Catalog No.
Product Name
Application
Product Information
Citations
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5-HT6R Agonist
EMD386088 is a highly potent and selective agonist of the 5-HT6 receptor (5-HT6R) with an EC50 of 1.0 nM. This compound exhibits minimal activity against other serotonin receptors, displaying an IC50 of 34 nM primarily at the 5-HT3R. EMD386088 is known to modulate ERK1/2 activity, indicating its potential role in signaling pathways. This reagent is relevant for research applications related to Alzheimer's disease and schizophrenia, providing insight into neuropsychiatric disorders and their treatment. -
5-HT Receptor Agonist
25C-NBOH hydrochloride is a potent agonist targeting 5-HT receptors, specifically exhibiting a strong preference for the 5-HT2A receptor over the 5-HT2C receptor, with EC50 values of approximately 0.40 nM and 15 nM, respectively. This compound is a derivative of 2C-C featuring an N-(2-hydroxybenzyl) substitution at the amine position. 25C-NBOH hydrochloride plays a significant role in neuropharmacological research, facilitating the investigation of serotonin signaling pathways and their implications in various neurological disorders. -
Sigma/5-HT1A Receptor Agonist
OPC-14523 free base is a potent sigma and 5-HT1A receptor agonist. With a high affinity for sigma receptors (σ1/2 IC50=47/56 nM) and the 5-HT1A receptor (IC50=2.3 nM), along with activity at the 5-HT transporter (IC50=80 nM), it exhibits significant antidepressant-like effects. This compound is valuable for research applications investigating mood disorders and serotonergic signaling pathways. -
5-HT2C Receptor Agonist
Org-12962 is a selective agonist of the 5-HT2C receptor, demonstrating a pEC50 value of 7.01. In addition to its primary target, Org-12962 shows significant efficacy for the 5-HT2A and 5-HT2B receptors with pEC50 values of 6.38 and 6.28, respectively. This compound is notable for its anti-aversive effects observed in rat models of panic-like anxiety, making it a valuable tool for investigating anxiety disorders and related neuropharmacology. -
5-HT1A Receptor Agonist
Repinotan is a potent and selective agonist of the 5-HT1A receptor, exhibiting strong brain penetration and oral bioavailability. With Ki values of 0.19 nM in the calf hippocampus, 0.25 nM in rat and human cortex, and 0.59 nM in rat hippocampus, it displays high affinity for target sites while maintaining weak interaction with other related receptors. Repinotan is recognized for its significant neuroprotective properties, making it valuable for research in neuroscience and related therapeutic applications. -
5-HT3 Receptor Antagonist
(R)-Mirtazapine is a selective 5-HT3 receptor antagonist known for its antinociceptive properties demonstrated in animal models of acute thermal nociception. This R( )-enantiomer of Mirtazapine contributes to various neurological studies, particularly in the context of pain modulation and serotonin pathway interactions. (R)-Mirtazapine undergoes metabolism primarily by the enzyme CYP3A4, making it a relevant compound for pharmacokinetic studies in drug metabolism. -
5-HT4 Agonist
ML 10302 is a potent 5-HT4 receptor agonist with a Ki value of 1.07 nM. This compound enhances gut motility by stimulating cholinergic pathways, leading to significant prokinesia in both the small intestine and colon. Additionally, ML 10302 holds potential for research applications in neurological diseases, providing insights into therapeutic mechanisms targeting the gastrointestinal and nervous systems. -
5-HT Agonist
PNU-22394 hydrochloride is a potent agonist for the 5-hydroxytryptamine (5-HT) receptors, specifically engaging the 5-HT2C and 5-HT2A receptor subtypes with Ki values of 6.1 nM and 10 nM, respectively. This compound is valuable for studying the roles of 5-HT in neurobiology and its implications in various psychiatric disorders. Its selective action on serotonin receptors makes it a useful tool for investigating serotonin signaling pathways and potential therapeutic interventions. -
5HT3A Receptor Antagonist Ligand
GR119566X is a high-affinity antagonist of the 5HT3A receptor, effectively inhibiting receptor activity. This compound is suitable for use in affinity purification experiments involving 5-HT3 receptors, providing a valuable tool for investigating receptor function and pharmacology. Its specificity for the 5HT3A receptor makes it useful for diverse applications in neurobiology and drug discovery research. -
5-HT2 Receptor Antagonist
Fananserin is a potent and selective antagonist of the 5-hydroxytryptamine 2 (5-HT2) receptor, exhibiting a Ki value of 0.37 nM for the rat 5-HT2A receptor. Additionally, Fananserin serves as a selective antagonist for the dopamine D4 receptor, with a Ki of 2.93 nM for the human variant. This compound is valuable for research exploring the modulation of serotonin and dopamine pathways, offering insights into potential therapeutic applications in neuropsychiatric disorders. -
