Catalog No.
Product Name
Application
Product Information
Citations
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histamine H1 receptor agonist and H3 receptor antagonist
Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA). -
beta-adrenoceptor antagonist
DL 071-IT is a potent non-selective beta-adrenoceptor antagonist. . -
adenosine receptor antagonist
AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities. -
norepinephrine reuptake inhibitor
(R)-Viloxazine Hydrochloride is the R-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
norepinephrine reuptake inhibitor
(S)-Viloxazine Hydrochloride is the S-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
antagonist of histamine H1
Cyclizine is an antagonist of histamine H1. Cyclizine is an antihistamine drug that can be used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids. -
LPA Receptor Activator
1-Oleoyl lysophosphatidic acid sodium is a potent LPA receptor activator, functioning primarily as a bioactive phospholipid. This compound promotes mitosis by inducing DNA synthesis, making it critical for studies in cell proliferation. Additionally, 1-Oleoyl lysophosphatidic acid sodium plays a role in mediating both normal and pathological emotional responses, including anxiety and depression, contributing to research in neurobiology and mental health disorders. -
Orexin Receptor Agonist
RTIOXA-43 is an orexin receptor agonist that exhibits potent activity with EC50 values of 24 nM for both OX1 and OX2 receptors. This compound is valuable for research applications related to sleep regulation, appetite control, and energy metabolism. By activating orexin receptors, RTIOXA-43 facilitates investigations into neurodegenerative diseases and sleep disorders. -
GPR18 Agonist
N-Arachidonylglycine (NA-Gly) selectively acts as an agonist for the GPR18 receptor, exhibiting an EC50 value of 44.5 nM. Unlike its structural analog anandamide, NA-Gly does not engage with CB1 or CB2 receptors. This compound also demonstrates inhibitory activity on GLYT2 with an IC50 of 5.1 μM. Additionally, N-Arachidonylglycine has been shown to effectively promote the migration of endometrial cells, making it a valuable tool for research in cellular migration and cannabinoid receptor activity. -
Adrenergic Receptor Antagonist
Propranolol hydrochloride is a nonselective β-adrenergic receptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1AR and β2AR receptors, with Ki values of 1.8 nM and 0.8 nM, respectively, and inhibits [3H]-DHA binding in rat brain membranes with an IC50 of 12 nM. This reagent is widely used in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
Antihypertensive Agent
Indoramin is an orally active antihypertensive agent targeting the α1A-adrenoceptor. This compound works by selectively blocking α1-adrenoceptors, leading to vasodilation and a reduction in blood pressure. Indoramin is utilized in cardiovascular research to study blood pressure regulation and the mechanisms of hypertension. -
Smo Agonist
GSA-10 is a potent agonist of the smooth (Smo) receptor, playing a crucial role in mediating Hedgehog (Hh) signaling pathways. This compound exhibits significant osteogenic activity and is valuable in regenerative medicine and research on cancer pathologies. Additionally, GSA-10 can be utilized in studies focused on adipogenesis and fat development, making it a versatile tool in biological research. -
Serotonergic Receptor Antagonist
Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology. -
Prostaglandin E2 Inhibitor
Thielavin B is an inhibitor of prostaglandin biosynthesis, specifically targeting the synthesis of prostaglandin E2 from endoperoxide precursors. This compound demonstrates significant anti-inflammatory activity, as evidenced by its efficacy in reducing carrageenan-induced edema in rat models following intravenous administration. Thielavin B is valuable for research focused on inflammation and pain pathways. -
Endogenous Glucocorticoids
Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
β2-Adrenergic Receptor Agonist
Levalbuterol hydrochloride is a potent β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. It exhibits enhanced bronchodilator activity, making it a valuable reagent in respiratory research. Primarily, it is utilized in studies focusing on the treatment of chronic obstructive pulmonary disease (COPD) and other airway obstruction disorders. -
L-glutamate Uptake Inhibitor
