Catalog No.
Product Name
Application
Product Information
Citations
-
S1P1/S1P5 Agonist
AMG 369 is a potent, orally bioavailable dual agonist of the sphingosine-1-phosphate receptors S1P1 and S1P5, with minimal activity at S1P3 and no affinity for S1P2 or S1P4. This compound effectively reduces blood lymphocyte counts, demonstrating its immunomodulatory effects. AMG 369 has been shown to delay the onset and diminish the severity of experimental autoimmune encephalomyelitis in rat models, making it a valuable tool for research into autoimmune diseases and inflammatory responses. -
S1P1 Receptor Agonist
BMS-960 free base is a potent and selective agonist of the S1P1 receptor, featuring an isoxazole structure. This compound demonstrates significant biological activity in modulating immune responses and has potential applications in the study of immune and vascular diseases. BMS-960 free base is a valuable tool for researchers investigating the therapeutic implications of S1P1 receptor modulation. -
S1P1 Agonist
S1P1 agonist 6 is a selective S1P1 receptor agonist that modulates immune responses by inhibiting lymphocyte trafficking. This compound exhibits notable immunosuppressive activity, making it a valuable tool for the investigation of autoimmune diseases. Research applications include studying mechanisms of autoimmunity and evaluating potential therapeutic interventions for related disorders. -
LPA1/LPA3 Antagonist
VPC12249 is a competitive dual antagonist of LPA1 and LPA3, exhibiting Ki values of 137 nM and 428 nM, respectively. It effectively inhibits calcium mobilization in HEK293T cells with a Ki of approximately 130 nM. This compound is useful for investigating the roles of LPA receptors in ovarian cancer and hypertensive diseases, providing valuable insights into potential therapeutic strategies. -
S1P1 Antagonist
W123 is an S1P1 receptor antagonist derived from FTY720. This compound exhibits significant biological activity by inhibiting GTPĪ³S activation, MAPK recruitment, and cell migration while also promoting ligand-induced receptor internalization. W123 is valuable for research applications focused on sphingosine 1-phosphate signaling pathways and their role in various physiological and pathological processes. -
S1P1 Receptor Agonist Prodrug
GSK1842799 is an orally active prodrug that selectively targets the S1P1 receptor. Its primary mechanism involves agonistic activity that modulates immune cell trafficking and is of particular interest in the study of multiple sclerosis. This compound is valuable for research focused on autoimmune diseases and neurological disorders. -
S1P1 Agonist
TC-SP 14 is a potent and orally active S1P1 agonist, exhibiting an EC50 of 0.042 Ī¼M, while demonstrating minimal activity at S1P3 with an EC50 of 3.47 Ī¼M. This compound significantly reduces blood lymphocyte counts and attenuates delayed type hypersensitivity (DTH) responses upon antigen challenge. TC-SP 14 is valuable for research focusing on immune modulation and the therapeutic potential in autoimmune diseases. -
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. -
S1P Modulator
RP-1859 is a sphingosine 1-phosphate (S1P) modulator that exhibits anti-inflammatory and immunomodulatory properties. This compound is particularly relevant in the study of iatrogenic autoimmune colitis, facilitating investigations into the underlying mechanisms of this condition and potential therapeutic interventions. RP-1859's modulation of S1P signaling pathways may provide valuable insights into inflammatory responses and immune regulation. -
S1P/S1PR Signaling Axis Modulator
LX2932 is an orally active modulator of the sphingosine 1-phosphate (S1P) signaling axis, impacting S1PR receptor activity. It demonstrates a dose-dependent reduction in circulating lymphocyte populations, which may aid in the treatment of autoimmune disorders. LX2932 has shown efficacy in improving collagen-induced arthritis, making it a valuable compound for research in immunology and inflammatory disease models. -
S1P1 Agonist
S1P1 agonist 6 hemicalcium is a selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1), primarily functioning to inhibit lymphocyte trafficking. This mechanism results in the reduction of autoimmune responses, making it a valuable tool for studying various autoimmune diseases. Its immunosuppressive properties allow researchers to investigate potential therapeutic applications in immune modulation and related research areas. -
