Catalog No.
Product Name
Application
Product Information
Citations
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Vasopressin Receptor Agonist
Argipressin acetate is a potent vasopressin receptor agonist, primarily targeting the V1, V2, and V3 receptors. It exhibits high affinity for the V1 receptor, with a dissociation constant (Kd) of 1.31 nM in A7r5 rat aortic smooth muscle cells. This compound is valuable for research applications exploring vascular physiology, fluid balance, and the modulation of blood pressure. -
Stable Isotope
Anandamide-d8 is a deuterated form of the endocannabinoid Anandamide, primarily known for its interaction with cannabinoid receptors CB1 and CB2. This compound modulates various neuronal and immune functions and can also engage additional receptors, including PPARs, TRPV1, and GPR18/GPR55. Anandamide-d8 exhibits potential anti-fungal and anti-inflammatory properties, making it valuable for research applications in fields such as neurodegenerative diseases, including Alzheimer's disease, and inflammatory conditions like ulcerative colitis. -
PARP-1 Inhibitor
Benzo[c][1,8]naphthyridin-6(5H)-one is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) and aurora kinase A, exhibiting IC50 values of 0.311 μM and 5.5 μM, respectively. This compound demonstrates low micromolar affinity for human adenosine receptors AR A1 and hA2A, with Ki values of 4.6 and 4.8 μM. Due to its mechanistic action, Benzo[c][1,8]naphthyridin-6(5H)-one is valuable for research applications targeting DNA repair pathways and cancer therapies. -
Histamine H2-Receptor Antagonist
Ranitidine hydrochloride is a selective histamine H2-receptor antagonist that effectively inhibits gastric secretion. It demonstrates significant antagonism of histamine-induced cardiac and uterine responses in isolated animal models, with pA2 values of 7.2 and 6.95, respectively. Additionally, ranitidine hydrochloride has been shown to inhibit the development and metastasis of breast tumors in murine models, indicating its potential utility in cancer research. -
5-HT1 Agonist
Rizatriptan benzoate is a selective agonist of the 5-HT1B and 5-HT1D serotonin receptors. It exhibits vasoconstrictive properties that affect peripheral blood flow and effectively penetrates the blood-brain barrier, thereby inhibiting pain neurotransmission within the central nervous system. This compound is primarily utilized in research focused on migraine pathophysiology and the modulation of serotonergic signaling. -
5-HT1 Receptor Agonist
Sumatriptan succinate is a selective agonist for the 5-HT1 receptor subtype, notably demonstrating IC50 values of 7.3 nM, 9.3 nM, and 17.8 nM for the 5-HT1D, 5-HT1B, and 5-HT1F receptors, respectively. This compound is primarily utilized in the study of migraine pathophysiology and therapeutics, providing insights into serotonin modulation during migraine attacks. Its pharmacological profile makes it an essential reagent for research investigating the efficacy of triptans in headache relief. -
A2A Receptor/HDAC Inhibitor
IHCH-3064 is a dual-target compound that inhibits the Adenosine A2A Receptor and histone deacetylase (HDAC). It demonstrates potent binding affinity for the A2A receptor (Ki = 2.2 nM) and selectively inhibits HDAC1 with an IC50 of 80.2 nM. This compound exhibits significant antiproliferative activity against various tumor cell lines in vitro, making it a valuable tool for tumor immunotherapy research applications. -
Dopamine D2/D3 Agonist
Piribedil maleate is a potent agonist of dopamine D2 and D3 receptors, with additional activity as an α2-adrenoceptor antagonist. It has been shown to inhibit MLL1 methyltransferase activity with an EC50 of 0.18 μM. Piribedil maleate is of interest for research applications related to Parkinson’s disease, circulatory disorders, and various cancers. -
Dopamine D2/D3 Agonist
Piribedil hydrochloride is a potent agonist of dopamine D2 and D3 receptors, serving as a valuable tool for investigating dopaminergic signaling pathways. In addition to its agonistic activity, it acts as an antagonist at α2-adrenoceptors and inhibits MLL1 methyltransferase with an EC50 of 0.18 μM. This compound is primarily utilized in research related to Parkinson's disease, circulatory disorders, and certain types of cancer, making it an important reagent for studies focused on neurodegeneration and tumor biology. -
Dopamine D2/D3 Agonist