Evans Blue is a potent inhibitor of L-glutamate uptake through the membrane-bound excitatory amino acid transporter (EAAT). This compound effectively inhibits L-glutamate and kainate receptor-mediated currents, making it valuable for research into neurophysiological processes. Additionally, due to its strong affinity for serum albumin, Evans Blue serves as a high molecular weight protein tracer and is widely used to investigate blood-brain barrier (BBB) permeability. -
Endothelin Receptor Inhibitor
Carperitide is a synthetic analogue of Atrial Natriuretic Peptide (ANP) that acts as an endothelin receptor inhibitor. This 28-amino acid peptide significantly reduces endothelin-1 secretion in a dose-dependent manner, thereby promoting vasodilation and natriuresis. It is primarily used in research applications related to cardiovascular physiology, providing insights into heart failure mechanisms and the regulation of blood pressure. -
Histamine H1 Receptor Antagonist
Epinastine is a selective histamine H1 receptor antagonist, known for its effectiveness as a mast cell stabilizer. It exhibits high affinity for neuronal octopamine receptors in various insects, demonstrating potential roles in modulating immune responses. Epinastine also inhibits pro-inflammatory cytokines such as TARC, IL-8, and IL-4, making it valuable for research into allergic diseases and anti-cancer immunity mechanisms. Its ability to reduce scratching behavior and vascular permeability further underscores its relevance in studying allergic and inflammatory conditions. -
Histamine H1 Receptor Antagonist
Mebhydrolin is a selective antagonist of the histamine H1 receptor, primarily known for its role in mediating allergic responses. This compound exhibits significant antihistaminic activity, making it valuable for research in allergy and immunology. Its effectiveness in blocking histamine-induced physiological effects allows for the exploration of H1 receptor pathways and the development of related therapeutic strategies. -
NPRs Agonist
Nesiritide, a recombinant form of human B-type natriuretic peptide, primarily functions as an agonist of natriuretic peptide receptors (NPRs), specifically NPR-A and NPR-C, with affinity constants of 7.3 pM and 13 pM, respectively. It effectively regulates the activation and inactivation of L-type calcium channels, resulting in significant vasodilatory, diuretic, and natriuretic effects. Nesiritide is utilized in research on cardiovascular diseases, particularly in models of heart failure and vascular remodeling following arterial injury. -
MC4R Agonist
Tetracosactide is a potent agonist of the melanocortin-4 receptor (MC4R), activating human MC4R with an EC50 of 0.65 nM. This synthetic analogue of adrenocorticotrophic hormone (ACTH) is known to stimulate the release of corticosteroids, including cortisol, from the adrenal gland. Tetracosactide is utilized in research investigating conditions such as ulcerative colitis, Crohn's disease, and various forms of arthritis, including juvenile and adult rheumatoid arthritis and osteoarthrosis. -
α-adrenergic Receptor Agonist
Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research. -
β1-Adrenergic Blocker
Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker, primarily targeting the β1-adrenergic receptors. This compound demonstrates significant antiarrhythmic properties and is effective in mitigating post-resuscitation myocardial dysfunction. Additionally, esmolol hydrochloride inhibits aldose reductase activity, reducing advanced glycation end products and enhancing fibroblast migration, which contributes to improved diabetic wound healing. It serves as a valuable tool for research into cardiac diseases, including arrhythmias and diabetic foot ulcers. -
5-HT2BR Antagonist
PRX-08066 maleate is a selective antagonist of the 5-hydroxytryptamine receptor 2B (5-HT2BR) with a Ki value of 3.4 nM. It effectively inhibits the MAPK signaling pathway, as well as the release of serotonin and the expression of key fibrotic factors such as TGFβ1, CTGF, and FGF2. PRX-08066 maleate demonstrates the ability to inhibit the proliferation of KRJ-I cells and induce apoptosis via caspase-3 activation. This compound shows potential for research in the context of pulmonary arterial hypertension (PAH) and neuroendocrine tumors (NET). -
β2-adrenergic receptor Antagonist
Zenidolol is a selective β2-adrenergic receptor antagonist, exhibiting a Ki value of 0.7 nM for the β2 receptor, alongside higher Ki values for β1 and β3 receptors at 49.5 nM and 611 nM, respectively. This compound demonstrates significant antitumor activity by inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway in tumor cells. Additionally, Zenidolol has a unique vasodilatory effect specific to pulmonary vessels in mouse models and can serve as an intraocular pressure-lowering agent in ophthalmic research applications. -