LPA Receptor Agonist
2ccPA sodium is a potent lysophosphatidic acid (LPA) receptor agonist. By activating LPA receptors and inhibiting the activity of the autotaxin (ATX) enzyme, it plays a significant role in regulating cell proliferation, migration, and apoptosis. This compound is valuable for research into various biological processes and disease states, including cancers, inflammation, and fibrosis. -
S1P1 Receptor Agonist
BMS-960 is a potent and selective agonist of the S1P1 receptor. It has been demonstrated to modulate immune responses and improve vascular function, making it a valuable tool in the study of immune and vascular diseases. Research applications include exploring pathways related to inflammation, lymphocyte trafficking, and cardiovascular health. -
S1P4 Receptor Antagonist
CYM50358 hydrochloride is a potent and selective antagonist of the sphingosine-1-phosphate 4 (S1P4) receptor. This compound exhibits significant biological activity by inhibiting S1P4-mediated signaling pathways, making it a valuable tool in research focused on the immune response and inflammation. Its application extends to the study of influenza infection, facilitating investigations into viral pathogenesis and potential therapeutic interventions. -
S1PR1 Agonist
S1PR1 Agonist 1 is a potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), a member of the G protein-coupled receptor family. This compound modulates cellular signaling pathways linked to immune response and inflammation, making it a valuable tool for investigating autoimmune diseases. Its application extends to research focused on understanding the role of sphingolipid signaling in various physiological and pathological conditions. -
S1PR1 Agonist
RP101442 is a selective and potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 of 2.6 nM. Additionally, it shows activity toward S1PR5 with an EC50 of 171 nM. This compound is primarily utilized in research exploring immune responses and neuroprotection, making it valuable for studies on inflammatory diseases and related therapeutic areas. -
S1PR1 Agonist
S1PR1 Agonist 2 is a potent agonist targeting the S1P receptor 1 (S1PR1). This compound, derived from sphingosine-1-phosphate (S1P), engages G protein-coupled receptors, influencing various physiological processes. S1PR1 Agonist 2 is primarily utilized in research studies focused on autoimmune diseases, facilitating the exploration of therapeutic strategies in this area. -
S1P5 Receptor Antagonist
S1P5 receptor antagonist 1 is a selective antagonist targeting the S1P5 receptor, characterized by an EC50 of 0.1 nM and a Ki of 4.4 nM. This compound is capable of inhibiting the migration of natural killer cells towards sphingosine 1-phosphate in vitro, while leaving T cell migration unaffected. S1P5 receptor antagonist 1 is employed in research focused on central nervous system diseases, providing insights into the modulation of immune responses within the brain. -
LPAR1 Antagonist
LPAR1 Antagonist 2 is a selective antagonist of the lysophosphatidic acid receptor 1 (LPAR1), demonstrating an average IC50 of 130 nM. This compound is utilized in research to investigate the role of LPAR1 in various physiological and pathological processes, including cancer progression and neurodegenerative diseases. Its inhibition of LPAR1 signaling makes it a valuable tool for studying receptor-mediated pathways and developing therapeutic strategies targeting this receptor. -
LPAR1 antagonist
BMT-136088 is an LPAR1 antagonist that effectively inhibits the activity of the lysophosphatidic acid receptor 1. This compound can be utilized as a positron emission tomography (PET) radioligand for the quantitative assessment of specific binding to LPA1 in lung tissues. Its application in research can enhance the understanding of LPAR1ās role in various biological processes and pathological conditions. -
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. -
LPA Receptor Antagonist
