Catalog No.
Product Name
Application
Product Information
Citations
-
OX Receptor Antagonist
SB408124 Hcl is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. -
NK3 receptor antagonist
Talnetant Hcl is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM. -
5HT1A antagonist
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 - 0.12 nM for 5-HT. -
5-HT/dopamine receptor antagonist
Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
LPA2 agonist
GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM). -
glutamate receptors agonist
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI). -
5-HT3 receptor antagonist
Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor. -
5HT3 receptor antagonist
Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. -
5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. - Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
- Thioridazine is a dopamine receptor antagonist that displays antipsychotic activity. Recently thioridazine is also reported to successfully kill human cancer stem cells.
-
AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. -
CaSR antagonist
NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM. -
5-HT1D receptor antagonist
BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.
-
Opioid Receptors agonist
BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM). -
Dopamine D2 inhibitor
Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions. -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
5-HT3 antagonist
Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy. - Metoprolol succinate is a cardioselective β-adrenergic receptor blocker with IC50 of 42 ng/mL.
-
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. -
A1 Adenosine Receptor Agonist
CCPA (2-Chloro-N6-cyclopentyladenosine) is a highly selective agonist for A1 adenosine receptors, demonstrating a Ki value of 0.4 nM. This compound effectively inhibits adenylate cyclase, with an IC50 of 33 nM. CCPA is relevant in studies investigating anti-seizure and cardioprotective effects, making it a valuable tool for research related to seizures and myocardial infarction. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Adrenergic Receptor Antagonist
Aaptamine is an alkaloid derived from the marine sponge Aaptos suberitoides, functioning primarily as a competitive antagonist of the α-adrenergic receptor. This compound exhibits significant cytotoxicity against tumor cells, inducing apoptosis and cell cycle arrest while promoting p21 expression through a p53-independent mechanism. Aaptamine also demonstrates a variety of biological activities, including anti-tumor, antioxidant, antibacterial, and analgesic effects, making it a valuable tool for cancer research and therapeutic applications.