5-HT Receptor Antagonist
5-HT2A antagonist 1 is a selective antagonist of the 5-HT2A receptor, playing a crucial role in modulating serotonin signaling. This compound demonstrates potential in alleviating gastrointestinal disorders and may also have applications in addressing circulatory system irregularities. Its pharmacological profile makes it a valuable tool for research in serotonergic pathways and their implications in various biological systems. -
5-HT4 Receptor Partial Agonist
CJ033466 is a selective partial agonist of the 5-HT4 receptor, exhibiting an EC50 of 9 nM. This compound demonstrates significant gastroprokinetic effects, making it a valuable tool for research applications related to gastrointestinal motility and related disorders. Its specificity towards the 5-HT4 receptor aids in elucidating receptor-mediated pathways and potential therapeutic interventions. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole (hydrochloride) functions as an α2-adrenoceptor antagonist and a serotonin (5-HT) reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is particularly relevant for research into depression and related neuropsychiatric disorders, facilitating studies on serotonin modulation and adrenergic signaling pathways. Its dual action can provide insights into the mechanisms underlying mood regulation and therapeutic interventions. -
5-HT1A Agonist
R(+)-8-OH-DPAT hydrobromide is a selective agonist of the 5-HT1A receptor, known for its significant efficacy in modulating serotonergic signaling. This compound enhances dopamine release in the medial prefrontal cortex, thereby providing valuable insights into the relationship between serotonin and dopamine neurotransmission. R(+)-8-OH-DPAT is widely utilized in research focused on neuropharmacology and behavioral studies related to mood disorders and cognition. -
5-HT Receptor
(R,R)-Palonosetron Hydrochloride is a selective antagonist of the 5-HT3 receptor. This compound exhibits significant antiemetic properties, making it valuable in the prevention of chemotherapy-induced nausea and vomiting. Its high affinity for the 5-HT3 receptor can also facilitate research on serotonin signaling pathways and their role in gastrointestinal function and neurological disorders. -
5-HT Receptor Agonist
Revexepride is a selective agonist of the 5-HT4 receptor, exerting effects on gastrointestinal motility and potentially influencing CYP3A4 enzyme induction. Its primary biological activity includes the enhancement of gastrointestinal function, making it a candidate for research in digestive disorders such as gastroesophageal reflux disease. This compound is relevant for studies investigating serotonergic modulation in gastrointestinal diseases and the metabolic implications associated with CYP3A4 activity. -
5-HT2C Receptor Agonist
Ro60-0175 fumarate acts as a potent and selective agonist of the 5-HT2C receptor, which is involved in various neurophysiological processes. This compound has demonstrated significant activity in modulating serotonin signaling pathways, making it a valuable tool for research into mood regulation, anxiety, and appetite control. It is suitable for studies focused on the pathophysiology of psychiatric disorders and the development of novel therapeutic strategies. -
D3R/5-HT2AR Antagonist/5-HT1AR Agonist
D3/5-HT receptor modulator-1 is a selective antagonist for dopamine D3 receptors and 5-HT2A receptors, while also functioning as a partial agonist at 5-HT1A receptors. With measured Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the respective targets, this compound exhibits a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. Its unique pharmacological profile suggests potential applications in the development of atypical antipsychotic therapies and for studying dopaminergic and serotonergic signaling pathways. -
5-HT2C/2B Receptor Antagonist
SB228357 is a selective and potent antagonist of the 5-HT2C and 5-HT2B receptors, exhibiting pKi values of 6.9, 8.0, and 9.0 for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. This compound demonstrates significant antidepressant and anxiolytic effects, making it valuable for research focused on mood disorders and anxiety-related conditions. Its oral bioavailability further enhances its utility in pharmacological investigations. -
5-HT Antagonist
(S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of the 5-HT 1A receptor, exhibiting an IC50 of 33.9 nM. This compound demonstrates anxiolytic effects in animal models, making it a valuable tool for research in anxiety disorders and related neuropharmacological studies. Its specificity for the 5-HT 1A target enables investigations into serotonin receptor-mediated signaling pathways and their implications in various psychiatric conditions. -
