Catalog No.
Product Name
Application
Product Information
Citations
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α/β Adrenergic Receptor Blocker
Primidolol is an orally active α/β Adrenergic Receptor blocker that exhibits antihypertensive properties. This compound demonstrates significant antibacterial and antioxidant activities, making it relevant in studies focused on both cardiovascular diseases and infectious processes. Its dual mechanism of action positions Primidolol as a valuable tool for research aimed at understanding the interplay between adrenergic signaling and microbial resistance. -
β2-Drenergic Receptor Agonist
Terbutaline is an orally active β2-adrenergic receptor agonist that effectively stimulates the β2-adrenergic receptors. Its primary biological activity includes bronchodilation, making it relevant for research on asthma symptoms and respiratory disorders. Terbutaline is commonly used in studies investigating the therapeutic effects of β2-agonists in pulmonary conditions. -
β2-Drenergic Receptor Agonist
Terbutaline sulfate is an orally active β2-adrenergic receptor agonist, primarily utilized in the treatment of asthma and other bronchospastic conditions. As an active metabolite of bambuterol, it promotes bronchodilation by relaxing smooth muscle in the airways. This compound is essential for research applications focused on respiratory pharmacology and the therapeutic evaluation of β2-adrenergic systems in asthma symptom management. -
Antibiotic
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic primarily targeting bacterial growth inhibition. It exhibits significant antibacterial activity, particularly against methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 5 μg/mL. In addition to its antibacterial properties, Kendomycin acts as a potent antagonist of the endothelin receptor and a calcitonin receptor agonist, highlighting its potential applications in anti-osteoporotic research. -
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. -
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. -
Dopamine/5-HT2A Antagonist
Paliperidone palmitate is a competitive antagonist of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A) receptors with the capability to cross the blood-brain barrier. By binding to these receptors, it modulates the activity of dopamine and serotonin, thereby exerting antipsychotic effects. This compound is primarily utilized in research related to schizophrenia and other neuropsychiatric disorders, contributing to the understanding of antipsychotic mechanisms and therapeutic strategies. -
5-HT2B Receptor Agonist
(+)-Norfenfluramine hydrochloride is a selective agonist of the 5-HT2B receptor, exhibiting a Ki value of 11.2 nM. This compound effectively stimulates the hydrolysis of inositol phosphates and enhances intracellular calcium levels. Its biological activity makes it a valuable tool for studies related to primary pulmonary hypertension and valvular heart disease. -
Rat 5-HT1B Antagonist
NAS-181 dimesylate is a selective antagonist of the rat 5-HT1B receptor, exhibiting a Ki value of 47 nM. With a notable 13-fold selectivity for the r5-HT1B receptor compared to the bovine equivalent (Ki=630 nM), NAS-181 effectively enhances serotonin (5-HT) turnover and improves synaptic 5-HT concentration by blocking terminal r5-HT1B autoreceptors. This compound is valuable for research involving serotonin modulation and related neuropharmacological studies. -
5-HT Receptor Inhibitor
Ansofaxine hydrochloride is a potent triple reuptake inhibitor that targets the serotonin, dopamine, and norepinephrine transporters. It demonstrates inhibition with IC50 values of 723 nM for serotonin, 491 nM for dopamine, and 763 nM for norepinephrine. This compound is primarily used in research to investigate the mechanisms underlying mood disorders and has potential applications in studies focused on neuropharmacology and the treatment of depression and anxiety. -
β-arrestin-biased 5-HT2AR Agonist
IHCH-7086 is a partial β-arrestin-biased agonist of the 5-HT2A receptor, exhibiting a Ki value of 12.59 nM, and capable of crossing the blood-brain barrier. This compound has demonstrated effectiveness in blocking D-lysergic acid diethylamide-induced head-twitch responses in murine models and alleviating depression-like behaviors in mice subjected to acute restraint stress or corticosterone administration. IHCH-7086 is particularly relevant for research focused on depression and related neuronal signaling pathways.
