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Catalog No.
Product Name
Application
Product Information
Citations
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LTA4H Inhibitor
JNJ-40929837 succinate is a selective and orally active inhibitor of leukotriene A4 hydrolase (LTA4H). This compound effectively inhibits aminopeptidase activity, leading to the accumulation of Pro-Gly-Pro in serum. JNJ-40929837 succinate is particularly relevant for asthma research, providing a valuable tool for investigating inflammatory pathways and potential therapeutic interventions in respiratory conditions. -
Leukotriene Receptor Inhibitor
(R)-Ontazolast is a potent leukotriene receptor inhibitor that effectively blocks leukotriene biosynthesis. It demonstrates a remarkable IC50 value of 0.001 µM in human polymorphonuclear leukocytes, inhibiting the release of arachidonic acid. This compound is valuable for research applications related to inflammation and immune response modulation. -
Leukotriene B4 Inhibitor
Chamazulene is a natural compound that acts as an inhibitor of leukotriene B4 formation. Its antioxidant properties contribute to modulating inflammatory responses, making it relevant for research in inflammation and immune response studies. Chamazulene is particularly useful in exploring pathways related to leukotriene signaling and its role in various pathologies. -
Leukotriene Inhibitor
FK-664 is a potent leukotriene inhibitor that enhances ventricular contractility and reduces the time to peak tension in cardiac cells. In canine models of heart failure, FK-664 has been shown to decrease mean circulating pressure (MCP), indicating its potential therapeutic effects. This compound is valuable for research focused on cardiovascular diseases, particularly heart failure, and its underlying mechanisms. -
Leukotriene Receptor/FLAP Inhibitor
(S)-Veliflapon is a potent inhibitor of leukotriene biosynthesis targeting the 5-lipoxygenase activating protein (FLAP). It effectively inhibits the formation of leukotriene B4 (LTB4) in rat, mouse, and human leukocytes with IC50 values of 0.026 µM, 0.039 µM, and 0.22 µM, respectively. Additionally, (S)-Veliflapon demonstrates enantioselectivity in human whole blood, making it a valuable reagent for research in inflammation and related biological processes. -
Leukotriene Biosynthesis Inhibitor
L-691678 is an inhibitor of leukotriene biosynthesis that selectively binds to the 5-lipoxygenase-activating protein (FLAP). This compound disrupts leukotriene production, making it a valuable tool for investigating leukotriene-associated pathologies, including allergic responses, asthma, and inflammatory conditions. Its ability to modulate leukotriene levels provides insights into their role in various biological processes and disease mechanisms. -
Leukotriene Biosynthesis Inhibitor
ABT-080 is an orally active inhibitor of leukotriene biosynthesis, specifically targeting the pathways responsible for the production of LTB4 and LTC4. This compound effectively prevents bronchoconstriction, making it valuable for research into asthma and related inflammatory conditions. By selectively inhibiting leukotriene synthesis without affecting PGH2 biosynthesis, ABT-080 provides a critical tool for studying the role of leukotrienes in respiratory diseases. -
LTB4 Inhibitor
Ontazolast is a potent inhibitor of leukotriene B4 (LTB4) biosynthesis, making it a valuable tool for studying inflammatory pathways. Its primary mechanism targets the LTB4 synthesis pathway, which is associated with various inflammatory conditions. Ontazolast is particularly relevant in research applications focused on asthma and related respiratory disorders. -
Leukotriene Receptor Inhibitor
Bunaprolast is a potent leukotriene receptor inhibitor that effectively reduces LTB4 production in human whole blood. Additionally, it demonstrates significant inhibition of lipoxygenase activity and TXB2 release. This compound is valuable for research applications related to inflammatory diseases and respiratory conditions. -
Leukotriene Receptor Inhibitor
LTB4-IN-1 is a selective leukotriene receptor inhibitor, effectively blocking leukotriene B4 synthesis with an IC50 of 70 nM. This compound serves as a valuable tool for research in inflammation and immune response, potentially aiding in the investigation of leukotriene-mediated pathophysiological conditions. Its application can extend to studies focused on cellular signaling and therapeutic interventions targeting leukotriene pathways. -
Spns2 Inhibitor
