Catalog No.
Product Name
Application
Product Information
Citations
-
TRPV1 Antagonist
(S)-AMG-628 is a selective TRPV1 antagonist that effectively inhibits capsaicin- and acid-induced calcium influx, demonstrating IC50 values of 7 nM and 5 nM, respectively, in CHO cells. This compound has shown significant efficacy in reducing capsaicin-induced flinching behavior in rats and reversing thermal hypersensitivity in CFA-induced inflammatory pain models. As such, (S)-AMG-628 serves as a valuable tool in research addressing pain mechanisms and potential therapeutic interventions for inflammatory pain conditions. -
TRPV1 Agonist
MSK-195 is a potent agonist of the transient receptor potential vanilloid 1 (TRPV1) channel, demonstrating a potency of 120 nM and an efficacy of 71% in inducing arteriolar responses. This compound is valuable for research applications aimed at understanding pain pathways, neurogenic inflammation, and the physiological role of TRPV1 in various tissues. Its ability to selectively activate TRPV1 makes it a useful tool for dissecting the functions and mechanisms associated with this receptor in preclinical studies. -
TRPV1 Antagonists
A778317 is a potent TRPV1 antagonist, designed to inhibit the activation of TRPV1 receptors. With a pIC50 value of 8.31, it effectively blocks intracellular calcium level changes mediated by TRPV1. This compound has demonstrated the capability to prevent capsaicin and acid-induced activation of natural rat TRPV1 receptors in dorsal root ganglion neurons, making it a valuable tool for research focused on pain mechanisms and sensory nerve function. -
TRPV1 Stimulator Activator
Cyclo(-asp-gly) is a cyclic dipeptide that functions as a TRPV1 stimulator, enhancing the activity of the transient receptor potential vanilloid 1 ion channel. This compound is utilized in research applications related to pain signaling and sensory perception, making it a valuable tool in studies focused on nociception and the mechanisms of pain modulation. Its role in activating TRPV1 provides insights into potential therapeutic approaches for pain management. -
TRPV1 Agonist
JYL-79 is a potent TRPV1 agonist, exhibiting an IC50 of 3.9 nM. It is primarily used in research focused on neuropathic pain, allowing for the exploration of TRPV1's role in pain pathways and potential therapeutic interventions. This compound provides valuable insights into the mechanisms of pain modulation and serves as a tool for investigating the biology of sensory neurons. -
TRPV3 Modulator
TRPV3 modulator-1 is a selective modulator of the transient receptor potential vanilloid 3 (TRPV3) channel. It exhibits the ability to regulate TRPV3 activity, influencing calcium ion influx in response to thermal and chemical stimuli. This compound has potential applications in research related to pain sensation, skin physiology, and itch, making it a valuable tool for studying TRPV3-mediated signaling pathways. -
TRPC4/5 Inhibitor
M084 hydrochloride is a selective inhibitor of the TRPC4 and TRPC5 ion channels, exhibiting IC50 values of 10.3 μM and 8.2 μM, respectively. This compound demonstrates significant antidepressant and anxiolytic effects, making it a valuable tool for studying anxiety and mood disorders. Its ability to modulate calcium influx through TRPC channels positions M084 hydrochloride as an important reagent for research in neurobiology and pharmacology. -
TRPV4 Antagonist
TRPV4 antagonist 5 is a selective antagonist of the TRPV4 channel, which is involved in various physiological processes including osmoregulation and pain sensation. This compound demonstrates potential in modulating TRPV4-mediated responses and can be utilized in research focusing on inflammation, pain management, and sensory neuronal pathways. Its application may also extend to investigations of cellular calcium signaling and the development of therapeutics targeting TRPV4-related disorders. -
TRPV1 Antagonist
AC4 is a potent TRPV1 antagonist that acts as a trans antagonist upon voltage activation of the receptor and functions as a cis antagonist in response to capsaicin stimulation. This compound serves as a valuable tool for investigating TRPV1 signaling pathways and the modulation of nociceptive responses. Its unique photoswitchable properties allow for the combined use of an antagonist and an agonist, making it an essential reagent for research in pain mechanisms and sensory biology. -
TRPV1 Inhibitor
