Catalog No.
Product Name
Application
Product Information
Citations
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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. -
CXCR4 Antagonist
TC14012 is a peptidomimetic antagonist targeting the chemokine receptor CXCR4, exhibiting a high level of selectivity with an IC50 of 19.3 nM. In addition, TC14012 acts as a potent agonist for CXCR7, demonstrating an EC50 of 350 nM in β-arrestin 2 recruitment assays. This compound is utilized in research focused on HIV and cancer therapy, showcasing its potential in modulating chemokine signaling pathways. -
CXCR4 Antagonist
FC131 TFA is a potent CXCR4 antagonist that effectively inhibits the binding of [125I]-SDF-1 to CXCR4, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-HIV activity, making it a valuable tool for research in HIV treatment and other CXCR4-related studies. Its ability to disrupt CXCR4 signaling can be explored in various biological contexts, including cancer metastasis and immune response regulation. -
CXCR4 Antagonist
AMD 3465 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of both the 12G5 monoclonal antibody and CXCL12AF647 to CXCR4, demonstrating IC50 values of 0.75 nM and 18 nM in SupT1 cells, respectively. Additionally, AMD 3465 significantly impedes the replication of X4-tropic HIV strains, with IC50 values ranging from 1 to 10 nM, while showing no activity against CCR5-using (R5) viruses. This compound is suitable for research applications focusing on HIV treatment and CXCR4-related signaling pathways. -
HIV Inhibitor
Schisantherin D is a dibenzocyclooctadiene lignan that exhibits significant anti-HIV activity with an EC50 of 0.5 μg/mL. This compound selectively inhibits endothelin receptor B (ETBR) and demonstrates hepatoprotective properties. Schisantherin D is valuable for research applications focused on HIV replication and the exploration of liver protective mechanisms. -
CXCR4 Antagonist
KRH-3955 hydrochloride is a potent CXCR4 antagonist that effectively inhibits the binding of SDF-1α to CXCR4 with an IC50 of 0.61 nM. This compound demonstrates strong selectivity and efficacy against X4 HIV-1, with an EC50 ranging from 0.3 to 1.0 nM. KRH-3955 hydrochloride is suitable for research applications focused on HIV-1 pathogenesis and CXCR4-related signaling pathways. -
CXCR4 Antagonist
FC131 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. Due to its mechanism of action, FC131 demonstrates significant anti-HIV activity, making it a valuable tool for research into HIV pathogenesis and potential therapeutic interventions. -
Stable Isotope
Plerixafor-d4 is a deuterated derivative of Plerixafor, a selective antagonist of the CXCR4 receptor with an IC50 of 44 nM. This compound serves as an immunostimulant and is known for its ability to mobilize hematopoietic stem cells (HSCs). Additionally, Plerixafor has demonstrated efficacy in inhibiting HIV-1 and HIV-2 replication, with an EC50 ranging from 1 to 10 nM. Plerixafor-d4 is useful in research applications requiring stable isotopes for tracking and quantification purposes. -
HIV-1 Entry Inhibitor
RPR103611 is a derivative of betulinic acid that functions as a potent HIV-1 entry inhibitor. It displays IC50 values of 80 nM for CCR5-tropic virus YU2, 0.27 nM for CXCR4-tropic virus NL4-3, and 0.17 nM for dual tropic virus 89.6. This compound is valuable for research focused on the mechanisms of HIV-1 entry and the development of antiviral therapies. -
CXCR4 Antagonist
CXCR4 antagonist 7 is a potent CXCR4 antagonist with an IC50 of 9.3 nM. It effectively inhibits CXCR4 receptor activity, making it a valuable tool in the investigation of HIV infection, inflammatory diseases, cancer, and WHIM syndrome. This compound provides essential insights into the roles of CXCR4 signaling in various pathological conditions. -
CXCR Inhibitor
AMD 3329 octahydrobromide is a potent CXCR4 inhibitor that effectively reduces HIV-1 and HIV-2 viral replication. It demonstrates exceptional antiviral activity with EC50 values of 0.8 nM and 1.6 nM, surpassing the efficacy of related compounds. Additionally, AMD 3329 significantly obstructs the binding of specific CXCR4 monoclonal antibodies and inhibits SDF-1 alpha-induced Ca(2+) influx. This compound also disrupts virus-induced syncytium formation, with an EC50 of 12 nM, making it a valuable tool for HIV research and therapeutic development. -
