Catalog No.
Product Name
Application
Product Information
Citations
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Histamine Receptor Inhibitor
Azatadine is a histamine receptor inhibitor that functions by antagonizing H1 and H2 subtypes. This compound exhibits significant biological activity in blocking histamine-mediated processes, making it valuable in research related to allergic responses and motion sickness. Azatadine's mechanism of action also extends to cholinergic pathways, providing further insights into neuropharmacological studies. -
Histamine Receptor Antagonist
(±)-Tazifylline functions as a potent and selective histamine H1 receptor antagonist. This compound exhibits long-acting biological activity, making it valuable in studies related to allergic responses, inflammation, and histamine-mediated physiological processes. Its targeted mechanism allows for exploration in various research applications, including asthma and allergic condition therapeutics. -
5-HT Receptor Inhibitor
Proxibarbal is a barbiturate derivative that acts as a selective inhibitor of the 5-HT receptor. It demonstrates notable anti-anxiety properties and is utilized in research focused on migraine headache mechanisms. This compound serves as a valuable tool for understanding serotonergic pathways and their implications in anxiety and migraine disorders. -
Histamine H2 Receptor Antagonist
FR-145715 is a selective histamine H2 receptor antagonist that exhibits specific activity against Helicobacter pylori. Its inhibition of H2 receptors contributes to its role in research studies focused on gastric lesions and related gastrointestinal disorders. This compound is valuable for investigating therapeutic strategies targeting H. pylori infection and associated pathologies. -
Histamine Receptor Control
Promethazine sulfoxide is a metabolite of the histamine H1 receptor antagonist, promethazine, formed through the action of the cytochrome P450 isoform CYP2D6. This compound exhibits potential biological activity related to histamine receptor modulation, making it relevant for research focused on allergic responses and central nervous system effects. Its involvement in metabolic pathways provides valuable insights for studies examining drug interactions and individual variability in histamine response. -
Histamine Receptor Inhibitor
(S)-Azelastine is a selective antihistamine that primarily targets the histamine H1 receptor. This compound exhibits antiallergic and antiasthmatic properties, demonstrating the ability to downregulate levels of histamine receptors H1R, M1R, and M3R. Additionally, (S)-Azelastine has been found to inhibit the proliferation of human nasal epithelial cells, making it a valuable reagent for research in allergy and asthma mechanisms. -
Histamine Inhibitor
Elbanizine is a potent histamine inhibitor that effectively suppresses histamine and bradykinin release from rat mast cells, demonstrating an IC50 of 0.26 μM. This compound has been shown to inhibit IgE-mediated passive cutaneous anaphylaxis (PCA) reactions. Additionally, Elbanizine exhibits significant antiallergic and antiasthmatic properties in guinea pig models, making it a valuable tool for research in allergy and asthma mechanisms. -
PFA Antagonist
SCH-44643 is a potent antagonist of platelet activating factor (PAF) and histamine receptors. This compound exhibits significant inhibitory activity on PAF-mediated platelet aggregation and histamine-induced responses. It is utilized in research applications focusing on inflammatory processes, cardiovascular disorders, and allergic reactions, contributing to the understanding of PAF and histamine-related pathways in various biological contexts. -
Stable Isotope
Asenapine-d3,13C is a stable isotope-labeled form of Asenapine, an atypical antipsychotic that acts as an antagonist at various serotonin, adrenoceptor, dopamine, and histamine receptors. This compound is valuable for studies investigating the pharmacokinetics and metabolism of Asenapine, particularly in the context of schizophrenia and bipolar disorder research. Its unique isotopic labeling allows for precise tracking and analysis in biochemical assays and in vivo studies. -
Dopamine Receptor Inhibitor
BL-1020 mesylate is a dopamine receptor inhibitor with high affinity for D2L, D2S, and 5-HT2A receptors, exhibiting Ki values of 0.066, 0.062, and 0.21 nM, respectively. This compound functions as an antipsychotic agent and also acts as an agonist at the GABAA receptor, enhancing GABA release with a Ki of 3.74 μM. Furthermore, BL-1020 mesylate interacts effectively with histamine receptors (Ki of 0.47 nM) and demonstrates the ability to diminish amphetamine-induced hyperactivity while minimizing catalepsy and sedation. It penetrates the blood-brain barrier, making it suitable for neurological research applications. -
Histamine H3 Receptor Antagonist