LPA Receptor Antagonist-1 functions as a selective antagonist of lysophosphatidic acid (LPA) receptors, which play a crucial role in various cellular signaling pathways. This compound demonstrates significant biological activity by inhibiting LPA-mediated responses, making it a valuable tool for research into cellular processes related to cancer, fibrosis, and neurodegenerative diseases. Researchers can utilize LPA Receptor Antagonist-1 to investigate the implications of LPA signaling in multiple biological contexts. -
S1PR1 ligand
S1PR1 ligand 1 is a specific agonist targeting the S1PR1 receptor with an IC50 of 8.7 nM. This compound demonstrates favorable brain permeability, making it suitable for exploring S1PR1 functions in neurological disorders. Additionally, S1PR1 ligand 1 can be labeled with 18F for imaging studies, facilitating research into its role in brain pathologies. -
S1P1 Receptor Agonist
ACT-209905 is an agonist of the S1P1 receptor, demonstrating potent inhibition of glioblastoma (GBM) cell growth and migration. In addition to its antitumor properties, ACT-209905 exhibits immunomodulating activity, making it a valuable tool for investigating autoimmune diseases. This compound is suitable for research applications aimed at elucidating the roles of S1P1 signaling in cancer and immune regulation. -
S1P1 Receptor Partial Agonist
BMS-986104 hydrochloride is a selective partial agonist of the S1P1 receptor, involved in modulating sphingosine-1-phosphate signaling pathways. This compound exhibits potential therapeutic effects in the context of autoimmune diseases by influencing lymphocyte trafficking and immune response. It serves as a valuable tool for research aimed at understanding and developing treatments for various autoimmune disorders. -
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. -
Antispasmodic Opioid Alkaloid
Pargeverine hydrochloride is an antispasmodic opioid alkaloid that primarily targets muscarinic cholinergic receptors, exhibiting a moderate and non-selective blockade. This compound is utilized in research to investigate mechanisms underlying painful spasms and their management. Its application in understanding muscle contraction and relaxation makes it a valuable reagent in pharmacological studies. -
M1 Muscarinic Agonist
McN-A-343 is a selective M1 muscarinic agonist that enhances muscarinic transmission in sympathetic ganglia. This compound significantly inhibits muscarine-induced catecholamine secretion in isolated perfused rat adrenal glands and plays a role in neuronal firing regulation. Additionally, McN-A-343 activates enteroendocrine L cells to promote the release of glucagon-like peptide 1 (GLP-1) and modulates Ī±-melanocyte stimulating hormone (Ī±-MSH) secretion from the pituitary gland. Its capacity to reduce colonic inflammation and oxidative stress makes McN-A-343 a valuable tool for studying ulcerative colitis. -
mAChR Antagonist
4-Piperidyl N-(2-biphenyl)carbamate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting notable selectivity for the M2 and M3 subtypes. With pKi values of 7.33 for M2 and 7.51 for M3, this compound demonstrates a markedly higher affinity compared to Ī²2 adrenergic receptors, which has a pKi of 4.94. This specificity makes it a valuable tool for research into mAChR-related signaling pathways and potential therapeutic applications in various neurological disorders. -
DRD4 Antagonist
PD 168568 is a potent and orally active antagonist of the dopamine receptor D4 (DRD4), featuring an isoindolinone structure. It demonstrates strong selectivity for the D4 receptor over D2 and D3 receptors, with Ki values of 8.8 nM, 1842 nM, and 2682 nM, respectively. This compound is valuable for research applications focusing on glioblastoma (GBM), providing insights into the role of DRD4 in tumor biology. -
D3R Antagonist
PF-04363467 is a selective antagonist of the dopamine D3 receptor (D3R). It demonstrates dose-dependent modulation of the electroencephalogram (EEG) profile in freely moving rats, highlighting its potential to influence neural activity. This compound effectively reduces opioid drug-seeking behavior while minimizing undesired side effects associated with D2 receptor antagonism. PF-04363467 is valuable for research into addiction, cognitive disorders, and mental illness. -
Haloperidol Analogue