CXCR4 Antagonist
CXCR4 Antagonist 4 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 of 24 nM. It demonstrates enhanced permeability as assessed by PAMPA and has reduced activity on CYP 2D6. This compound is particularly effective in inhibiting the entry of human immunodeficiency virus, with an IC50 value of 7 nM, making it a valuable tool for research in virology and therapeutic development targeting CXCR4-mediated pathways. -
CXCR Antagonist
GSK812397 is a potent CXCR4 antagonist that functions by inhibiting the CXC chemokine receptor 4, a critical co-receptor for HIV-1 entry into host cells. This compound has demonstrated significant biological activity, making it a promising candidate for HIV treatment research. Its ability to suppress the replication of various late cytopathic viruses marks GSK812397 as a valuable reagent in the development of innovative anti-HIV therapies. Additionally, scalable synthetic routes enable efficient production, ensuring sufficient quantities for comprehensive investigation. -
CXCR Antagonist
CXCR4 antagonist 1 is a selective antagonist of the chemokine receptor CXCR4. It exhibits significant anti-HIV activity by inhibiting the interaction of CXCR4 with its ligands, thereby blocking viral entry into host cells. This compound is valuable in research focused on HIV pathogenesis and the development of therapeutic strategies targeting CXCR4. -
CXCR4 Antagonist
HF50731 is a potent antagonist of CXCR4, demonstrating a binding affinity with an IC50 value of 19.8 nM. This compound effectively inhibits key biological processes such as calcium mobilization and cell migration, with IC50 values of 119.2 nM and 621.4 nM, respectively. Additionally, HF50731 demonstrates the ability to inhibit HIV-1 infection through CXCR4 coreceptor blockade, achieving an IC50 of 1.5 μM. HF50731 is valuable for research in immunology, virology, and cancer biology focused on CXCR4 signaling pathways. -
CXCR Inhibitor
AMD-3329 is a selective CXCR4 inhibitor that targets the chemokine receptor involved in HIV-1 and HIV-2 entry into host cells. By obstructing CXCR4, AMD-3329 effectively inhibits viral replication, making it a valuable tool in HIV research. This compound is suitable for studies focused on developing therapeutic strategies against X4-tropic HIV strains and understanding the mechanisms of viral entry and infection. -
Platelet-Activating Factor Antagonist
Acopafant is a potent platelet-activating factor antagonist that plays a critical role in modulating inflammatory responses. Its ability to inhibit human immunodeficiency virus (HIV) expression in chronically infected cells highlights its potential utility in HIV research. Acopafant is valuable for studies investigating the mechanisms of HIV infection and the development of therapeutics targeting viral latency and reactivation. -
HIV Inhibitor
KRH-3955 is a potent CXCR4 antagonist that demonstrates significant anti-HIV-1 activity, particularly against X4 strains. It effectively inhibits the replication of various X4 HIV-1 clinical isolates and is active against recombinant strains with resistance mutations in reverse transcriptase, protease, and tyrosinase. KRH-3955 disrupts the binding of SDF-1alpha to CXCR4, thereby interfering with calcium signaling through this receptor, along with inhibiting antibody binding to CXCR4. With an oral bioavailability of 25.6% in rats, KRH-3955 has shown efficacy in vivo, making it a valuable tool for HIV research. -
PAFR Antagonist
(Rac)-Modipafant is a selective, long-acting irreversible antagonist of the platelet activating factor receptor (PAFR). This compound demonstrates significant biological activity by effectively inhibiting PAFR-mediated pathways, which plays a critical role in regulating inflammatory responses. Research applications include the investigation of dengue virus infection mechanisms and the potential therapeutic effects of PAFR blockade in various inflammatory diseases.