AMG-628 is a potent orally active inhibitor of the transient receptor potential vanilloid 1 (TRPV1). It effectively blocks capsaicin and acid-induced calcium influx in TRPV1-expressing CHO cells, with IC50 values of 4.9 nM and 3.1 nM, respectively. AMG-628 demonstrates significant analgesic effects in capsaicin-induced rat pain models and has a half-life of approximately 2.4 hours in rats, making it a valuable tool for studying pain mechanisms and potential therapeutic applications. -
TRPC3/6 Blocker
TRPC3/6-IN-1 is a selective blocker of the canonical transient receptor potential channels TRPC3 and TRPC6, exhibiting IC50 values of 1260 nM and 500 nM, respectively. This compound is instrumental for investigating the role of TRPC3 and TRPC6 in cardiac physiology and pathophysiology, particularly in chronic models of heart failure. Its specific inhibitory action makes it a valuable tool for studying the mechanisms underlying cardiovascular diseases. -
TRPA1 Antagonis
Ibuprofen acyl-β-D-glucuronide is a selective antagonist of the TRPA1 ion channel. This compound effectively reduces the calcium response induced by allyl isothiocyanate (AITC), exhibiting an IC50 value of 60 μM. It is a valuable tool for investigating TRPA1-related pathways and for exploring potential therapeutic applications in pain modulation and sensory signal transduction. -
TRPA1 Inhibitor
TRPA1-IN-3 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel. This compound is primarily utilized in research focused on skin and respiratory tract conditions, where TRPA1 activation is implicated in nociceptive signaling and inflammatory responses. Its inhibitory properties make it valuable for studying pain mechanisms and potential therapeutic interventions in related disorders. -
TRPV1 Antagonist
JNJ-39729209 is a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel, displaying pIC50 values of 7.9 to 8.5 across various species including human, rat, canine, and guinea pig. This compound effectively inhibits capsaicin-induced hypotension and associated hypothermia. Additionally, JNJ-39729209 demonstrates significant anti-inflammatory and analgesic effects in carrageenan and CFA-induced thermal hyperalgesia models in rats, as well as anti-cough activity in guinea pigs, making it a valuable tool for research in pain and inflammatory response. -
TRP Channel Antagonist
TRPV Antagonist 1 is a selective transient receptor potential vanilloid (TRPV) channel antagonist, exhibiting an IC50 of less than 250 nM. This compound effectively inhibits TRPV-mediated calcium influx, making it a valuable tool for investigating TRPV-related signaling pathways. It is applicable in research focused on pain, inflammation, and sensory neuron function, facilitating the study of TRPV channels in various biological contexts. -
URAT Inhibitor
Xininurad is a selective urate transporter (URAT) inhibitor that modulates uric acid levels in the body. By inhibiting URAT, it promotes renal excretion of uric acid, making it a valuable tool for studying hyperuricemia and related conditions such as gout. This compound serves as a potential therapeutic agent in research aimed at understanding and treating disorders associated with elevated urate concentrations. -
URAT1 Inhibitor
URAT1 inhibitor 3 is a selective inhibitor of the urate transporter 1 (URAT1), demonstrating a potent inhibition with an IC50 value of 0.8 nM. This compound effectively lowers urate levels, making it valuable for studies focused on gout and hyperuricemia. Its oral bioavailability allows for convenient administration in various biological assays and preclinical research settings. -
URAT1 Inhibitor
Ruzinurad is a highly selective inhibitor of the URAT1 transporter, which plays a critical role in the regulation of uric acid levels. By inhibiting URAT1, Ruzinurad effectively reduces uric acid reabsorption, making it a valuable tool in the study of hyperuricemia and related metabolic disorders. This compound has potential applications in research focusing on conditions such as gout and other diseases associated with elevated uric acid levels. -
URAT Inhibitor
Puliginurad is a potent inhibitor of the urate transporter (URAT), which plays a critical role in uric acid reabsorption in the renal system. This compound is valuable for research in hyperuricemia and gout, offering insights into uric acid metabolism and potential therapeutic interventions. Its application in experimental studies can help elucidate the mechanisms underlying these conditions and support the development of novel treatment strategies. -
URAT1 Inhibitor