5-HT2A Receptor Agonist
LPH-5 is a selective agonist of the 5-HT2A receptor, exhibiting an EC50 of 190 nM. Through its activation of the 5-HT2A receptor, LPH-5 plays a critical role in modulating mood, perception, and various central nervous system processes. This compound is valuable for investigating the involvement of the 5-HT2A receptor in psychiatric disorders such as depression, anxiety, and substance use disorders. -
5-HT4 Receptor Agonist
Relenopride hydrochloride is a selective agonist of the 5-HT4 receptor, exhibiting a Ki value of 4.96 nM, which confirms its high affinity for this target. With significantly lower affinities for the 5-HT2A and 5-HT2B receptors, Relenopride hydrochloride is a valuable tool for studying gastrointestinal physiology. It is primarily utilized in research on enhancing gastrointestinal motility and investigating conditions related to digestive function. -
α2B/C-Adrenergic Receptor Antagonist
ARC 239 is a selective antagonist of the α2B and α2C adrenergic receptors, exhibiting a pKi of 7.06 for rat kidney α2B and 6.95 for human α2C. In addition, ARC 239 inhibits the 5-HT1A receptor with a Ki value of 63.1 nM. This compound is valuable in research involving adrenergic signaling pathways and the modulation of neurotransmitter systems, making it suitable for studies on cardiovascular function and psychiatric disorders. -
5-HT2C Agonist
5-HT2C agonist-3 is a selective agonist for the 5-HT2C receptor, exhibiting an EC50 of 24 nM and a Ki of 78 nM. This compound demonstrates antipsychotic-like properties and effectively inhibits amphetamine-induced hyperactivity. It serves as a valuable tool for research into neuropharmacology and the modulation of serotonergic systems. -
5-HT/Serotonin Receptors Ligand
1-(2-Methoxyphenyl)piperazine hydrochloride is a ligand targeting 5-HT (serotonin) receptors, crucial for the development of various antipsychotic agents. Its high affinity for serotonin receptors makes it a valuable compound in synthesizing pharmacological agents, such as Piperazine phosphate, Piperazine citrate, and Fluphenazine dihydrochloride. Additionally, this reagent can be utilized in the synthesis of Rifampicin, contributing to studies in neuroscience and psychiatric research. -
Ziprasidone Impurity
Keto Ziprasidone is a known impurity of the antipsychotic agent Ziprasidone, which functions primarily as a combined antagonist of serotonin (5-HT) and dopamine receptors. This compound is crucial for research applications focusing on drug metabolism and pharmacokinetics, particularly in understanding the potential effects of impurities on therapeutic efficacy and safety profiles. Its analysis can aid in the development of quality control measures in pharmaceutical formulations. -
5-HT(6/7/2A)/ Dopamin D2 Receptors Antagonist
5-HT6/7 Antagonist 1 is a potent antagonist of the 5-HT6, 5-HT7, and D2 receptors, exhibiting selectivity that spares M1 receptors and hERG channels. This compound's multifunctional activity makes it valuable for research into neuropharmacology and the modulation of serotonergic and dopaminergic systems. It provides a useful tool for studying disorders related to these receptor pathways, including anxiety, depression, and schizophrenia. -
5HT-4/5HT-3 Antagonist
Lintopride is a benzamide that acts as a potent antagonist of the 5HT-4 receptor, with moderate antagonistic properties at the 5HT-3 receptor. This compound enhances gastric emptying, stimulates motility in the antrum and duodenum, and accelerates intestinal transit in animal models. Additionally, Lintopride significantly increases the basal tone of the lower oesophageal sphincter, highlighting its potential applications in gastrointestinal research and therapy. -
Ziprasidone Impurity
Hydroxy ziprasidone is a known impurity of the antipsychotic agent ziprasidone, which functions primarily as a combined antagonist of both serotonin (5-HT) and dopamine receptors. This compound is useful for researchers studying the pharmacological properties and metabolic pathways of ziprasidone, as well as for quality control in the synthesis of pharmaceutical formulations. Its presence can provide insights into the drug's safety, efficacy, and potential side effects. -
Cannabinoid Receptor Agonist
AM9405 is a selective agonist for cannabinoid receptor type 1 (CB1) and serotonin type 3 (5-HT3) receptors. It demonstrates potent inhibitory effects on twitch contractions in the ileum and colon, with half-maximal inhibitory concentrations (IC50) of 45.71 nM and 0.076 nM, respectively. AM9405 is valuable for research in gastrointestinal motility and cannabinoid signaling pathways. -
5-HT5A Receptor Probe