SLF1081851 is a selective inhibitor of Spns2, effectively inhibiting sphingosine-1-phosphate (S1P) release with an IC50 of 1.93 μM. This compound is crucial for studying developmental processes and immune responses, making it a valuable tool in research focused on modulating these biological pathways. Its ability to target Spns2 provides insight into the mechanisms regulating S1P availability and its subsequent effects on cell signaling and function. -
Spns2 Inhibitor
SLF80821178 is a potent inhibitor of the Sphingosine-1-Phosphate Transporter (Spns2), exhibiting an IC50 of 51 nM for the inhibition of S1P release in HeLa cells. This orally active compound demonstrates a half-life of 2.4 hours in mouse models. Research applications include the investigation of sphingosine metabolism and transport in cellular signaling pathways. -
S1P Lyase Inhibitor
2-Acetyl-4-tetrahydroxybutyl imidazole is a potent inhibitor of sphingosine-1-phosphate (S1P) lyase, demonstrating significant biological activity in vivo. This compound is useful for investigating the role of S1P metabolism in various physiological and pathological processes. Research applications include studying cell signaling pathways and exploring therapeutic targets in diseases related to S1P dysregulation. -
LPL Receptor Inhibitor
S1PR1 modulator 1 is a selective inhibitor of the S1PR1 receptor, demonstrating a pIC50 of 7.6 and exhibiting greater than 40-fold selectivity over S1PR2 and over 80-fold selectivity over S1PR3 and S1PR4. This compound is valuable for investigating S1PR1-mediated signaling pathways and its role in various biological processes, including immune response regulation and cardiovascular function. Its specificity makes it an important tool for research applications focused on the modulation of S1P receptor activity in disease models. -
Autotaxin Inhibitor
CRT0273750 is an inhibitor of autotaxin (ATX), which plays a crucial role in the modulation of lysophosphatidic acid (LPA) levels, exhibiting an IC50 of 0.014 μM. This compound is valuable in the study of ATX/LPA-dependent cancer models, contributing to research on tumor progression and metastasis. Its specificity for ATX provides a useful tool for elucidating the underlying mechanisms of LPA-mediated signaling pathways in various biological contexts. -
S1PL Inhibitor
LX2931 is an inhibitor of Sphingosine 1-Phosphate Lyase (S1PL), which functions by elevating levels of Sphingosine 1-Phosphate (S1P) both intracellularly and extracellularly. This inhibition results in a marked increase in S1P concentrations in lymphoid tissues, potentially leading to restricted lymphocyte trafficking from secondary immune sites and contributing to lymphocytopenia and immunosuppressive effects in the peripheral circulation. LX2931 is valuable for research in autoimmune disease studies, particularly in the context of rheumatoid arthritis. -
S1PL Inhibitor
A6770 is a potent inhibitor of sphingosine 1-phosphate lyase (S1PL), an enzyme involved in sphingolipid metabolism. As an orally active compound, A6770 is phosphorylated to exert direct inhibitory effects on S1PL, leading to an increase in [3H]dhS1P levels. This reagent is valuable for research applications focused on sphingolipid signaling pathways and their roles in various biological processes. -
S1PR5 Antagonist, S1PR5 Inhibitor
S1PR5-IN-1 is a selective antagonist of the sphingosine-1-phosphate receptor 5 (S1PR5), exhibiting an IC50 of 85.4 nM in human assays and a binding affinity (Ka) of 2.173 nM. This orally bioavailable inhibitor effectively impedes the migration of natural killer cells towards sphingosine-1-phosphate. S1PR5-IN-1 is a valuable tool for research applications related to multiple sclerosis and other conditions involving S1PR5 signaling pathways. -
Spns2 Inhibitor
SLB1122168 is a selective inhibitor of Spns2 that significantly impairs the release of sphingosine-1-phosphate (S1P) with an IC50 of 94 nM. This compound is useful for investigating the role of S1P in various biological processes, including immune response and cardiovascular regulation. Its application in research can help elucidate the mechanisms underlying Spns2 activity and S1P signaling pathways. -
Sphingosine-1-phosphate Lyase Inhibitor
S1PL-IN-1 is a selective sphingosine-1-phosphate lyase inhibitor with an IC50 of 210 nM. This compound exhibits potential in modulating S1P signaling pathways and may serve as a Smoothened receptor antagonist with an IC50 of 440 nM. S1PL-IN-1 is primarily utilized in the study of experimental autoimmune encephalomyelitis and related neurological disorders. Its capacity to influence sphingolipid metabolism makes it a valuable tool for research into neuroinflammatory conditions. -
Spns2 Inhibitor