GSK334429 is a selective, orally active non-imidazole antagonist of the histamine H3 receptor, exhibiting a pKi of 9.49 against the human H3 receptor. This compound is important for studies related to neurological disorders and may help elucidate the role of histaminergic signaling in the central nervous system. Its targeted mechanism makes it a valuable reagent for research applications involving neuropharmacology and related fields. -
Histamine Receptor Antagonist
OUP-186 is a selective antagonist of the histamine H3 receptor, which plays a critical role in neurotransmission and the modulation of various physiological processes. It exhibits potent biological activity in blocking H3 receptor-mediated signaling pathways. This compound is useful in research applications focused on understanding central nervous system disorders, sleep regulation, and cognitive functions, making it a valuable tool for pharmacological studies targeting histamine receptors. -
H2 Receptor Agonist
Impromidine is a selective agonist of the histamine H2 receptor, effectively stimulating gastric mucosal blood flow and promoting acid secretion. Its potent activity makes it a valuable tool in studies investigating gastric physiology and the mechanisms underlying acid secretion. Impromidine can be utilized in research related to gastrointestinal disorders and the effects of histamine receptor modulation on gastric function. -
Histamine H1 Receptor Antagonist
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that inhibits histamine activity by competitively binding to H1 receptors in gastrointestinal, vascular, and respiratory tissues. This compound undergoes biotransformation in human liver microsomes, producing hydroxylated and S-oxidized metabolites. Additionally, (R)-(+)-Mequitazine has been shown to inhibit CYP3A-catalyzed midazolam 1'-hydroxylase activity. Its properties make it a valuable reagent for investigating various allergic diseases and related pharmacological studies. -
Histamine Receptor Inhibitor
D18024 is a potent histamine receptor inhibitor that demonstrates antiallergic and antihistaminic properties. This compound exhibits significant activity in modulating histamine-mediated processes, making it useful for research focused on allergy and inflammation pathways. D18024 can be employed in studies investigating the role of histamine receptors in various biological systems, contributing to the understanding of allergic responses and potential therapeutic interventions. -
Histamine Receptor Antagonist
Minocromil is a histamine receptor antagonist primarily employed in the treatment of asthma. It functions by inhibiting the histamine H1 receptor, leading to the reduction of bronchoconstriction and inflammation. This compound is valuable in research related to allergic responses and the development of therapeutic strategies for asthma management. -
Histamine Receptor Inhibitor
CI-949 is a potent histamine receptor inhibitor known for its ability to suppress the release of key allergic mediators. It demonstrates inhibition of histamine, leukotriene C4/D4, and thromboxane B2 with IC50 values of 11.4 μM, 0.5 μM, and 0.1 μM, respectively. This compound is useful for studies focused on allergic reactions and inflammation, providing insights into therapeutic strategies for allergic conditions. -
Histamine Receptor Inhibitor
KP136 is a potent histamine receptor inhibitor that exhibits antiallergic properties. It effectively blocks histamine release with an IC50 of 76.1 μg/mL and degranulation at 63 μg/mL. This compound is valuable for research applications focusing on allergic responses and related inflammation processes. -
Histamine Receptor Antagonist
FRG8701 is a selective antagonist of the Histamine H2 receptor, demonstrating an IC50 range of 0.25 to 0.43 μM. This compound exhibits significant inhibitory activity, making it a valuable tool for investigating histamine signaling pathways and their implications in various physiological processes. Research applications include studies on gastric acid secretion, allergic reactions, and potential therapeutic interventions for related pathologies. -
Histamine Receptor Modulator
H3 receptor-MO-1 is a selective modulator of the histamine H3 receptor, functioning as an antagonist to enhance release of neurotransmitters. This compound is pivotal for research into neurological disorders and sleep regulation, making it a valuable tool in studying the role of histamine in the central nervous system. Its unique pharmacological profile enables investigation into potential therapeutic applications for conditions such as cognitive deficits and mood disorders. -
Stable Isotope
Salbutamol-d3 is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. This compound is primarily employed as a stable isotope for metabolic tracing and pharmacokinetic studies. Salbutamol exhibits significant therapeutic effects by relaxing bronchial smooth muscle, making it a valuable tool in research involving asthma and chronic obstructive pulmonary disease. Additionally, it has been identified to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT pathway, highlighting its utility in oncology research. -
