcium channel blocker that exerts antihypertensive and antiarrhythmic effects. It is utilized in research related to cardiac arrhythmias, hypertension, and angina pectoris, making it valuable for studies focused on cardiovascular health. Its mechanism of action contributes to the modulation of calcium influx, which is critical in various cardiac and vascular functions. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
TRPM2 Agonist
Farnesyl pyrophosphate ammonium is an agonist of the TRPM2 channel, facilitating calcium influx and promoting cell death. It serves as a crucial intermediate in the mevalonate pathway, with significant roles in cholesterol and ubiquinone synthesis, as well as protein farnesylation. This compound is utilized in research focusing on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune disorders. -
TRPC6 Activator
Hyperforin dicyclohexylammonium salt is a selective activator of transient receptor potential canonical 6 (TRPC6) channels. By modulating Ca2+ flux, this compound influences a variety of biological processes and exhibits notable pharmacological activities, including anti-depression, anti-tumor, anti-dementia, and anti-diabetic effects. Additionally, Hyperforin dicyclohexylammonium salt has been shown to enhance the secretion of IL-17α from γδ T cells and demonstrates efficacy in improving psoriasis-like symptoms in the Imiquimod-induced mouse model. This compound serves as a valuable tool in research focused on calcium signaling and related therapeutic applications. -
Potassium Supplement
Potassium chloride, AR, 99.5% serves as an essential potassium supplement, playing a critical role in various biochemical applications. This compound is particularly valuable in research related to hyperkalemia, where it aids in studying potassium ion regulation in biological systems. Additionally, it functions as a potassium source in agronomy, contributing to plant nutrition and growth. -
Calcium Channels Antagonist
Fluspirilene is a non-competitive antagonist of L-type calcium channels, demonstrating an IC50 of 0.03 μM. This compound exhibits significant antipsychotic activity, making it a valuable tool for research on schizophrenia and related neuropsychiatric disorders. Its long-acting injectable formulation facilitates studies on sustained pharmacological effects in therapeutic applications. -
T Calcium Channel Antagonist
Ulixacaltamide is a potent T-type calcium channel antagonist that demonstrates significant efficacy in modulating neurological disorders. It has been shown to slow the progression of epilepsy and effectively reduce tremors in an alkaline tremor animal model. Additionally, Ulixacaltamide reverses thermal hyperalgesia, providing a mechanism for pain relief in various preclinical settings. This compound is valuable for research applications focusing on neurological function and pain management. -
SERCA Blocker
JTV-519 hemifumarate is a selective blocker of the sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA), with additional activity as a partial agonist of ryanodine receptors in striated muscle. It exhibits antiarrhythmic and cardioprotective properties, making it a valuable tool for research on cardiac function and rhythm disorders. This compound is useful in studies exploring calcium handling in myocardial cells and its implications for heart disease therapies. -
T-type Calcium Channel Blocker
TTA-P2 is a selective T-type calcium channel blocker with a primary mechanism of inhibiting calcium influx through T-type channels, exhibiting an IC50 of 22 nM. This compound demonstrates significant biological activity by reducing mechanical hypersensitivity and alleviating both acute and chronic pain. Additionally, TTA-P2 lowers firing rates in neurons associated with temporal lobe epilepsy, effectively controlling synaptically evoked burst firing. Research applications include investigations into neurological disorders such as tremor and absence epilepsy. -
Calcium Channel Inhibitor
Tetracaine hydrochloride is a calcium channel inhibitor that effectively blocks the voltage-sensitive release of Ca2+ from the sarcoplasmic reticulum. This compound exhibits significant biological activity and is primarily utilized in topical applications within ophthalmology, as well as serving as an antipruritic agent. Its mechanism of action makes it valuable for research in pain relief and modulation of calcium signaling pathways. -
Neuroprotective Compound
REM127 is a neuroprotective small molecule that modulates calcium homeostasis in cells. It effectively restores calcium balance in cellular models affected by the pathological accumulation of tau protein, demonstrating potential to mitigate synaptic and cognitive deficits in Alzheimer's disease models. REM127 is capable of crossing the blood-brain barrier and may slow the progression of amyloid-beta and tau protein pathologies. This compound is suitable for research applications in neurodegenerative diseases. -
