Catalog No.
Product Name
Application
Product Information
Citations
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S1P2 Receptor Antagonist
AB1 is a highly selective antagonist of the sphingosine-1-phosphate receptor 2 (S1P2) with an IC50 of 3.5 nM. It effectively inhibits S1P signaling pathways, leading to the suppression of tumor cell migration, angiogenesis, and the expression of the profibrotic mediator CTGF, while promoting apoptosis in cancer cells. This compound demonstrates significant potential for research focused on solid tumors and their microenvironment. -
Stable Isotope
Adenosine-d-1 is a deuterium-labeled derivative of adenosine, an endogenous autacoid that interacts with four G protein-coupled receptors: A1, A2A, A2B, and A3. This stable isotope serves as a valuable tool for studying adenosine's diverse biological functions and its role in various physiological and pathological processes. Applications include pharmacological research, metabolic studies, and the investigation of signal transduction pathways mediated by adenosine receptors. -
Somatostatin Receptor Agonist
Octreotide pamoate is a synthetic octapeptide and a somatostatin receptor agonist that primarily targets subtypes 2, 3, and 5. It enhances Gi protein activity, leading to a reduction in intracellular cAMP levels. Octreotide pamoate exhibits antitumor activity and induces apoptosis, making it valuable for research in conditions such as acromegaly and other diseases related to somatostatin signaling. Its unique pharmacological profile allows for exploration in various therapeutic applications and biological studies. -
Antitumor Somatostatin Analogue
TT-232 TFA is a somatostatin analogue that primarily targets antitumor activity. It has been shown to effectively induce apoptosis in pancreatic tumor cell lines while simultaneously inhibiting tyrosine kinase activity and stimulating tyrosine phosphatase activity in colon tumor cell lines. TT-232 TFA demonstrates strong anti-tumor effects by inhibiting tumor cell proliferation and promoting apoptosis. This compound is valuable for the development of anti-tumor therapeutics and for investigating the mechanisms of apoptosis. -
PAF Antagonist
Pinusolide is a potent antagonist of the platelet-activating factor (PAF) receptor, critically involved in inflammatory responses and cancer progression. This compound has been shown to inhibit tumor cell proliferation and to induce apoptosis, making it a valuable tool in cancer research. Pinusolide's unique mechanism of action provides insights into PAF-related signaling pathways and potential therapeutic strategies. -
Histamine H1 Receptor Antagonist
Meclizine-d8 is a deuterated derivative of Meclizine, functioning primarily as a histamine H1 receptor antagonist. This compound exhibits significant efficacy in alleviating nausea and preventing motion sickness. Additionally, Meclizine serves as an agonist for the mouse constitutive androstane receptor (CAR) while acting as an inverse agonist for the human CAR, making it relevant for studies on receptor modulation and signaling pathways in pharmacology. -
mGluR5 Antagonist
Fenobam hydrate is a selective mGluR5 antagonist with an IC50 of 84 nM, capable of crossing the blood-brain barrier. It exhibits Kd values of 54 nM and 31 nM for rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate demonstrates anxiolytic properties, inhibits self-administration behavior in rodent models, and induces apoptosis in cancer cells. This compound is valuable for research in neurological disorders, cancer biology, and addiction studies. -
Stable Isotope
D-Mannitol-d2 is a deuterium-labeled derivative of D-Mannitol, primarily used as a stable isotope in various research applications. D-Mannitol is an osmotic diuretic with significant biological activity, promoting calcium and magnesium absorption while reducing tissue edema. Additionally, it has been shown to enhance brown adipocyte formation and improve insulin sensitivity by activating the β3-adrenergic receptor pathway, leading to the conversion of white fat cells into brown fat. This compound is particularly useful in studies involving osmotic pressure regulation and cellular protection in plant and mammalian cell cultures. -
Dopamine D4 Receptor Antagonist
L 741742 is a highly selective antagonist of the dopamine D4 receptor, exhibiting a Ki of 3.5 nM for this target and demonstrating significantly lower affinity for the D2 and D3 receptors. This compound effectively suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, disrupts lysosomal function, and impairs autophagic flux. L 741742 induces G0/G1 cell-cycle arrest and apoptosis, enhances neuronal differentiation in human neural stem cells, and selectively targets the growth of glioblastoma neural stem cells. Its potential therapeutic applications include research in schizophrenia and glioblastoma, with demonstrated synergy when combined with Temozolomide in vitro. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine hydrochloride is a potent modulator of the 5-HT receptor system, functioning as an agonist at the 5-HT1A receptor while antagonizing the 5-HT2A receptor. This compound has demonstrated significant biological activity by inducing apoptosis in various cell types. Additionally, it exhibits potential in combatting immunosuppression and preventing photocarcinogenesis, making it a valuable tool for research in neuroscience and cancer studies. -