Piribedil dihydrochloride is a potent dopamine D2 and D3 agonist, also functioning as an antagonist at α2-adrenoceptors. This compound exhibits inhibitory activity on MLL1 methyltransferase with an EC50 of 0.18 μM. It is primarily utilized in research focused on Parkinson's disease, circulatory disorders, and various types of cancers. -
Histamine N-Methyltransferase Inhibitor
SKF 91488 dihydrochloride is a potent, noncompetitive inhibitor of histamine N-methyltransferase, exhibiting a Ki value of 0.9 μM. This compound effectively blocks the metabolism of histamine, leading to elevated concentrations of histamine in biological systems. SKF 91488 dihydrochloride plays a significant role in research focusing on infection, inflammation, and cardiovascular diseases, including studies on Mycoplasma pneumonia and hemorrhagic hypotension. Its influence on blood pressure and bronchoconstriction further underscores its utility in exploring related pathophysiological mechanisms. -
Stable Isotope
Dopamine-d5 hydrochloride is a deuterium-labeled analogue of dopamine, a catecholamine neurotransmitter primarily synthesized in the substantia nigra, ventral tegmental area, and hypothalamus. This compound retains the essential biological functions of dopamine, including its interaction with D2 dopamine receptors, which mediates the endocytosis of VEGFR2, a key process in angiogenesis. Dopamine-d5 hydrochloride is valuable for research applications involving neurotransmitter dynamics, neuropharmacology, and angiogenic pathways. -
Antipsychotic Agent
Penfluridol is a potent, long-acting antipsychotic agent that primarily targets D2-like dopamine receptors. It exhibits significant anti-inflammatory properties by inhibiting TNFα-induced NF-κB activation and demonstrates efficacy in models of arthritis and colitis. Additionally, Penfluridol acts as a Ca2+-calmodulin inhibitor, inducing apoptosis and autophagy in various cellular contexts. This compound is utilized in research focusing on chronic schizophrenia, acute psychosis, Tourette syndrome, autoimmune diseases, and it also shows antibacterial activity against E. faecalis with a minimum inhibitory concentration of 7.81 μg/ml. -
Dopamine Receptor Antagonist
Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes. -
H1 Receptor Antagonist
Pheniramine maleate is a first-generation histamine H1 receptor antagonist that primarily targets the central nervous system to produce sedative and hypnotic effects. In addition to its antihistaminic activity, Pheniramine maleate exhibits antitumor properties by inducing apoptosis in leukemia cells. It also demonstrates effectiveness as a local agent to alleviate pain and provide antipruritic effects in various applications. -
5-HT4 Agonist
Prucalopride succinate is a selective 5-HT4 receptor agonist known for its high affinity for human 5-HT4a and 4b receptors, with pKis of 8.6 and 8.1, respectively. This compound enhances intestinal motility and promotes regeneration of the enteric nervous system, making it relevant for research in chronic constipation and pseudo-intestinal obstruction. Additionally, Prucalopride succinate exhibits anticancer properties by inhibiting the PI3K/AKT/mTOR signaling pathway, thereby facilitating its application in cancer studies. -
Antibiotic
Adenoregulin, also known as Dermaseptin b2, is an antimicrobial peptide antibiotic that targets a broad spectrum of microorganisms. It exhibits activity against both Gram-negative and Gram-positive bacteria, as well as yeast and fungi. Additionally, Adenoregulin enhances the binding of agonists to the A1 adenosine receptor, making it valuable for research applications in microbiology and pharmacology. -
CXCR Inhibitor
Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications. -
CXCR Inhibitor
Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies. -
Stable Isotope
Rimonabant-d10 is a deuterium-labeled analog of Rimonabant, a highly potent and selective antagonist of the central cannabinoid receptor (CB1) with a Ki of 1.8 nM. This compound not only exhibits strong brain penetration but also inhibits Mycobacterial membrane protein Large 3 (MMPL3). Rimonabant-d10 serves as a valuable tool for studying cannabinoid receptor signaling and the role of CB1 in various biological processes, as well as for applications in mycobacterial research. -
Cannabinoid
O,O-Dimethyl-cannabigerol primarily targets cannabinoid receptors and is derived from Cannabis sativa. It exhibits antibacterial activity against drug-resistant strains of Staphylococcus aureus, demonstrating a minimum inhibitory concentration (MIC) of 1 to 2 μg/mL. As a nonpsychoactive constituent, O,O-Dimethyl-cannabigerol is valuable for research into therapeutic applications of cannabinoids, particularly in antimicrobial studies. -