SLF1081851 TFA is a selective inhibitor of Spns2, effectively inhibiting sphingosine-1-phosphate (S1P) release with an IC50 of 1.93 μM. This compound is instrumental in studies related to developmental biology and immune regulation. Its ability to modulate S1P levels makes it a valuable tool for investigating pathways involved in immune responses and developmental processes. -
hS1PL Inhibitor
RBM10-8 is an irreversible inhibitor of recombinant human sphingosine-1-phosphate lyase (hS1PL). This compound modulates the sphingosine-1-phosphate (S1P) signaling pathway, which plays a critical role in regulating various biological processes including cell proliferation, differentiation, angiogenesis, and immune responses. RBM10-8 is valuable for research applications focused on inflammation and developmental biology, providing insights into the therapeutic potential of targeting S1P-related pathways. -
Spns2 Inhibitor
SLF80821178 hydrochloride is a selective inhibitor of the sphingosine-1-phosphate transporter (Spns2), effectively reducing sphingosine-1-phosphate (S1P) release in HeLa cells with an IC50 value of 51 nM. This compound demonstrates the capability to decrease circulating lymphocyte levels in mice without altering plasma S1P concentrations, making it a valuable tool for studying immune response and signaling pathways. Research applications include investigations into lymphocyte trafficking and potential therapeutic strategies targeting sphingosine metabolism. -
Spns2 Inhibitor
SLF1081851 hydrochloride is a potent inhibitor of Spns2, effectively suppressing sphingosine-1-phosphate (S1P) release with an IC50 of 1.93 μM. This compound is significant for research into immune system development and related biological processes. It serves as a valuable tool for investigating the role of S1P in various cellular functions and pathological conditions. -
SPL Inhibitor
SPL-IN-1 is a selective sphingosine-1-phosphate lyase inhibitor that targets the SPL enzyme. It has demonstrated significant biological activity in modulating sphingolipid metabolism and influencing cellular signaling pathways. This compound is valuable for research applications involving inflammation, cancer progression, and other diseases associated with sphingosine-1-phosphate signaling dysregulation. -
S1PL Inhibitor
S1PL-IN-2 is a potent sphingosine-1-phosphate lyase (S1PL) inhibitor with an IC50 of 120 nM. It effectively inhibits S1PL activity by blocking the conversion of Vitamin B6 into the active cofactor pyridoxal-4-phosphate, which is essential for S1P lyase function. This compound is valuable for research in inflammation and immunology, with potential applications in studying conditions such as rheumatoid arthritis. -
LPA Inhibitor
L-NASPA ammonium is an effective LPA inhibitor that targets lysophosphatidic acid signaling pathways. It is utilized in research focused on platelet activation and related cellular processes. By inhibiting LPA, this compound aids in elucidating the mechanisms underlying platelet function and potential therapeutic interventions in related disorders. -
SPNS2 Inhibitor
Spns2-IN-3 is a selective SPNS2 inhibitor that targets sphingolipid metabolism. This compound exhibits significant biological activity in modulating sphingolipid pathways, making it crucial for research applications involving cellular signaling and lipid biology. Its unique structure may facilitate the development of drug carriers, enhancing the delivery and penetration of therapeutic molecules across biological membranes, particularly in dermatological settings. -
LPA Inhibitor
L-NASPA is a potent lysophosphatidic acid (LPA) inhibitor that plays a significant role in research related to platelet activation. By blocking LPA signaling pathways, L-NASPA enables the investigation of its effects on cellular processes involved in thrombosis and inflammation. This compound is valuable for studies aimed at understanding the physiological and pathological roles of LPA in various biological contexts. -
Dopamine Receptor Inhibitor
SV 293 is a selective antagonist that primarily targets dopamine D2 receptors with a binding affinity that is 100-fold greater than that of D3 and D4 receptor subtypes. This compound exhibits neutral antagonist activity and effectively blocks the effects of the full agonist quinpirole in forskolin-dependent adenylate cyclase inhibition assays and electrophysiological assays. SV 293 serves as a valuable pharmacological tool for investigating the role of D2-like receptor subtypes in dopamine-related pathways associated with neurological, neuropsychiatric, and movement disorders. -
Dopamine Uptake Inhibitor