UCSF34 is a Haloperidol analogue that selectively binds to the human D2L receptor, exhibiting an estimated pKi of 7.49. This compound is significant for its potential applications in schizophrenia research, facilitating the investigation of dopamine receptor modulation and related therapeutic strategies. -
Dopamine Receptor Antagonist
Seridopidine is a potent dopamine receptor antagonist that primarily targets D2 and D3 receptors. It exhibits significant antipsychotic activity, making it valuable for research in neurological and psychiatric disorders. This compound is useful in studies investigating the roles of dopamine in the central nervous system, particularly in understanding mechanisms underlying schizophrenia and related conditions. -
Dopamine D2 Receptor Agonist
U 101958 is a potent full agonist of the dopamine D4 receptor, exhibiting a pEC50 of 8.7 in HEK293 cells expressing the D4 receptor. This compound demonstrates significant biological activity and is valuable for research in neuropharmacology, particularly in studies examining the role of dopamine signaling in psychiatric disorders. Its selectivity for the D4 receptor can aid in the exploration of D4-mediated effects in various biological systems. -
Dopamine Receptor
Quinagolide is a non-ergot dopamine D(2) receptor agonist that enhances dopamine activity. It is primarily utilized in the modulation of endocrine function, particularly in the suppression of hyperprolactinemia and its associated clinical symptoms. Quinagolide's significant biological activity makes it a valuable reagent for research in endocrine disorders and drug development, facilitating the study of dopamine's role in various physiological processes. -
D3R Ligand
D3R ligand 1 is a potent and selective antagonist targeting the dopamine receptor D3R, with a Ki value of 66 nM. Utilizing a THPB template, this compound effectively inhibits both G-protein- and Ī²-arrestin-mediated signaling pathways. D3R ligand 1 is valuable for researchers investigating dopamine receptor signaling and its implications in neuropharmacology. -
D2R Agonist
UNC9975 is a D2 receptor (D2R) agonist that demonstrates signaling bias through Ī²-arrestin-mediated pathways while also acting as an antagonist of Gi-regulated cAMP production and a partial agonist for D2R/Ī²-arrestin-2 interactions. This compound is valuable for research in antipsychotic drug development, facilitating the exploration of novel therapeutic approaches targeting dopaminergic signaling. -
Dopamine D1 Receptor Agonist
Zelandopam free base is a specific agonist of the dopamine D1 receptor, demonstrating notable renal vasodilatory effects. This compound is effective in mitigating acute renal failure induced by Cisplatin, making it a valuable tool for research investigating renal protection and dopamine receptor signaling. Its oral bioactivity further enhances its utility in pharmacological studies related to renal function and neurotransmitter interactions. -
D3 Dopamine Receptor Agonist
7-Hydroxy-DPAT is a selective agonist of the D3 dopamine receptor, known for its ability to modulate locomotor behavior and influence dopamine metabolism in the brain. This compound demonstrates significant pharmacological activity that can be utilized in research focused on neurological diseases and disorders. Its selectivity for the D3 receptor makes it a valuable tool for studies investigating dopamine-related pathways and their implications in various neurological conditions. -
D3R Agonist
OS-3-106 is a potent and selective agonist of the dopamine D3 receptor (D3R), demonstrating a high binding affinity with a Ki value of 0.2 nM. This compound serves as a valuable tool in the study of D3R-mediated pathways, particularly in the context of psychoactive substance addiction research. Its specificity and efficacy make it suitable for exploring mechanisms underlying dopamine signaling and addiction-related behaviors. -
Dopamine D2 Receptor Agonist
PF-00217830 is a selective agonist of the dopamine D2 receptor, demonstrating substantial efficacy in modulating dopaminergic signaling. It has been shown to inhibit spontaneous locomotor activity as well as reduce 2,5-dimethoxy-4-iodoamphetamine-induced head twitches in rodent models. This compound is valuable for studying the role of dopamine in neuropharmacology and assessing potential therapeutic strategies for disorders associated with dopamine dysregulation. -