Stable Isotope
(R)-Propranolol-d7 is a deuterated derivative of (R)-Propranolol, serving as a stable isotope-labeled compound. This reagent is invaluable for pharmacokinetic studies and metabolic pathway analysis, enabling the tracking of drug metabolism and distribution in biological systems. Researchers can utilize (R)-Propranolol-d7 in studies focused on cardiovascular research, anxiety treatments, and the mechanisms of action associated with beta-adrenergic receptors. -
Platelet Aggregation Inhibitor
SCH 38519 is a potent platelet aggregation inhibitor that effectively inhibits thrombin-induced aggregation of human platelets, exhibiting an IC50 of 68 μg/mL. In addition to its antiplatelet activity, SCH 38519 demonstrates antibacterial properties against both Gram-positive and Gram-negative bacteria. This compound is valuable for research applications focused on thrombosis, cardiovascular diseases, and bacterial infections. -
Endothelin Receptor Antagonist
Sulfisoxazole diethanolamine is an endothelin receptor antagonist, exhibiting IC50 values of 0.60 μM and 22 μM for endothelin receptor A and endothelin receptor B, respectively. This sulfonamide antibacterial compound, characterized by its oxazole substituent, demonstrates significant inhibition of breast cancer exosome release through the selective targeting of endothelin receptor A. Its mechanism of action holds potential for applications in cancer research and related therapeutic studies. -
5-HT2A Regulator
2-Bromo-LSD D-Tartrate is a selective 5-HT2A receptor partial agonist and competitive antagonist. It exhibits significant biological activity, displaying an EC50 of 0.81 nM for Gq dissociation and a KB of 0.18 nM, making it a valuable tool for studying serotonergic signaling pathways. Additionally, it promotes dendritogenesis and spinogenesis while effectively reversing the behavioral impacts of chronic stress in animal models, enhancing active coping behaviors. This compound is suitable for research involving neurological and behavioral studies related to serotonin modulation. -
5-HT2A/5-HT2C Receptor Agonist
DOI hydrochloride is a potent agonist of the serotonin 5-HT2A and 5-HT2C receptors, exhibiting Ki values of 0.7 nM and 2.4 nM, respectively, while also targeting the 5-HT2B receptor with a Ki of 20 nM. This compound effectively crosses the blood-brain barrier, making it valuable for neurological research. DOI hydrochloride has been shown to induce head twitches in murine models, providing insight into its psychotropic effects and facilitating the study of serotonergic signaling pathways. -
5-HT2B Agonist
BW-723C86 is a selective agonist of the 5-HT2B receptor, demonstrating significant anxiolytic-like effects. In animal models, it has been shown to induce hyperphagia and decrease grooming behavior in rats. Additionally, BW-723C86 exhibits the ability to dilate pulmonary arteries and inhibit gastric accommodation following liquid meal intake, making it a useful reagent for research into anxiety, appetite regulation, and gastrointestinal physiology. -
5-HT4 Receptor Antagonist
GR 113808 is a potent and highly selective antagonist of the 5-HT4 receptor, exhibiting a pKb of 8.8. It demonstrates substantial selectivity, being 300-fold more effective against the 5-HT4 receptor compared to 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors. This compound is widely utilized in research applications focusing on gastrointestinal motility and cognitive function related to serotonin signaling pathways. -
5-HT2B Antagonist
SB 204741 is a selective high-affinity antagonist of the 5-HT2B receptor, exhibiting a pKi value of 7.1. This compound is utilized in research exploring the role of 5-HT2B in various physiological and pathological processes. Its antagonistic properties make it valuable for studies on cardiac function, pulmonary effects, and potential therapeutic interventions in diseases related to serotonergic dysregulation. -
5-HT Biosynthesis Inhibitor
4-Chloro-L-phenylalanine is a potent inhibitor of serotonin (5-HT) biosynthesis, acting as a nonspecific antagonist of the tryptophan hydroxylase isoforms TPH1 and TPH2. This compound is valuable for studying serotonin-related pathways and their implications in psychiatric and neurological disorders. It serves as an important tool for researchers investigating the regulation of serotonin levels and the biochemical basis of 5-HT modulation. -