Stable Isotope
Salbutamol-d9 acetate is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. This compound is primarily utilized as a stable isotope for research applications, specifically in studying its effects on bronchial smooth muscle relaxation and the β2-adrenergic receptor pathways. Salbutamol has also been implicated in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling cascade, making it relevant for cancer research as well as respiratory studies. -
Stable Isotope
Salbutamol-d9 is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. It is primarily utilized as a stable isotope in biological research, allowing for the precise tracking of Salbutamol's pharmacokinetics and metabolism. Salbutamol is known for its ability to relax bronchial smooth muscle and is widely studied in the context of asthma and chronic obstructive pulmonary disease, as well as its role in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway. -
mGlu5 Receptor NAM
STX107 is a negative allosteric modulator (NAM) of the metabotropic glutamate 5 (mGlu5) receptor, exhibiting a pKi of 8.32. This compound effectively inhibits glutamate-induced calcium mobilization, inositol monophosphate (IP1) accumulation, and ERK1/2 phosphorylation. Additionally, STX107 prevents glutamate-induced mGlu5 internalization, making it a valuable tool for researching mGlu5 receptor signaling pathways and potential therapeutic applications for neurological disorders. -
Antagonist
Peptide E5 is an antagonist that targets the CXCR4/CXCL12 signaling axis. By blocking this interaction, Peptide E5 downregulates CXCR4 expression and inhibits the phosphorylation of key downstream proteins, Akt and Erk, leading to apoptosis in breast cancer cells. Additionally, Peptide E5 suppresses cellular migration and adhesion, as well as the recruitment of endothelial progenitor cells, thereby inhibiting tumor angiogenesis. This peptide is a valuable tool for research related to breast cancer and tumor microenvironment interactions. -
A1/A2A/A2B Adenosine Receptor Antagonist
Adenosine receptor antagonist 7 is a potent triple antagonist of A1, A2A, and A2B adenosine receptors, demonstrating Ki values of 1.5 nM, 0.6 nM, and 21 nM, respectively. It effectively inhibits cAMP production in A2AR-HEK293 cells with an IC50 of 0.8 nM. This compound enhances the infiltration of effector T cells and increases the CD8+/Treg ratio in conjunction with Avelumab. Adenosine receptor antagonist 7 is valuable for cancer research, particularly in the study of colon cancer. -
CXCR4 Antagonist
Peptide R analogue 10 is a potent CXCR4 antagonist, demonstrating enhanced antagonistic activity, specificity, and plasma stability compared to its predecessor, Peptide R. This compound effectively inhibits CXCL12-mediated cell migration, ERK phosphorylation, and CXCR4 internalization. Peptide R analogue 10 is valuable for research applications involving CXCR4 overexpression in models of leukemia and colon cancer. -
Adrenergic Receptor Agonist
Salbutamol adipate is an orally active short-acting β2-adrenergic receptor agonist. It is known to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT pathway. Additionally, Salbutamol adipate is effective in relaxing bronchial smooth muscle, making it a valuable tool for researching bronchospasm associated with asthma and chronic obstructive pulmonary disease. -
Stable Isotope
Salbutamol-d4 is a deuterated form of the beta-2 adrenergic receptor agonist Salbutamol, designed for stable isotope applications in biochemical research. This compound has been shown to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway. In addition, Salbutamol-d4 is utilized in studies investigating bronchospasms associated with asthma and chronic obstructive pulmonary disease (COPD), allowing for precise tracking of biological processes and metabolic pathways. -
DPP4 Inhibitor
Sitagliptin hydrochloride is a selective DPP4 inhibitor, demonstrating an IC50 of 19 nM. By inhibiting DPP4, this compound prevents the breakdown of incretin hormones, such as GLP-1 and GIP, ultimately increasing their active levels. Additionally, sitagliptin can stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, independent of DPP-4 inhibition. This reagent is applicable in research involving type 1 and type 2 diabetes, and it also exhibits protective effects on pancreatic islet grafts in type 1 diabetes models. -
Stable Isotope
Sitagliptin-d6 is a deuterium-labeled derivative of Sitagliptin, a selective DPP-4 inhibitor that demonstrates an IC50 of 19 nM. By inhibiting the degradation of incretins such as GLP-1 and GIP, Sitagliptin-d6 promotes increased levels of active glucagon-like peptides, thereby enhancing insulin secretion in a glucose-dependent manner. Additionally, it can stimulate GLP-1 secretion from intestinal L cells independently of DPP-4 inhibition, engaging the cAMP/PKA and ERK1/2 signaling pathways. This reagent is valuable for research on type 1 and type 2 diabetes, as well as the protective effects on pancreatic islet grafts. -