Noradrenergic Reuptake Inhibitor
Maprotiline is a selective noradrenergic reuptake inhibitor that exhibits significant antidepressant activity and also shows promise in antitumor and neuropathic pain relief. It facilitates cancer cell apoptosis through modulation of the ERK signaling pathway and interaction with cellular retinoic acid-binding protein 1 (CRABP1). This compound is valuable for research in mental health disorders, oncology, and pain management. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine is a modulator of the 5-HT receptors, functioning as an antagonist at the 5-HT2A receptor and an agonist at the 5-HT1A receptor. It demonstrates a binding affinity for the human 5-HT6 receptor with a Ki value of 120 nM. Additionally, 1-(1-Naphthyl)piperazine has been shown to inhibit forskolin-stimulated adenylate cyclase activity in calf substantia nigra, and it mitigates UV-induced immunosuppression. This compound induces S-phase cell cycle delay and apoptosis while elevating ROS levels, ultimately leading to the inhibition of MNT-1 cell proliferation, making it a valuable tool for melanoma research. -
Dopamine Receptor Antagonist
Flupentixol is an orally active antagonist of D1 and D2 dopamine receptors. This compound exhibits anti-proliferative effects on cancer cells, promoting apoptosis, and has potential applications in the study of schizophrenia, anxiety, and depression. Additionally, Flupentixol has been identified as a new inhibitor of PI3Kα, with an IC50 value of 127 nM, making it a valuable reagent for research in neuropsychiatric disorders and cancer biology. -
Stable Isotope
D-Mannitol-13C,d2 is a stable isotope-labeled form of D-Mannitol, which serves as an osmotic diuretic and explores its role in cellular osmoregulation. D-Mannitol is utilized in various research applications, including the study of calcium and magnesium absorption, as well as promoting brown adipose tissue formation through the activation of β3-adrenergic receptors. It is also valuable in plant cell culture, helping maintain osmotic balance and protecting cells, particularly when cell walls are compromised. This reagent is essential for researchers investigating metabolic pathways, therapeutic interventions, and plant physiology. -
H1 Receptor Antagonist
Chloropyramine is a competitive reversible antagonist of the H1 receptor. It exhibits anti-tumor activity, particularly in breast cancer models. This compound is valuable for research into allergic conditions, including conjunctivitis and bronchial asthma, providing insights into histamine-mediated physiological responses and potential therapeutic interventions. -
LPAAT-β Inhibitor
CT 32228 is an inhibitor of lysophosphatidic acid acyltransferase-β (LPAAT-β), showing significant inhibition of tumor cell growth. It exhibits IC50 values in the range of 0.1-0.8 μM across various leukemia cell lines and effectively induces caspase activation in DHL-4 and Ramos cells. In combination with Rituximab, CT 32228 promotes apoptosis and demonstrates a 50% growth delay in xenograft models. This reagent is suitable for research applications targeting acute leukemia. -
Platelet Aggregation Inhibitor
Ergosta-7,22-dien-3-one functions as a platelet aggregation inhibitor, derived from the fruiting bodies of Ganoderma lucidum. This compound is known to enhance nitric oxide production and promote the expression of specific genes alongside the synthesis of Toll-like receptors (TLRs), cytokines, chemokines, and cellular adhesion molecules in vitro. Ergosta-7,22-dien-3-one is valuable for research in hematology, inflammation, and cellular signaling pathways. -
Monosaccharide
Rhamnose (L-Rhamnose) is a naturally occurring deoxysugar that primarily targets inflammatory pathways. It has been shown to inhibit pro-inflammatory interleukins and matrix metalloproteinases (MMPs) in models of skin aging, highlighting its potential in anti-aging research. Additionally, Rhamnose enhances the phosphorylation of protein kinase A (PKA) substrates and hormone-sensitive lipase (HSL) in adipocytes, promoting PKA signaling and fat metabolism. Its ability to stimulate dopamine receptors and induce thermogenesis makes Rhamnose a valuable compound in obesity studies, while Rhamnose monohydrate is also utilized in research involving Ehrlich’s solid tumors and sarcomas. -
CXCR2 Agonist