Dopamine Receptor Antagonist
Spiperone is a potent antagonist of dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A receptors. With its capability to enhance intracellular calcium levels and inhibit the Wnt signaling pathway, Spiperone serves as a valuable tool in the study of neurological disorders. Its role as a labeled ligand for neuroleptic receptors further underscores its utility in receptor binding studies and neurotransmitter research. This compound is particularly relevant for investigating the mechanisms underlying various neuropsychiatric conditions. -
5-HT2C Receptor Agonist
Bexicaserin is a selective agonist of the 5-HT2C receptor, primarily involved in the regulation of appetite and mood. This compound demonstrates potential therapeutic applications in the study of obesity and psychiatric disorders, such as epilepsy. Its unique mechanism of action makes it a valuable tool for researchers investigating the role of serotonin receptors in these conditions. -
5-HT Receptor Agonist
8-OH-DPAT hydrobromide is a potent and selective 5-HT1A receptor agonist with a high pIC50 of 8.19. This compound demonstrates exceptional selectivity, being nearly 1000 times more selective for the 5-HT1A subtype compared to other serotonin receptor subtypes. It is primarily utilized in neuropharmacological research to investigate serotonin-mediated signaling pathways and to explore its effects on various neurological conditions. -
5-HT1A Agonist
Gepirone is a selective 5-HT1A agonist that binds specifically to the 5-HT1A receptor binding site. Its primary biological activity includes acting as an antidepressant, making it a valuable tool in research related to anxiety and major depressive disorders. Gepirone can be utilized to explore the underlying mechanisms of these conditions and aid in the development of new therapeutic strategies. -
5-HT2A Receptor Antagonist
Lumateperone is a potent 5-HT2A receptor antagonist with a Ki of 0.54 nM, exhibiting dual action as a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM). Additionally, it modulates dopamine D1 receptors. This compound demonstrates significant antipsychotic properties and supports research in schizophrenia and bipolar depression, while also presenting potential anticancer activity. -
5-HT Receptor Agonist
2-Methyl-5-HT is a selective agonist for the 5-HT3 receptor. This compound exhibits significant biological activity, particularly in demonstrating anti-depressive-like effects in preclinical models. It is utilized in research to explore serotonergic pathways and contribute to studies on mood regulation and anxiety disorders. -
5-HT Receptor Agonist
Bretisilocin is a selective agonist for the 5-HT2A receptor and functions as a serotonin releaser. This compound demonstrates significant antidepressant activity, making it an important tool for the investigation of depression and related neuropsychiatric disorders. Its role in modulating serotonin pathways provides valuable insights into the underlying mechanisms of mood regulation and potential therapeutic approaches. -
Dopamine D1/D5 Receptor Antagonist
SKF-83566 is a selective antagonist of the D1-like dopamine receptors, specifically targeting the dopamine D1 and D5 receptors. This compound exhibits potent inhibition of the dopamine transporter (DAT) with an IC50 of 5.7 μM, and shows competitive antagonism at the vascular 5-HT2 receptor. In addition, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it relevant for research into neurological disorders such as Parkinson's disease and studies focused on alleviating nicotine cravings. -
5-HT3 Receptor Agonist
SR 57227A is a potent, orally active selective agonist of the 5-HT3 receptor, capable of crossing the blood-brain barrier. This compound exhibits binding affinities (IC50) ranging from 2.8 to 250 nM for 5-HT3 receptor sites in rat cortical membranes and NG 108-15 cell membranes. SR 57227A is primarily utilized in research focused on neuropharmacology and has demonstrated potential anti-depressant effects. -
5-HT Uptake Inhibitor
Norfluoxetine hydrochloride is a potent 5-HT uptake inhibitor, serving as an active N-demethylated metabolite of Fluoxetine. It inhibits serotonin reuptake and has been shown to inhibit CaV3.3 T current with an IC50 of 5 μM. Due to its mechanism of action, Norfluoxetine hydrochloride is relevant in research focusing on mood disorders and anticonvulsant activity, providing insights into serotonin modulation and potential therapeutic applications. -
5-HT4 Receptor Agonist