ICMT Inhibitor
POP-3MB is an inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 value of 2.5 μM. It effectively alters the subcellular localization of K-Ras, leading to inhibition of Ras activation. Additionally, POP-3MB demonstrates the capacity to inhibit Erk phosphorylation, making it a valuable tool for research into Ras signaling pathways and related oncogenic processes. -
GPR119 Agonist
2-Oleoylglycerol is a GPR119 agonist that activates hGPR119 in transiently transfected COS-7 cells with an EC50 value of 2.5 μM. This lipid enhances the inflammatory response in macrophages and promotes fibrosis through the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. Additionally, 2-Oleoylglycerol stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. Its effects make it a valuable tool for research into non-alcoholic steatohepatitis (NASH) and related metabolic disorders. -
Stable Isotope
2-Oleoylglycerol-d5 is a deuterium-labeled derivative of 2-Oleoylglycerol, a known agonist of GPR119. It exhibits significant biological activity by activating human GPR119 with an EC50 of 2.5 μM in COS-7 cells, enhancing macrophage inflammatory responses and promoting fibrosis through the GPR119/TAK1/NF-κB/TGF-β1 signaling cascade. Additionally, this compound stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol-d5 is particularly useful for studying mechanisms underlying non-alcoholic steatohepatitis (NASH). -
S1P2 Receptor Inhibitor
S118 is an orally active inhibitor of the sphingosine-1-phosphate receptor 2 (S1P2 receptor), which blocks the binding of Dpr1, subsequently reducing β-catenin accumulation. This mechanism inhibits nuclear translocation of the S1P2 receptor, contributing to the attenuation of inflammation, fibrosis, and epithelial-mesenchymal transition (EMT). S118 demonstrates potential for use in research related to idiopathic pulmonary fibrosis (IPF) and other fibrotic diseases. -
Bone Marrow Mesenchymal Stem Cell Inducer
Herpetin is an active lignan that functions as a bone marrow mesenchymal stem cell inducer. It activates the SDF-1/CXCR4 axis and the Wnt/β-catenin signaling pathway, promoting stem cell recruitment and differentiation. This compound is relevant for research applications focused on acute liver injury and related regenerative processes. -
Platelet Aggregation Inhibitor
12(S)-HETrE is a fatty acid metabolite that serves as a potent inhibitor of platelet aggregation. This compound demonstrates significant biological activity in modulating thrombus formation and is valuable in thrombosis-related research applications. Researchers can utilize 12(S)-HETrE to study the molecular mechanisms underlying platelet function and explore potential therapeutic targets in cardiovascular diseases. -
Adenosine Receptor Antagonist
Adenosine receptor antagonist 6 selectively targets the A2A adenosine receptor, exhibiting a Ki value of 19.18 nM. This compound inhibits NECA-mediated cAMP production with an IC50 of 0.089 μM and mitigates immunosuppressive effects by promoting IL-2 and IFN-γ secretion. Additionally, adenosine receptor antagonist 6 counteracts the immunosuppressive actions of adenosine on T-cell activation and cytokine release, demonstrating potential in inhibiting tumor growth in CT26/MC38 xenograft models. It is suitable for research focused on colon cancer. -
PAF Antagonist
Dersalazine sodium is a platelet-activating factor (PAF) antagonist that demonstrates significant anti-inflammatory properties in intestinal models. It has been shown to effectively downregulate IL-17 expression in rodent colitis studies, making it a valuable tool for investigating inflammatory bowel disease and related conditions. Its mechanism of action allows for exploration of PAF-related pathways in various biological contexts. -
PTP4A3 Inhibitor
JMS-053 is a potent and reversible inhibitor of PTP4A3, with an IC50 value of 18 nM. This compound also exhibits significant inhibitory activity against PTP4A1 and PTP4A2, with IC50s of 50 nM and 53 nM, respectively. Additionally, JMS-053 demonstrates inhibition of CDC25B and DUSP3 with IC50 values of 92.6 nM and 207.6 nM, respectively. Through mechanisms such as interference with RhoA and STAT3/p38 signaling pathways, JMS-053 effectively suppresses tumor cell proliferation and migration, making it a valuable tool for investigating various cancers, including ovarian, breast, and colon cancer. -
CXCR4/STAT3 Inhibitor
Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development. -
Dopamine Receptor Antagonist