GBR-12879 dihydrochloride is a potent dopamine uptake inhibitor that selectively targets the dopamine transporter. Its primary mechanism involves preventing the reabsorption of dopamine, thus enhancing dopaminergic signaling. This compound is widely utilized in research to investigate the role of dopamine in neurological disorders and to explore potential therapeutic strategies for conditions such as depression and schizophrenia. -
DAT/NET/SERT Inhibitor
Amitifadine is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) that targets the dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT). It exhibits inhibitory concentrations of 12 nM for serotonin, 23 nM for norepinephrine, and 96 nM for dopamine in HEK 293 cells. This compound is pertinent for research applications exploring the modulation of monoaminergic systems and investigating potential therapeutic effects in mood disorders. -
ETA Inhibitor
Diosuxentan is a selective inhibitor of the endothelin A (ETA) receptor. It demonstrates significant biological activity in suppressing vascular responses associated with endothelin-1, making it relevant for studies investigating cardiovascular, renal, and neuroinflammatory conditions. Diosuxentan provides valuable insights for research focused on the therapeutic modulation of ETA-mediated pathways. -
Endothelin converting enzyme inhibitor
Daglutril targets the endothelin receptor, exhibiting the ability to modulate cytokine-induced endothelin-1 production in astrocytes. Its inhibitory effects on endothelin-1 generation make it a valuable research tool for screening compounds that regulate this peptide's synthesis in glial cells. This compound is particularly relevant for studies investigating the role of endothelin-1 in neuroinflammation and related neurological disorders. -
Platelet Aggregation Inhibitor
Cloricromen hydrochloride is a potent platelet aggregation inhibitor that effectively targets and modulates platelet activation pathways. This compound has demonstrated the ability to inhibit platelet aggregation in both human and experimental thrombosis models, making it a valuable reagent for research into cardiovascular diseases and thrombotic disorders. Cloricromen hydrochloride is suitable for studies focused on the mechanisms of platelet function and the development of antithrombotic therapies. -
Platelet Aggregation Inhibitor
KP-10614 is a potent, orally active inhibitor of platelet aggregation, primarily targeting ADP-induced aggregation with an IC50 of 1 nM. This compound exhibits dose-dependent inhibition of ex vivo platelet aggregation in rat models. KP-10614 demonstrates significant antithrombotic effects across various thrombosis models, making it a valuable tool for research into thrombotic diseases. -
5-HT/Norepinephrine Reuptake Inhibitor
Desvenlafaxine is a selective 5-HT and norepinephrine reuptake inhibitor, primarily targeting the serotonin transporter (hSERT) and norepinephrine transporter (hNET) with IC50 values of 47.3 nM and 531.3 nM, respectively. This orally active compound effectively penetrates the blood-brain barrier, making it applicable in the treatment of major depressive disorders. Additionally, Desvenlafaxine exhibits weak binding affinity to the human dopamine transporter, with 62% inhibition observed at 100 μM, which may have implications for its overall pharmacological profile. -
Dopamine Receptor Inhibitor
Fluphenazine dihydrochloride is a potent dopamine receptor antagonist primarily targeting dopamine D2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This phenothiazine derivative also exhibits the ability to inhibit neuronal voltage-gated sodium channels. Its key biological activities include the suppression of Methylphenidate-induced stereotyped behaviors and climbing in murine models. Fluphenazine dihydrochloride is widely utilized in research related to psychosis, diabetic peripheral neuropathy, and may also have implications for the inhibition of SARS-CoV-2. -
Platelet Aggregation Inhibitor
Prostaglandin I3 sodium is a potent inhibitor of platelet aggregation, primarily acting through the stimulation of adenylate cyclase, which increases cyclic AMP levels in platelets. This compound also exhibits vasodilatory properties, making it useful in studies related to cardiovascular health and thrombotic disorders. Its applications include research into the modulation of vascular tone and the prevention of platelet-related complications in various disease models. -
Platelet Aggregation Inhibitor
Evategrel is a potent platelet aggregation inhibitor that primarily targets ADP receptors on platelets. This compound effectively reduces thrombus formation, making it useful for research in cardiovascular diseases and the study of clotting mechanisms. Its ability to modulate platelet activity supports investigations into antiplatelet therapies and their applications in preventing thrombotic events. -