Stable Isotope
Terfenadine-d3 is the deuterated form of Terfenadine, which primarily targets the hERG potassium channel as a potent open-channel blocker with an IC50 of 204 nM. As an H1 histamine receptor antagonist, Terfenadine-d3 demonstrates significant biological activity by inducing apoptosis in melanoma cells through the modulation of calcium homeostasis. Its mechanism includes the generation of reactive oxygen species (ROS) and the subsequent activation of caspases -4, -2, and -9, making it valuable for research in cancer biology and apoptosis pathways. -
CXCR4 Antagonist
Nef-M1 is a CXCR4 antagonist peptide derived from the myristoylated protein encoded by the nef gene in HIV. It induces apoptosis by enhancing caspase-3 levels in cancer cells and inhibits critical processes associated with tumor progression, including angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 reduces levels of VEGF-A, phosphorylated GSK-3β, and vimentin while promoting E-cadherin expression. This compound is valuable for research applications focused on colorectal cancer and breast cancer. -
Dopamine Receptor Antagonist
Flupentixol dihydrochloride is a potent antagonist of D1 and D2 dopamine receptors, demonstrating significant inhibition of PI3Kα with an IC50 of 127 nM. This compound exhibits anti-proliferative effects on cancer cells and promotes apoptosis, making it a valuable tool in oncology research. Additionally, Flupentixol has applications in studies related to schizophrenia, anxiety, and depression, contributing to the understanding of these complex neuropsychiatric disorders. -
PAR2 Antagonist
ENMD-1068 hydrochloride is a selective antagonist of protease-activated receptor 2 (PAR2). This compound effectively reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling pathways. Additionally, ENMD-1068 hydrochloride demonstrates the ability to inhibit the proliferation of endometrial cells and induce apoptosis in epithelial cells associated with lesions. This reagent is valuable for research applications in endometriosis and liver fibrosis. -
σ2 Receptor Agonist
PB28 dihydrochloride is a potent σ2 receptor agonist, exhibiting high affinity with a Ki of 0.68 nM, and also acts as a σ1 antagonist with a Ki of 0.38 nM. This compound demonstrates significant biological activity by inhibiting electrically evoked twitch responses in guinea pig bladder and ileum, with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride has been shown to modulate SARS-CoV-2-human protein-protein interactions, induce caspase-independent apoptosis, and display antitumor effects, making it a valuable tool for research in neuropharmacology and cancer biology. -
H1-histamine/P2X7 Receptor Antagonist
Oxatomide is a dual antagonist of the H1-histamine receptor and the P2X7 receptor, noted for its oral bioavailability. It exhibits significant antihistaminic, antiallergic, and anti-inflammatory properties, making it a valuable compound for the study of allergic diseases. Researchers can utilize Oxatomide to investigate mechanisms of allergy and inflammation, contributing to potential therapeutic advancements. -
PAR-1 Antagonist
Atopaxar is a selective and reversible antagonist of the thrombin receptor protease-activated receptor-1 (PAR-1). By inhibiting PAR-1 signaling, Atopaxar serves as an effective antiplatelet agent, disrupting platelet activation and aggregation. This compound is valuable for research applications related to atherothrombotic diseases, providing insights into the mechanisms of platelet-mediated thrombosis and potential therapeutic interventions. -
Adenosine Receptor Agonist
N6-Benzyladenosine is an adenosine receptor agonist that demonstrates significant cytotoxic activity. It effectively induces apoptosis in cells and arrests the cell cycle at the G0/G1 phase, making it a valuable tool for studying cell proliferation and death. Additionally, N6-Benzyladenosine inhibits Toxoplasma gondii adenosine kinase, providing insights into its potential applications in antiparasitic research and glioma studies. -
CBR1 Inhibitor
Hydroxy-PP-Me is a selective inhibitor of the cannabinoid receptor type 1 (CBR1) with an IC50 of 759 nM. It effectively inhibits serum starvation-induced apoptosis and enhances the cytotoxic effects of chemotherapeutic agents such as Daunorubicin and Arsenic Trioxide (As2O3) on tumor cells. Hydroxy-PP-Me is a valuable tool for cancer research, particularly in the study of leukemia and related malignancies.