UCSF648 is a chemical probe targeting the 5-HT5A serotonin receptor. It demonstrates weak activation of the ADRA2A and MTNR1A receptors, making it valuable for studies investigating serotonin signaling pathways. This reagent is suitable for research applications related to neuropharmacology and the modulation of serotonin receptor activity. -
5-HT1A Receptor Agonist
Tandospirone hydrochloride is a selective partial agonist of the 5-HT1A receptor, exhibiting a Ki value of 27 nM. This compound displays notable anxiolytic and antidepressant properties, making it valuable in the study of central nervous system disorders. Its unique action at the 5-HT1A receptor contributes to the understanding of underlying mechanisms related to anxiety and depression, facilitating research aimed at developing novel therapeutic approaches. -
Dopamine D2/D3/5-HT7 Receptor Inhibitor
LB-102 is an orally bioavailable inhibitor of dopamine D2, D3, and 5-HT7 receptors. It exhibits significant antagonistic activity, making it a valuable tool for investigating the neurochemical pathways involved in schizophrenia and other psychiatric disorders. This compound is useful for studies aimed at understanding the role of these receptors in various neuropsychiatric conditions. -
5-HT/DA Receptor Antagonist
Ziprasidone mesylate trihydrate is an orally active antagonist of serotonin (5-HT) and dopamine (DA) receptors, primarily targeting the 5-HT2A and D2 receptor subtypes. With a high affinity for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM), and 5-HT1A (Ki=3.4 nM), this compound is significant for studies related to mood disorders, schizophrenia, and neuropharmacology. Ziprasidone mesylate trihydrate serves as a valuable tool for exploring receptor mechanisms and assessing therapeutic effects in relevant biological models. -
TAAR1/5-HT1A Agonist
Ulotaront is a novel TAAR1 and 5-HT1A agonist that operates through a distinct mechanism separate from traditional D2 and 5-HT2A pathways. This compound exhibits significant antipsychotic-like properties, making it a valuable tool for researching schizophrenia and related neuropsychiatric disorders. Its unique profile allows for exploration of alternative treatment strategies that may enhance therapeutic options for psychiatric conditions. -
5-HT Receptor Antagonist
Clocapramine is a selective antagonist of the 5-HT2A receptor, with additional inhibitory effects on D2 dopamine receptors. This compound exhibits notable properties in modulating serotonin and dopamine signaling, making it relevant for neuropharmacological research. Clocapramine can be utilized in studies related to psychiatric disorders, including depression and schizophrenia, as well as the characterization of receptor interactions in neural pathways. -
PKC Inhibitor
NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways. -
Protein Kinase C Inhibitor/LTD4 Antagonist
LY 170198 is a potent protein kinase C inhibitor and LTD4 antagonist. This compound exhibits significant biological activity relevant to studies on tumor promotion, oncogene activation, and protein phosphorylation. Additionally, it is valuable for investigating feedback mechanisms in signal transduction pathways and cellular responses to growth factors, making it a useful tool for cancer research and related fields. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
Sigma Receptor Antagonist
NE-100 hydrochloride is a selective antagonist of the sigma-1 receptor, exhibiting an IC50 value of 4.16 nM. This compound demonstrates significant neuroprotective effects and has been shown to improve cognitive impairment, making it valuable in studies related to neurodegenerative disorders and psychiatric conditions. NE-100 hydrochloride is a useful tool for investigating the role of sigma receptors in the nervous system. -
Stable Isotope
Fluphenazine-d8 is a deuterium-labeled derivative of fluphenazine, functioning primarily as a dopamine receptor antagonist. It effectively inhibits postsynaptic dopamine-2 receptors in key neural pathways, including the mesolimbic, nigrostriatal, and tuberoinfundibular systems. This reagent is valuable in research areas such as psychosis and diabetic peripheral neuropathy, and it has shown potential in studies related to SARS-CoV-2 inhibition. Fluphenazine-d8 serves as a useful tool for elucidating the pharmacodynamics of dopaminergic activity and its downstream effects. -
Dopamine Receptor Antagonist
Fluphenazine hydrochloride functions as a potent dopamine receptor antagonist, primarily targeting postsynaptic dopamine-2 receptors within mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This compound exhibits significant biological activity by blocking neuronal voltage-gated sodium channels, leading to effects on behavior, such as the antagonism of methylphenidate-induced stereotyped gnawing and inhibition of climbing behavior in murine models. Fluphenazine hydrochloride is valuable for research into psychotic disorders and painful peripheral neuropathy related to diabetes, and it has demonstrated potential for inhibition of SARS-CoV-2. -