Pimozide-d4 is a deuterated derivative of Pimozide, functioning primarily as a dopamine receptor antagonist. It demonstrates potent inhibitory activity with Ki values of 1.4 nM, 2.5 nM, and 588 nM against the dopamine D2, D3, and D1 receptors, respectively. Additionally, Pimozide-d4 exhibits affinity for the α1-adrenoceptor (Ki = 39 nM) and inhibits signaling pathways associated with STAT3 and STAT5. This compound is valuable for research focusing on neuropharmacology and the modulation of dopaminergic signaling pathways. -
Stable Isotope
Pimozide-d5 is a stable isotope-labeled form of Pimozide, a potent antagonist of dopamine receptors primarily targeting D2, D3, and D1 receptors with Ki values of 1.4 nM, 2.5 nM, and 588 nM, respectively. This compound also exhibits affinity for the α1-adrenoceptor with a Ki of 39 nM and has been shown to inhibit signaling pathways through STAT3 and STAT5. Pimozide-d5 is valuable in pharmacological studies and research involving dopamine signaling and receptor interaction. -
S1P Inhibitor
Pro-FTY is a sphingosine-1-phosphate (S1P) inhibitor functioning as an anticancer prodrug derived from FTY720. It selectively disrupts S1P signaling in cancer cells using a drug delivery system that reacts with acrolein, demonstrating significant cytotoxic effects on breast cancer cells, including multidrug-resistant variants. Pro-FTY effectively suppresses tumor growth in xenograft models with 4T1 cells and organoids, while maintaining immune cell integrity by avoiding lymphocytopenia. This reagent is valuable for research in cancer therapy and resistance mechanisms. -
Stable Isotope
Pimozide-d5 N-Oxide is a deuterium-labeled derivative of Pimozide, which primarily functions as a dopamine receptor antagonist, exhibiting Ki values of 1.4 nM, 2.5 nM, and 588 nM for dopamine D2, D3, and D1 receptors, respectively. Additionally, this compound has notable affinity for the α1-adrenoceptor with a Ki of 39 nM. Pimozide also inhibits the signaling pathways of STAT3 and STAT5, making it relevant for research applications in neurobiology and cancer biology studies. -
Histamine receptors inhibitor
Histamine Receptors Inhibitor 1 (compound 303) functions as an inhibitor of H1 and H4 histamine receptors. This compound demonstrates key biological activity in modulating inflammatory processes and is particularly relevant for research applications focusing on autoimmune, allergic, and ocular conditions. Its ability to selectively inhibit these receptors makes it a valuable tool for investigating histamine-mediated pathways in various biological contexts. -
Dopamine Receptor Agonist
Apomorphine is a potent dopamine receptor agonist with additional inhibitory effects on monoamine oxidases A and B. It demonstrates neuroprotective properties, evidenced by its ability to reduce reactive oxygen species production, inhibit DNA fragmentation, and downregulate JNK and ERK1/2 phosphorylation. Apomorphine also facilitates the degradation of intracellular Aβ40 and Aβ42, lowers tau protein levels, and suppresses MMP-9 expression. Its radical scavenging and iron chelating capabilities make it valuable for research in neurodegenerative conditions such as Alzheimer's disease and Parkinson's disease, as well as studies related to breast carcinoma and erectile dysfunction. -
PDD4 Inhibitor
Sitagliptin phosphate is a selective DPP4 inhibitor with a powerful mechanism of action, featuring an IC50 value of 19 nM. By inhibiting DPP4, this compound prevents the degradation of incretins such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), resulting in enhanced active incretin levels. Additionally, it can directly stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, which operates independently of DPP-4. Sitagliptin phosphate is valuable for researching both type 1 and type 2 diabetes and demonstrates protective effects on pancreatic islet grafts in type 1 diabetes models. -
CRFR Agonist
Urocortin II, human is a selective agonist of the type-2 corticotropin-releasing factor (CRF2) receptor, exhibiting key biological activities that include promoting satiety and providing neuroprotective effects. This peptide also demonstrates bactericidal and antiparasitic properties, as well as pro-inflammatory activity. Additionally, Urocortin II, human can activate the NF-κB pathway and ERK1/2 MAP kinase, making it relevant for research in pulmonary arterial hypertension and cardiac protection. Its diverse applications extend to studies in infection, inflammation, metabolic disorders, neurological conditions, and cardiovascular diseases. -
Stable Isotope
Sitagliptin-d4 phosphate is a deuterium-labeled derivative of Sitagliptin phosphate, a selective inhibitor of dipeptidyl peptidase-4 (DPP4) with an IC50 value of 19 nM. This compound increases the levels of active incretins by inhibiting the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Additionally, Sitagliptin-d4 phosphate can stimulate GLP-1 secretion from intestinal L cells through the activation of the cAMP/PKA and ERK1/2 pathways, independent of DPP-4. This reagent is valuable for research into type 1 and type 2 diabetes and can contribute to studies exploring pancreatic islet function.