RS 67333 hydrochloride is a selective partial agonist of the 5-HT4 receptor, demonstrating a pKi of 8.7 in guinea pig striatum. This compound exhibits lower affinities for various other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2, and muscarinic M1-M3 receptors. RS 67333 hydrochloride is known for its neuroprotective properties, making it a valuable tool for research in Alzheimer's disease and related neurodegenerative disorders. -
5-HT Receptor Agonist
CP94253 hydrochloride is a selective agonist of the 5-HT1B receptor, demonstrating a Ki value of 2 nM in radioligand binding assays. It exhibits lower affinity for other serotonin receptor subtypes, with Ki values of 89 nM for 5-HT1A, 49 nM for 5-HT1D, 860 nM for 5-HT1C, and 1600 nM for 5-HT2. This compound is known for its central activity when administered systemically in vivo, making it valuable for research in neuropharmacology and the study of serotonin-related pathways. -
5-HT3 Agonist
m-CPBG hydrochloride is a selective agonist of the 5-HT3 receptor, influencing serotonin signaling pathways. It has demonstrated potential in research related to neurological diseases, allowing for the investigation of serotonin's role in various neurophysiological processes. This compound is valuable for studies aiming to elucidate the mechanisms underlying anxiety, depression, and other psychiatric conditions. -
D2R Agonist
UNC9994 hydrochloride is a functionally selective agonist of the dopamine D2 receptor (D2R), exhibiting β-arrestin–biased signaling and selectively activating β-arrestin recruitment. With a binding affinity of Ki 79 nM for D2R, it functions as an antagonist of Gi-mediated cAMP production and a partial agonist for D2R/β-arrestin-2 interactions. This compound demonstrates antipsychotic-like effects, making it a valuable tool for research in neuropharmacology and the study of dopamine receptor signaling pathways. -
5-HT Receptor Agonist
TCB2 is a potent agonist of the serotonin 5-HT2A receptor. It demonstrates significant activation of this receptor, crucial for mediating various psychological and physiological responses. TCB2 is utilized in research exploring the role of 5-HT2A activation in neuropsychiatric disorders and receptor signaling pathways. -
5-HT7 Receptor Antagonist
SB 258719 is a selective antagonist of the 5-HT7 receptor, exhibiting a high affinity with a pKi value of 7.5. This compound demonstrates significant potential in the research of various neurological disorders and cancer. Its targeted mechanism allows for the exploration of 5-HT7 receptor signaling pathways, contributing to a deeper understanding of their role in these diseases. -
5-HT2C Receptor Agonist
(Rac)-WAY-161503 is a selective agonist of the 5-HT2C receptor, exhibiting a Ki of 4 nM and an EC50 of 12 nM. This compound demonstrates significantly higher affinity for the 5-HT2C receptor compared to the 5-HT2A and 5-HT2B receptors. Due to its biological activity, (Rac)-WAY-161503 is valuable for research applications aimed at understanding obesity and depressive disorders. -
5-HT2C Receptor Antagonist
RS-102221 hydrochloride is a selective antagonist of the 5-HT2C receptor, exhibiting a Ki value of 10 nM. This compound demonstrates approximately 100-fold selectivity over the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride has been shown to stimulate the differentiation of new nerve cells and is associated with increased food intake and weight gain in rodent models, making it a useful tool for research in neurobiology and appetite regulation. -
5HT4 Agonist
Mosapride is a selective 5HT4 agonist known for its gastroenterokinetic properties. This compound enhances gastrointestinal motility and is used in research related to gastrointestinal diseases. Additionally, Mosapride acts as a CYP inducer and exhibits a concentration-dependent inhibitory effect on Kv4.3 with an IC50 value of 15.2 μM. Its pharmacological profile makes it a valuable tool for investigating gut-related disorders. -
Dopamine D3 Receptor Antagonist
SB-277011 hydrochloride is a selective antagonist of the dopamine D3 receptor (D3R), demonstrating potent inhibition with Ki values of 10.7 nM in rodents and 11.2 nM in humans. This compound exhibits significant selectivity, with an 80- to 100-fold preference for D3R over other dopamine receptors, including D2, 5-HT1B, and 5-HT1D. Due to its ability to penetrate the brain and oral bioavailability, SB-277011 hydrochloride is valuable in research investigating the role of D3R in various neurological and psychiatric disorders.