Ac-Pro-Gly-Pro-OH acts as a CXCR2 agonist and is an endogenous degradation product of extracellular collagen. This compound demonstrates significant bactericidal activity through hydrogen peroxide generation and plays a role in inhibiting pulmonary inflammation while reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH promotes the secretion of IFN-γ and suppresses the levels of pro-inflammatory cytokines such as TNF-α and IL-6 in leukocytes. It is relevant for research applications in sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcers, notably influencing neutrophil behavior and tissue remodeling processes. -
Soluble Guanylate Cyclase Stimulator
Zagociguat is a soluble guanylate cyclase (sGC) stimulator that is orally active and penetrates the blood-brain barrier. This compound enhances intracellular levels of cGMP, leading to regulation of blood pressure, improved neuronal function, reduced inflammatory responses, and neuroprotective effects. Zagociguat is primarily utilized in research focused on neurodegenerative diseases. -
CXCR2 Antagonist
Elubrixin tosylate is a selective and reversible antagonist of the CXCR2 receptor, functioning as an IL-8 receptor antagonist. This compound effectively inhibits neutrophil CD11b upregulation with an IC50 of 260.7 nM and neutrophil shape change with an IC50 of 310.5 nM. Its biological activity positions Elubrixin tosylate as a valuable tool in research aimed at understanding and treating inflammatory diseases, including inflammatory bowel disease and airway inflammation. -
Platelet Aggregation Inhibitor
5(S),15(S)-DiHETE is a platelet aggregation inhibitor that functions as an activated intermediate in the biosynthesis of specialized pro-resolving mediators. With an IC50 of 1.3 μM, it effectively reduces platelet aggregation. Additionally, 5(S),15(S)-DiHETE enhances the rate of biosynthesis for lipoxins A4 (LXA4) and B4 (LXB4), making it valuable for research applications in inflammation and resolution processes. -
CXCR2 Antagonist
Elubrixin is a potent and selective CXCR2 antagonist, functioning as a competitive and reversible inhibitor of the IL-8 receptor. It effectively impedes neutrophil CD11b upregulation with an IC50 of 260.7 nM and inhibits shape change with an IC50 of 310.5 nM. This compound is valuable in the study of inflammatory diseases, including inflammatory bowel disease and airway inflammation, facilitating insights into pathophysiological mechanisms and therapeutic interventions. -
LPA3 G-protein-coupled Receptor Agonist
(2S)-OMPT is a selective agonist for the LPA3 G-protein-coupled receptor, functioning as a lysophosphatidic acid analogue. This compound triggers downstream signaling pathways, including calcium influx and interleukin-6 (IL-6) release in cancer cells. Additionally, (2S)-OMPT activates critical signaling pathways such as MAPK and Akt. Its unique properties make it a valuable tool for research on ovarian cancer and other related studies. -
Formoterol Enantiomer
(S,S)-Formoterol is the (S,S)-enantiomer of Formoterol, primarily targeting beta-2 adrenergic receptors. This compound has been shown to enhance IL-4 production in mast cells, contributing to inflammatory responses associated with asthma. Its activities make it valuable for research in respiratory pharmacology and the study of asthma pathophysiology. -
CXCR2 Antagonist
Elubrixin hydrochloride is a potent, selective CXCR2 antagonist that operates as a competitive, reversible inhibitor of the IL-8 receptor. It effectively inhibits neutrophil CD11b upregulation and shape change, with an IC50 of 260.7 nM and 310.5 nM, respectively. This compound is valuable for research applications related to inflammatory diseases, including inflammatory bowel disease and airway inflammation. -
CXCR4 Antagonist
Burixafor hydrobromide is a potent CXCR4 antagonist with a pIC50 of 7.4, effectively inhibiting the binding of CXCL12 to the CXCR4 receptor. This compound antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, thereby obstructing the downstream Gαᵢ-mediated inhibition of cAMP signaling. Burixafor hydrobromide is utilized in research for mobilizing CD34+ hematopoietic stem/progenitor cells from the bone marrow to peripheral blood, making it valuable in studies related to autologous hematopoietic stem cell transplantation. -
hD4 Receptor Antagonist
L 741742 hydrochloride is a highly selective antagonist of the human D4 dopamine receptor, exhibiting a Ki value of 3.5 nM for the D4 receptor while demonstrating much lower affinity for D3 and D2 receptors. This compound disrupts signaling pathways associated with PDGFRβ, ERK1/2, and mTOR, and impairs autophagic processes by affecting lysosomal function. Biologically, it induces G0/G1 cell-cycle arrest and apoptosis in various cell types and promotes neuronal differentiation in human neural stem cells. L 741742 hydrochloride is particularly relevant for research on schizophrenia and glioblastoma, demonstrating efficacy against glioblastoma neural stem cells and enhancing the effects of Temozolomide in vitro. -
mGluR2 Negative Allosteric Modulator