SERCA2a Activator
SERCA2a Activator 1 is an activator of the sarco/endoplasmic reticulum Ca2+-dependent ATPase 2a (SERCA2a). This compound alleviates the inhibitory effects of phospholamban, thereby improving both systolic and diastolic cardiac functions. SERCA2a Activator 1 is primarily utilized in research related to heart failure and cardiac physiology. -
Potassium Channel Blocker
Azimilide dihydrochloride is a class III antiarrhythmic agent that functions primarily as a potassium channel blocker, targeting both IKs and IKr channels with IC50 values of 2.6 μM and 1 μM, respectively. Additionally, it inhibits the HERG channel at frequencies of 0.1 and 1 Hz, with IC50 values of 1.4 μM and 5.2 μM. Azimilide dihydrochloride also suppresses L-type calcium current and sodium current, with IC50 values of 17.8 μM and 19 μM, respectively. This compound is valuable for researching conditions such as atrial fibrillation and ventricular fibrillation. -
Calcium Ions Activator
Calcium citrate tetrahydrate is a calcium ions activator that efficiently releases calcium ions, enhancing biological activity in various applications. Its rapid solubility and ability to maintain elevated calcium ion concentrations make it particularly useful for research focused on bone formation and mineralization. This reagent is essential for studies investigating calcium-related signaling pathways and the effects of calcium on cellular processes. -
Calcium Channel Blocker
Prenylamine is a calcium channel blocker belonging to the amphetamine chemical class. It acts by inhibiting calcium influx through voltage-gated calcium channels, leading to vasodilation. This compound has potential applications in the research of cardiovascular conditions, particularly angina pectoris, by modulating vascular tone and reducing myocardial oxygen demand. -
Stable Isotope
Verapamil-d3 hydrochloride is a deuterium-labeled derivative of the calcium channel blocker, verapamil hydrochloride. It serves as a potent inhibitor of P-glycoprotein (P-gp) and CYP3A4, facilitating detailed pharmacological studies. This stable isotope is primarily utilized in research related to hypertension, cardiac arrhythmias, and angina, providing insight into drug metabolism and transport mechanisms in various biological systems. -
Ca2+-ATPase Inhibitor
IPrAuCl is a gold compound that functions as a selective inhibitor of sarcoplasmic reticulum Ca2+-ATPase, demonstrating an IC50 value of 16.3 µM. Its primary mechanism involves hindering calcium ion transport, making it a valuable tool for researching calcium homeostasis and muscle contraction dynamics. IPrAuCl may also be useful in studies investigating the role of Ca2+-ATPase in various cellular processes and diseases. -
Calcium Receptor Activator
γ-Glutamylserine (γ-Glu-Ser) is a calcium receptor activator that plays a critical role in various cellular signaling pathways. This compound exhibits potential neuroprotective effects, making it relevant for research in Parkinson's disease. Additionally, γ-Glutamylserine may be utilized in studies focused on metabolic disorders, including diabetes and obesity. -
mNCX Blocker
ITH12575 is a potent and selective blocker of the mitochondrial sodium-calcium exchanger (mNCX). This compound effectively reduces calcium influx through CALHM1 channels at low micromolar concentrations. ITH12575 is valuable for research applications focused on calcium homeostasis, cell signaling, and mitochondrial function. -
Phenylalkylamine Calcium Antagonist
Gallopamil hydrochloride is a phenylalkylamine calcium antagonist that exhibits potent antiarrhythmic and vasodilatory properties. It effectively inhibits acid secretion in a concentration-dependent manner, with an IC50 value of 10.9 μM. This compound is utilized in various research applications focused on cardiovascular function and gastrointestinal acid regulation. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Calcium Channel
D-myo-Inositol-1,3,4,5-tetraphosphate sodium functions as a signaling molecule by regulating calcium channels. It is produced through the phosphorylation of inositol 1,4,5-trisphosphate by inositol 1,4,5-triphosphate 3-kinase. This compound is utilized in research focused on cellular signaling pathways, particularly those involving calcium mobilization and inositol phosphate metabolism. Its key biological activity makes it valuable for studies exploring neurotransmission, smooth muscle contraction, and other calcium-dependent processes.