URAT1 inhibitor 6 is a selective inhibitor of the urate transporter URAT1, exhibiting an IC50 value of 35 nM for human URAT1. This compound demonstrates significantly enhanced potency compared to its parent compound, Lesinurad, and the reference compound Benzbromarone. URAT1 inhibitor 6 is valuable for investigating uric acid transport and inflammation-related research applications. -
URAT1 Inhibitor
URAT1 inhibitor 8 is a potent inhibitor of the urate transporter URAT1, exhibiting an IC50 of 0.001 μM. This compound is valuable for research applications focused on gout, offering insights into mechanisms of uric acid regulation and potential therapeutic strategies for hyperuricemia. Its high efficacy makes it a significant tool for studying renal handling of urate and related disorders. -
Xanthine Oxidase Inhibitor
URAT1&XO Inhibitor 1 is a dual inhibitor targeting both URAT1 and Xanthine Oxidase, with IC50 values of approximately 10 μM and 1.01 μM, respectively. This compound effectively induces a hypouricemic effect in a potassium oxonate-induced hyperuricemia rat model. URAT1&XO Inhibitor 1 is valuable for research applications focused on hyperuricemia and related disorders. -
URAT1&XO Inhibitor
URAT1&XO Inhibitor 2 is a dual inhibitor targeting xanthine oxidase and URAT1, exhibiting an IC50 of 3.3 μM for xanthine oxidase. This compound effectively inhibits uric acid uptake in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. In hyperuricemic mouse models, it has been shown to reduce serum urate levels and decrease uric acid excretion. URAT1&XO Inhibitor 2 is valuable for researching conditions related to hyperuricemia. -
hURAT1 Inhibitor
hURAT1 inhibitor 2 is a selective inhibitor of hURAT1 (uric acid transporter 1, SLC22A12), exhibiting an IC50 of 18 nM. Additionally, it demonstrates moderate inhibitory activity on OATP1B1 with an IC50 of 0.73 μM. This compound is valuable for research focused on disorders associated with dysregulated uric acid metabolism, including hyperuricemia and gout. -
URAT1 Inhibitor
Lingdolinurad is a selective inhibitor of the urate transporter URAT1. It effectively reduces urate reabsorption, making it a valuable tool in studying hyperuricemia. This compound can be applied in both in vitro and in vivo research to explore its potential therapeutic effects and underlying mechanisms in disorders associated with elevated uric acid levels. -
URAT1 Inhibitor
JTT-552 is a selective URAT1 inhibitor known for its ability to reduce uric acid reabsorption in the renal system. This compound demonstrates significant potential in managing hyperuricemia and treating gout by promoting uric acid excretion. Its application in research can aid in understanding the pathophysiology of gout and developing therapeutics aimed at uric acid regulation. -
URAT1 Inhibitor
URAT1 inhibitor 7 is a potent inhibitor of the urate transporter URAT1, demonstrating an IC50 of 12 nM. This compound exhibits excellent microsomal stability, with a hepatic microsomal clearance rate of less than 13 µL/min/mg. Additionally, it has been shown to inhibit CYP2C9 with an IC50 of 4.2 µM. URAT1 inhibitor 7 is suitable for research applications focused on gout and related disorders. -
XOR/URAT1 Inhibitor
XOR/URAT1-IN-1 is a dual inhibitor targeting xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), exhibiting IC50 values of 6 nM and 12.9 μM, respectively. This compound effectively reduces uric acid levels in models of acute hyperuricemia induced by potassium oxonate or hypoxanthine. It serves as a valuable tool for studying disorders related to hyperuricemia and offers potential therapeutic insights for conditions such as gout. -
URAT1 Inhibitor
URAT1 Inhibitor 10 is a potent inhibitor of the URAT1 transporter, demonstrating high selectivity for OAT1. This compound exhibits oral bioavailability and low cytotoxicity, making it suitable for in vivo studies. It is primarily used in research applications focused on renal physiology and uric acid transport, aiding investigations into gout and related disorders. -
URAT1 Inhibitor
Darbinuradum is an inhibitor of the urate transporter URAT1, primarily impacting uric acid reabsorption in the renal proximal tubule. This compound demonstrates significant potential in research related to hyperuricemia and gout management by reducing uric acid levels in plasma. It is utilized in studies investigating the therapeutic effects of urate-lowering therapies and their implications for cardiovascular health and kidney function. -
URAT1 Inhibitor