mG2N001 is a negative allosteric modulator of the metabotropic glutamate receptor mGluR2, exhibiting an IC50 of 93 nM and a binding affinity (Ki) of 63 nM. This compound demonstrates significant biological activity by modulating glutamatergic signaling pathways, making it valuable for neurological research. Additionally, its radioisotope [11C]mG2N001 is suitable for PET imaging, providing high brain heterogeneity and penetration, allowing for selective accumulation in mGluR2-rich regions, which enhances imaging contrast in neurobiological studies. -
mGluR5 Antagonist
AZD-2066 hydrochloride is a selective antagonist of the metabotropic glutamate receptor 5 (mGluR5) with the ability to penetrate the blood-brain barrier. This compound activates the brain-derived neurotrophic factor (BDNF) and trkB signaling pathway, making it relevant for research into neuropathic pain, major depressive disorder, and gastroesophageal reflux disease. AZD-2066 hydrochloride serves as a valuable tool for investigating the therapeutic potential of mGluR5 modulation in these conditions. -
H1 Receptor Blocker
(R)-(+)-Dimethindene maleate is a selective H1 receptor antagonist, displaying significant antihistaminic activity. It is utilized in research to study allergic responses and histamine-mediated mechanisms in various biological models, including porcine studies. This compound serves as a valuable tool for exploring the effects of histamine signaling and the therapeutic potential of H1 receptor blockade. -
βH Inhibitor AND H1 Receptor Antagonist
Desmethylastemizole is a β-hematin (βH) inhibitor and a Histamine H1 receptor antagonist. It exhibits potent antiplasmodium activity against Plasmodium falciparum, with IC50 values of 0.12, 0.11, and 0.06 μM for the Pf3D7, PfDd2, and PfItG strains, respectively. Additionally, Desmethylastemizole effectively blocks hERG K+ channels and inhibits histone-lysine N-methyltransferase EZH2 activity. This compound is relevant for research in long QT syndrome and malaria. -
H4/H1 Receptor Antagonist
H4R Antagonist 3 is a selective histamine H4 and H1 receptor antagonist with an EC50 of ≤10 mM. This compound is valuable for investigating the mechanisms underlying inflammatory, autoimmune, allergic, and ocular diseases. Its ability to modulate histamine receptor activity makes it a useful tool for research applications focused on these conditions. -
Histamine H3 Receptor Antagonist
Proxyfan is a potent antagonist of the histamine H3 receptor, exhibiting Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptors, respectively. This compound demonstrates over 1000-fold selectivity for the H3 receptor compared to other histamine receptors. Proxyfan is useful in research applications focused on neurological disorders, cognitive enhancement, and sleep regulation, making it a valuable tool for studying histaminergic signaling pathways. -
Histamine H3 Receptor Antagonist
PF-03654764 is a potent and selective antagonist of the histamine H3 receptor, demonstrating Ki values of 1.2 nM for human H3 and 7.9 nM for rat H3 in whole cell assays. This compound exhibits significant potential in research applications related to allergies, particularly in the treatment of allergic rhinitis when combined with other antihistamines. Its oral bioactivity provides a valuable tool for investigating the role of histamine signaling in various physiological and pathological processes. -
Histamine H1 Receptor Antagonist
Diphenylpyraline is a potent histamine H1 receptor antagonist. This compound exhibits anticholinergic and antiallergic properties, making it effective as an orally active antihistamine. Diphenylpyraline is applicable in research focused on allergic conditions, including rhinitis and hay fever, as well as pruritic skin disorders. -
Histamine H1 Receptor Antagonist/5-Lipoxygenase Inhibitor
UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions. -
Stable Isotope
Promethazine-d4 hydrochloride is a deuterated form of Promethazine hydrochloride, a first-generation antihistamine that primarily functions as a strong antagonist of the H1 receptor. It also exhibits moderate antagonistic activity at mACh receptors, alongside a moderate affinity for 5-HT2A, 5-HT2C, D2, and α1-adrenergic receptors. This stable isotope is useful for tracing studies, pharmacokinetic research, and metabolite identification in biological samples. -
Histamine Receptor Inverse Agonist
Mianserin-d3 is a deuterium-labeled form of Mianserin, primarily acting as an H1 receptor inverse agonist. It has demonstrated biological activity by activating κ-opioid and octopamine receptors, while also promoting ERK1/2 and CREB phosphorylation. Mianserin-d3 is valuable for investigating neurological disorders, including depression and epilepsy, and may influence social and exploratory behavior as well as electroconvulsive thresholds. -
Histamine H2 Receptor Antagonist