Dopamine Receptor Antagonist
Fluphenazine dimaleate is a potent dopamine receptor antagonist primarily targeting postsynaptic dopamine-2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. Its ability to antagonize neuronal voltage-gated sodium channels contributes to its effectiveness in modulating dopaminergic activity. Fluphenazine dimaleate is valuable in research addressing psychosis, diabetic neuropathy, and behavioral studies, including the inhibition of Methylphenidate-induced stereotyped behaviors in animal models. Emerging studies also suggest its potential in inhibiting SARS-CoV-2, positioning it as a multifaceted tool in scientific investigation. -
Dopamine Receptor Agonist
Mergocriptine is a dopamine receptor agonist that has been identified as a ligand for the SARS-CoV-2 main protease (Mpro). This compound plays a significant role in modulating ambulatory activity and may be utilized in research focused on neurological disorders and viral pathogenesis. Its dual action positions it as a valuable tool in studying dopamine-related pathways and potential antiviral mechanisms. -
Anti-tumor Agent
Scoulerine hydrochloride is a multi-target inhibitor primarily acting as an anti-tumor agent. It disrupts the PI3K/Akt/mTOR signaling pathway and α1D-adrenergic receptors, leading to microtubule destabilization, cell cycle arrest, and apoptosis in cancer cells. This compound also inhibits mitochondrial dehydrogenase activity and demonstrates effects on GABA receptors and BACE1, suppressing tumor cell proliferation, migration, invasion, and stem cell-like properties. Additionally, Scoulerine hydrochloride exhibits pharmacological activities against Plasmodium falciparum, as well as antibacterial, antiemetic, and antitussive properties, while also influencing endoplasmic reticulum stress and mitochondrial function. It is particularly relevant in studies focused on leukemia, ovarian cancer, and colorectal cancer. -
Stable Isotope
Gramine-d2 is a deuterium-labeled derivative of Gramine, a natural alkaloid derived from giant reed. This compound functions as an adiponectin receptor agonist, exhibiting IC50 values of 3.2 μM for AdipoR2 and 4.2 μM for AdipoR1. Additionally, Gramine acts as an agonist for human and mouse β2-Adrenergic receptors, demonstrating anti-tumor, anti-viral, and anti-inflammatory activities. Gramine-d2 is valuable for research applications that require stable isotopic labeling in biological studies. -
NMDA Receptor Antagonist
Ifenprodil is a noncompetitive antagonist of the NMDA receptor, with a strong affinity for the NR1A/NR2B subunit (IC50 = 0.34 μM) compared to NR1A/NR2A (IC50 = 146 μM). This compound also acts as an α1 adrenergic receptor antagonist and inhibits GIRK channels, reducing basal inward currents. Additionally, Ifenprodil demonstrates antiviral activity against A/H1N1 strains (EC50 = 6.6 µM) and possesses neuroprotective, anticonvulsant, and antinociceptive properties. It is suitable for research in cerebrovascular diseases and peripheral arterial obliterative disease. -
GPCRs/Adenosine Modulator
SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs), specifically targeting adenosine receptors (AR). This compound exhibits antiviral properties and effectively inhibits the 3CLpro enzyme in a time-dependent manner, with an IC50 value of 0.655 µM. SCH-202676 is valuable for research applications focusing on GPCR signaling pathways and the development of antiviral therapeutic strategies. -
CXCR4 Antagonist
Mavorixafor trihydrochloride is a potent and selective antagonist of the CXCR4 receptor, exhibiting an IC50 of 13 nM in inhibiting CXCR4 125I-SDF binding. This compound has demonstrated significant antiviral activity by inhibiting the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs, with IC50 values of 1 nM and 9 nM, respectively. Mavorixafor trihydrochloride is applicable in research studying WHIM syndrome and various CXCR4-related biological processes. -
CCR7 and CXCR2 Antagonist
Cosalane is a dual antagonist of the chemokine receptors CCR7 (IC50 = 2.43 μM) and CXCR2 (IC50 = 0.66 μM). This compound effectively inhibits HIV replication across a variety of strains, including HIV-1, HIV-2, Rauscher murine leukemia virus, as well as herpes simplex viruses HSV-1 and HSV-2, and human cytomegalovirus. Cosalane disrupts the interaction between gp120 and CD4, inhibiting signaling downstream of CCR7 in response to its ligands CCL19 and CCL21. Research applications include studies on HIV and the potential modulation of acute graft-versus-host disease in allogeneic hematopoietic stem cell transplantation.