URAT1 inhibitor 13 is a selective inhibitor of the urate transporter 1 (URAT1), which is primarily involved in renal urate reabsorption. This compound exhibits strong biological activity in reducing urate levels and is particularly relevant in the study of gout and other related hyperuricemia conditions. Researchers can utilize URAT1 inhibitor 13 to explore its therapeutic potential and the underlying mechanisms in urate regulation. -
URAT1 Inhibitor
URAT1 inhibitor 2 is a potent inhibitor of the URAT1 transporter, exhibiting an IC50 of 1.36 µM for URAT1-mediated 14C-UA uptake, alongside effective inhibition of CYP1A2 and CYP2C9 with IC50 values of 16.97 µM and 5.22 µM, respectively. This compound demonstrates significant potential in the investigation of hyperuricemia and gout, making it a valuable tool for biochemical research and therapeutic development. -
URAT1 Inhibitor
URAT1 Inhibitor 5 is an effective inhibitor of the urate transporter URAT1. This compound has demonstrated potential in modulating uric acid reabsorption, making it relevant for the investigation of hyperuricemia and related conditions. Its application in biochemical research can facilitate the development of therapeutics targeting disorders associated with elevated uric acid levels. -
URAT1 Inhibitor
URAT1 Inhibitor 9 targets the urate transporter URAT1, playing a crucial role in regulating uric acid levels. This compound demonstrates significant biological activity in the management of gout and hyperuricemia by inhibiting uric acid reabsorption in the kidneys. URAT1 Inhibitor 9 is valuable for research focusing on urate homeostasis and associated metabolic disorders. -
URAT1 Inhibitor
URAT1 Inhibitor 11 is a potent inhibitor of the URAT1 transporter, exhibiting an IC50 value of 0.18 μM. This compound demonstrates significant hypouricemic effects in hyperuricemic zebrafish models induced by potassium oxonate and xanthine sodium salt. URAT1 Inhibitor 11 serves as a valuable tool for research applications focused on hyperuricemia and related metabolic disorders. -
URAT1/XO Inhibitor
URAT1&XO Inhibitor 3 is a potent inhibitor of both xanthine oxidase (XO) and urate transporter 1 (URAT1), with IC50 values of 35 nM and 31 nM, respectively. This compound exhibits significant potential as an orally active anti-gout agent, demonstrating favorable pharmacological and pharmacokinetic properties. Additionally, URAT1&XO Inhibitor 3 has been shown to have in vivo safety, making it a valuable tool for research in the management of hyperuricemia and gout-related disorders. -
URAT1 Inhibitor
HC-1310 is a potent inhibitor of URAT1, a transporter involved in uric acid reabsorption in the renal system. This compound is primarily utilized in research focused on hyperuricemia and gout, providing valuable insights into therapeutic strategies for managing elevated uric acid levels. By inhibiting URAT1, HC-1310 facilitates increased uric acid excretion, making it a critical tool for studying conditions associated with abnormal purine metabolism. -
URAT1 Inhibitor
URAT1-IN-14 is a potent inhibitor of the urate transporter 1 (URAT1), demonstrating a human URAT1 inhibition IC50 of 0.72 μM in HEK293 cells. This compound exhibits minimal cytotoxicity in Hep-G2 cells, making it suitable for cellular applications. URAT1-IN-14 has been shown to effectively reduce urate levels in hyperuricemia mouse models, supporting its use in research related to hyperuricemia and gout. -
Calcium Channel Inhibitor
ω-Hexatoxin-Hv1a is a selective inhibitor of L-type voltage-dependent calcium channels. This neurotoxin reduces intracellular calcium ion concentration, thereby mitigating apoptosis, necroptosis, and oxidative stress, while enhancing cellular recovery and energy levels. Its ability to induce paralysis and mortality in insects through the disruption of central nervous system neurotransmission underscores its potency, although it has limited oral toxicity. Consequently, ω-Hexatoxin-Hv1a is a valuable tool for research into ischemia-reperfusion injury, atopic dermatitis, and ischemic damage in cardiomyocytes and neurons. -
Calcium Channel Antagonist
UK 52831 is a long-acting dihydropyridine calcium channel antagonist that selectively inhibits calcium influx through L-type calcium channels. This compound exhibits significant cardiovascular activity, making it valuable for research into conditions such as hypertension and myocardial ischemia. Additionally, UK 52831 has potential applications in anti-inflammatory studies, providing insights into the role of calcium signaling in inflammatory processes. -
Calcium/Sodium Channel Blocker