Cimetidine sulfoxide is a sulfoxide metabolite of the histamine H2 receptor antagonist Cimetidine. This compound demonstrates inhibitory activity at the H2 receptors, making it relevant for research applications involving gastric acid secretion and gastrointestinal disorders. Cimetidine sulfoxide may hold potential for exploring treatment options in peptic ulcer disease and upper gastrointestinal hemorrhage. -
anti-Allergic Agent
Setastine is an orally effective, non-sedative antihistamine that primarily targets H1 histamine receptors. It exhibits significant blocking properties, making it suitable for research applications related to allergies and rhinitis. Its long-acting effects further enhance its potential in exploring various allergic responses in scientific studies. -
Histamine H1 Antagonist
Noberastine is a potent antagonist of the Histamine H1 receptor, exhibiting significant peripheral antihistamine activity. This compound is primarily utilized in research focused on allergic responses and histamine-related disorders. Its ability to effectively inhibit H1 receptor activity makes it a valuable tool for studies investigating antihistaminic properties and related therapeutic applications. -
H4 Receptor Agonist
4-Methylhistamine hydrochloride is a highly selective agonist for the histamine H4 receptor (H4R), exhibiting a Ki value of 50 nM and over 100-fold selectivity compared to other histamine receptor subtypes. With a pEC50 of 7.4, it effectively activates H4R, making it a valuable tool for research in cancer, inflammation, and immunology. Applications include studies related to lung cancer and skin inflammatory conditions, providing insights into H4R-mediated pathways in these areas. -
Histamine Receptor Antagonist
Pimethixene is a potent antagonist of multiple receptor types, primarily functioning as a histamine receptor antagonist. It demonstrates significant activity against serotonin receptors (5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C), dopamine receptors (D2, D4), and muscarinic receptors (M1, M2), with reported pKis of 7.63 to 10.44. This pharmacological profile positions pimethixene as an effective agent for migraine management and offers valuable insights for research into antihistaminic and antiserotonergic therapies. -
Histamine Receptor Antagonist
SUN 1334H is a potent, orally active, and highly selective H1 receptor antagonist, exhibiting a Ki value of 9.7 nM. This compound effectively inhibits histamine-induced signaling, making it valuable for research on allergic responses and related conditions. Its specificity and potency make it suitable for studies investigating the role of H1 receptors in various biological systems. -
Histamine 3 Receptor Inverse Agonist
Samelisant free base is a selective inverse agonist of the histamine H3 receptor (H3R) that exhibits high binding affinity (Ki values of 8.7 nM for human H3R and 9.8 nM for rat H3R). It demonstrates effective brain penetration and oral bioavailability, making it a valuable tool in the study of sleep-related disorders. Research applications include exploring the mechanisms underlying sleep regulation and potential therapeutic interventions for insomnia and other sleep disturbances. -
Histamine H2 Receptor Antagonist
Cimetidine hydrochloride is a potent histamine H2 receptor antagonist with an inhibition constant (Ki) of 0.6 μM. It serves as an effective gastric acid reducer and is widely utilized in research pertaining to duodenal and gastric ulcers. Additionally, Cimetidine hydrochloride exhibits notable anti-cancer and anti-inflammatory properties, making it relevant for various therapeutic investigations. -
Histamine Receptor Antagonist
Adriforant is a selective antagonist of the histamine H4 receptor, exhibiting a binding affinity (Ki) of 2.4 nM and functional antagonism with a Ki of 1.56 nM. It effectively inhibits the actions of histamine, making it a valuable tool for studying the role of H4 receptors in various biological processes. This compound is particularly relevant for research in immunology, allergy, and inflammation, providing insights into potential therapeutic applications targeting histamine-mediated pathways. -
Histamine Receptor
Alcaftadine carboxylic acid selectively targets histamine H1 and H2 receptors, exhibiting broad-spectrum antihistaminic properties. This compound demonstrates significant efficacy in modulating immune cell recruitment and stabilizing mast cells, contributing to its therapeutic effects. Alcaftadine carboxylic acid effectively alleviates ocular itching associated with allergic conjunctivitis, showing superior performance compared to placebo and comparable efficacy to olopatadine 0.01%. This makes it a valuable candidate for research on allergy-related conditions and immune response modulation. -
Histamine 1 Receptor Antagonist
Acrivastine-d7 is a deuterated derivative of Acrivastine, targeting the histamine H1 receptor as an antagonist. It exhibits potent antihistaminic activity, making it valuable in studying allergic reactions and histamine-related pathways. This reagent can be utilized in pharmacokinetic studies and metabolic research involving H1 receptor interactions.