Dopamine D2 Receptor Antagonist
Dopamine D2 receptor antagonist-3 is a selective antagonist of the dopamine D2 receptor, displaying a pIC50 of 5.52. This compound demonstrates antipsychotic effects, evidenced by its ability to reduce apomorphine-induced agitation in rat models. It is a valuable tool for research into psychiatric and neurological disorders, facilitating the study of dopaminergic signaling pathways and potential therapeutic interventions. -
D4 dopamine receptor antagonist
L-750667 triHydrochloride is a selective antagonist of the D4 dopamine receptor, exhibiting a Ki value of 0.51 nM. Its radiolabeled derivative, [125I]L-750667, demonstrates a Kd of 0.16 nM for D4 receptor binding. This compound is capable of reversing dopamine-induced inhibition of cAMP accumulation, making it a valuable tool for investigating the distribution and function of D4 dopamine receptors in the central nervous system. L-750667 triHydrochloride has significant applications in neuroscience and psychiatry research. -
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 Receptor
LY 171859 is a selective D2 receptor agonist that also displays notable reductase activity. This compound demonstrates enzymatic function within the cytoplasm of various tissues, including liver, lung, and kidney, and exhibits significant reductase activity in both rat and human blood. The reduction process mediated by LY 171859 is NADPH-dependent, with an apparent Km of 14.8 Ī¼M, and specifically incorporates the A-side hydrogen of NADPH into the reaction product. Additionally, this compound's enzymatic activity is sensitive to inhibition by cyanide and thiol reagents, making it a useful tool for studying dopamine receptor signaling and associated metabolic pathways. -
Dopamine D2 Receptor Antagonist
BRL 34778 is a highly selective dopamine D2 receptor antagonist with a Ki value of 2.14 nM, demonstrating significant potency in receptor inhibition. It exhibits antipsychotic properties while minimizing extrapyramidal side effects and sedation. This compound is valuable for investigating neurological disorders, particularly schizophrenia, and contributes to research focused on the modulation of dopaminergic pathways in the brain. -
D2R Agonist
rel-Quinpirole dihydrochloride is a selective dopamine D2 receptor agonist that acts primarily on the D2R target. This compound exhibits significant biological activity in modulating dopamine signaling pathways and is utilized in research applications related to neurological diseases, including Parkinson's disease and schizophrenia. Its use can facilitate the investigation of dopaminergic functions and the development of potential therapeutic strategies. -
Dopamine Autoreceptor Antagonist
AJ-76, classified as a dopamine autoreceptor antagonist, plays a crucial role in modulating dopamine levels in the brain. Research shows that AJ-76 enhances the synthesis and turnover of dopamine while exhibiting minimal influence on serotonin and norepinephrine activity. Additionally, AJ-76 effectively counteracts the sedative effects associated with low-dose apomorphine and demonstrates a modest antagonistic effect at postsynaptic dopamine receptors, making it a valuable tool for research in neuropharmacology and the study of dopamine-related disorders. -
Dopamine Agonist
Lergotrile is a potent, orally active dopamine agonist that functions primarily as a prolactin secretion inhibitor. It exerts its biological activity by activating adenohypophyseal dopamine receptors, leading to the inhibition of prolactin release from the pituitary gland. This compound holds potential for research applications related to Parkinson's disease and other dopaminergic disorders. -
D3 Receptor Antagonist
Dopamine D3 receptor ligand-6 is a selective antagonist of the dopamine D3 receptor. This compound is valuable for investigating mechanisms involved in substance use disorders, including opioid and psychostimulant addiction. Its specificity for the D3 receptor makes it an important tool in pharmacological studies aimed at understanding and potentially mitigating addiction-related behaviors.