CCR5/CXCR4 Chemotaxis Inhibitor
Catenarin, an anthraquinone compound, serves as an inhibitor of CCR5 and CXCR4-mediated chemotaxis. It effectively reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), as well as calcium mobilization. Catenarin demonstrates anti-inflammatory properties and inhibits leukocyte migration, contributing to its potential in diabetes research. Additionally, it exhibits significant antibacterial activity against Gram-positive bacteria and has been shown to prevent type 1 diabetes in nonobese diabetic mice. -
CXCR5 Inhibitor
YU241279 is a selective inhibitor of CXCR5, targeting the CXCL13-mediated signaling pathways. It effectively inhibits Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells, leading to reduced proliferation of lymphoma cells. In preclinical studies, YU241279 demonstrated a significant reduction in tumor burden within the peripheral blood and bone marrow of mice with lymphoma. This compound is suitable for research into angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma. -
β-Glucuronidase Inhibitor
β-Glucuronidase-IN-5 is a selective inhibitor of β-glucuronidase with an IC50 value of 39.8 μM. This compound demonstrates low cytotoxicity in PC-3 cells, with an IC50 greater than 30 μM, and shows no affinity for adenosine receptors A₁ and A₂A. β-Glucuronidase-IN-5 is useful for investigating diseases associated with overexpression of β-glucuronidase, including colon cancer, arthritis, and complications related to AIDS. -
PAFAH1b2/1b3 Inhibitor
P11 is a selective inhibitor of platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3, demonstrating significant impairment of cancer cell survival. With IC50 values of approximately 40 nM for PAFAH1b2 and 900 nM for PAFAH1b3, P11 is a valuable tool for investigating the role of these enzymes in cancer biology and related research applications, including studies focused on cell proliferation and apoptosis. -
DA/NE/5-HT Inhibitor
Tesofensine is a triple monoamine reuptake inhibitor targeting dopamine (DA), norepinephrine (NE), and serotonin (5-HT). It effectively inhibits the reuptake of these neurotransmitters in the synaptic cleft, exhibiting IC50 values of 6.5 nM for DA, 1.7 nM for NE, and 11 nM for 5-HT. Tesofensine is primarily studied for its potential as an anti-obesity agent and may be useful in related central nervous system research applications. -
MAO-A And 5-HT-uptake Inhibitor
Sercloremine hydrochloride is a selective and reversible inhibitor of monoamine oxidase A (MAO-A) and serotonin (5-HT) uptake. This compound is primarily utilized in research related to depression, offering insights into the modulation of serotonin levels and its effects on mood regulation. Its dual mechanism of action makes it valuable for exploring therapeutic approaches in depressive disorders. -
5-HT Reuptake Inhibitor
Clomipramine is a potent 5-HT reuptake inhibitor with an IC50 value of 1.5 nM. As a tricyclic antidepressant, it is primarily utilized in research investigating the mechanisms of depression and obsessive-compulsive disorder (OCD). Its ability to influence serotonin levels makes it a valuable tool for studying various neuropsychiatric conditions. -
5-HT/NE Reuptake Inhibitor
Dextromilnacipran is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor, derived from the enantiomeric form of milnacipran. This compound also functions as a human alpha-adrenergic receptor antagonist, exhibiting an IC50 value of 3.4 μM. Dextromilnacipran is primarily utilized in research applications targeting mood disorders and neuropharmacology, facilitating investigations into its psychiatric and physiological effects. -
5-HT Transporter Inhibitor
6-Nitroquipazine is a highly potent and selective inhibitor of the serotonin transporter (5-HT transporter), exhibiting a Ki value of 0.17 nM. This compound significantly impacts serotonin reuptake, making it a valuable tool for investigating the pathophysiology and treatment of psychiatric disorders, including depression. Its ability to modulate serotonin levels can be instrumental in research aimed at understanding mood regulation and therapeutic interventions in related conditions. -
Vesicular Acetylcholine Transport Inhibitor
(±)-Vesamicol hydrochloride is a potent inhibitor of vesicular acetylcholine transport, exhibiting a Ki value of 2 nM. Additionally, it demonstrates a high affinity for σ1 and σ2 receptors, with Ki values of 26 nM and 34 nM, respectively. This compound is valuable for research into cholinergic signaling and receptor interactions, facilitating studies on neurological disorders and synaptic transmission mechanisms.