LY393615 (NCC1048) is a selective blocker of neuronal calcium (Ca2+) and sodium (Na+) channels, demonstrating IC50 values of 1.9 μM and 5.2 μM for the α1A and α1B calcium channel subunits, respectively. This compound exhibits excellent brain penetration and displays neuroprotective effects in cerebral ischemia models, making it a valuable tool for research in neurological diseases. Its dual-channel blocking mechanism contributes to its potential applications in understanding neuronal excitability and neuroprotection. -
Calcium Channel Blocker
Leualacin is a calcium channel blocker derived from the fungus Hapsidospora irregularis. This compound demonstrates significant inhibition of calcium influx through voltage-gated calcium channels, leading to potential therapeutic effects in conditions characterized by excitability and muscle contraction disorders. It is applicable in research exploring cardiovascular function and neurophysiology, providing insights into calcium signaling pathways. -
Calcium Channel
Semotiadil recemate fumarate is a vasoselective Ca2+ channel antagonist that inhibits calcium influx in vascular smooth muscle cells. It primarily targets L-type calcium channels, leading to vasodilation and reduced vascular resistance. This compound is significant in research related to cardiovascular diseases and may offer therapeutic insights into hypertension and related conditions. -
T-Type Calcium Channel Inhibitor
T-Type Calcium Channel Inhibitor 2 is a selective inhibitor of T-type calcium channels, specifically targeting Cav3.1 (α1G), Cav3.2 (α1H), and Cav3.3 (α1I), with IC50 values of 31.0, 83.1, and 69.3 µM, respectively. This compound exhibits significant cytotoxic activity against A549 and HCT-116 cancer cell lines, with IC50 values of 5.0 and 6.4 µM. It serves as a useful tool in the investigation of calcium channel involvement in various physiological processes and potential therapeutic targets in cancer research. -
Calcium Channel Antagonist
Flosatidil is an orally active calcium channel antagonist that effectively inhibits calcium influx through L-type calcium channels. Its primary biological activities include antianginal and antihypertensive effects, making it a valuable compound for cardiovascular research. Flosatidil is utilized in studies investigating the modulation of vascular tone and cardiac output, contributing to the understanding of hypertension and angina management. -
Calcium Channel Antagonist
Lomerizine is an antagonist of L- and T-type voltage-gated calcium channels, primarily inhibiting calcium influx into cells. This activity is associated with its potential to modulate vascular smooth muscle contraction and neurotransmitter release. Lomerizine is utilized in research to investigate cardiovascular diseases and neurological disorders related to calcium channel dysregulation. -
Anti-inflammatory Agent
LQFM020 is an orally active pyrazole derivative that functions as an anti-inflammatory agent. It effectively inhibits calcium channels while activating potassium and nitric oxide/cGMP pathways, leading to reduced vasoconstriction. LQFM020 exhibits significant anti-inflammatory and analgesic properties, making it a valuable reagent for research focused on inflammation and pain mechanisms. -
Ca2+‑ATPase Inhibitor
rel-(E)-6,7-Transdihydroxyligustilide is a potent inhibitor of Ca2+-ATPase, specifically in calmodulin-deficient human erythrocyte membranes. This compound, derived from the dried tuberous roots of Polygonum multiflorum, plays a significant role in the regulation of calcium homeostasis. It is particularly valuable in research related to hyperlipidemia and related metabolic disorders. -
Calcium Channel
Levamlodipine (gentisate) is a potent calcium channel blocker primarily employed for its antihypertensive and antianginal effects. This pharmacologically active amino ester exhibits significant biological activity by inhibiting calcium influx into cardiovascular cells, thereby reducing blood pressure and alleviating angina. Additionally, high enantiomeric purity can be assessed through fast capillary electrophoresis, yielding a resolution of 9.8, which underscores its utility in compound analysis and development within chemical research. -
Isotope-Labeled Compounds
Verapamil-d7 is a deuterium-labeled derivative of Verapamil, a calcium channel blocker and a potent inhibitor of the P-glycoprotein (P-gp) transporter. This isotope-labeled compound is utilized in pharmacokinetic studies and metabolic research, providing insights into drug interactions and transport mechanisms. Its applications extend to investigating conditions such as hypertension, cardiac arrhythmias, and angina, making it a valuable tool in cardiovascular research.
