Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Stable Isotope
Thioridazine-d3 hydrochloride is a deuterium-labeled derivative of Thioridazine, an antagonist of dopamine receptor D2 family proteins. It demonstrates significant anti-psychotic and anti-anxiety effects while also inhibiting the PI3K-Akt-mTOR signaling pathway, contributing to anti-angiogenic activity. Additionally, Thioridazine exhibits antiproliferative properties and induces apoptosis in various cancer cell types, with particular efficacy against cancer stem cells (CSCs). This stable isotope is valuable for pharmacokinetic studies and elucidating mechanisms of action in related research applications. -
ETA/ETB Antagonist
Macitentan-d4 is a deuterated analog of the dual ETA and ETB endothelin receptor antagonist, Macitentan. This compound exhibits significant biological activity by blocking the effects of endothelin-1, which is implicated in conditions such as pulmonary arterial hypertension (PAH) and idiopathic pulmonary fibrosis (IPF). Macitentan-d4 serves as a valuable tool for research into the underlying mechanisms of endothelin signaling and its role in cardiovascular and pulmonary disorders. -
Endocannabinoid
Arachidonoyl ethanolamide phosphate functions as an endogenous ligand for cannabinoid receptors, primarily targeting the CB1 subtype in the central nervous system and the CB2 subtype in peripheral immune cells. This compound is involved in modulating various physiological processes, including pain perception, mood regulation, and immune response. Its unique action profile makes it useful for research in neurobiology and immunology, particularly in studies focusing on the endocannabinoid system and its implications in various diseases. -
Stable Isotope
N-(Phenylacetyl-d5)glycine is a deuterated form of phenylacetylglycine, functioning as a stable isotope. This compound serves as a gut microbial metabolite that can activate the beta-2 adrenergic receptor (β2AR). Its biological activity includes providing protective effects against cardiac injury induced by ischemia and reperfusion, making it valuable for research in cardiac health and metabolic studies. -
Stable Isotope
D-Mannitol-13C6 is a stable isotope-labeled form of D-Mannitol, targeting metabolic pathways through its role as an osmotic agent. This compound is utilized in various research applications, including studies on calcium and magnesium absorption, cecal fermentation, and the modulation of insulin sensitivity. D-Mannitol has been shown to promote the browning of white adipose tissue by activating the β3-adrenergic receptor, which can lead to enhanced thermogenesis and potential reductions in blood glucose levels. Additionally, it is employed in plant cell culture to maintain osmotic balance and protect cellular integrity. -
Stable Isotope
D-Mannitol-13C is a stable isotope-labeled derivative of D-Mannitol. This compound serves as a valuable osmotic diuretic and is utilized in various research applications, including the study of calcium and magnesium absorption and retention through cecal fermentation. D-Mannitol is known to promote brown adipose tissue formation, enhance insulin sensitivity, and lower blood glucose levels by activating the β3-adrenergic receptor, leading to the conversion of white fat cells into brown fat cells. Additionally, it is employed to maintain osmotic pressure in plant cell cultures, aiding in cellular protection during physiological manipulation. -
Stable Isotope
Perphenazine-d4 is a deuterated derivative of Perphenazine, a typical antipsychotic agent primarily inhibiting the 5-HT2A receptor, alpha-1A adrenergic receptor, dopamine receptor D2/D3, D2L receptor, and histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, allowing for the precise tracking of Perphenazine metabolism and distribution in biological systems. Perphenazine-d4 is essential for researchers focusing on neuropharmacology and drug interaction studies involving antipsychotic medications. -
Antihistamine Agent
Meclizine is an antihistamine that reversibly inhibits the binding of histamine to H1 receptors, making it effective as an anti-motion sickness agent. As a piperazine derivative, it can cross the blood-brain barrier, enabling its use in neurological research. Additionally, Meclizine acts as an agonist for the mouse constitutive androstane receptor (CAR) and serves as an inverse agonist for the human equivalent. This compound is also relevant for studying polyglutamine (polyQ) toxicity disorders, including Huntington's disease. -
Stable Isotope
D-Mannitol-2-13C is a stable isotope-labeled derivative of D-Mannitol. This 13C-labeled compound plays a critical role in metabolic studies, particularly in understanding carbohydrate metabolism and energy homeostasis. D-Mannitol serves as an osmotic diuretic, promotes the absorption of minerals, enhances brown adipose tissue formation, and demonstrates potential for reducing blood glucose levels through β3-adrenergic receptor activation. It is frequently employed in cell culture applications to maintain osmotic pressure and protect cells, particularly when cell walls are compromised. -
Antihistamine Agent
Meclizine dihydrochloride monohydrate is an antihistamine that reversibly inhibits histamine interactions at the H1 receptor. As a member of the piperazine class of H1 antagonists, it is primarily utilized as an effective anti-motion sickness agent. This compound also demonstrates the ability to cross the blood-brain barrier and functions as an agonist for the mouse constitutive androstane receptor (CAR), while acting as an inverse agonist for the human CAR. It has applications in research focusing on polyQ toxicity disorders, including Huntington's disease. -
Somatostatin Receptor Agonist
Octreotide dihydrochloride is a synthetic octapeptide that acts as an agonist for somatostatin receptors, primarily targeting subtypes 2, 3, and 5. By increasing Gi protein activity, it effectively reduces intracellular cAMP levels, contributing to its antitumor effects. Octreotide dihydrochloride is utilized in research applications related to apoptosis and is particularly relevant in studies of acromegaly and other disorders associated with aberrant somatostatin signaling. -
A1 Adenosine Teceptors Agonist
CCPA hemihydrate is a highly selective agonist of the A1 adenosine receptors, exhibiting a Ki value of 0.4 nM. It demonstrates preferential binding to the A1 receptor over the A2 receptor, with a Ki of 3900 nM. As a purine nucleoside analog, CCPA hemihydrate has demonstrated broad antitumor activity, particularly in the context of indolent lymphoid malignancies. Its anticancer effects are mediated through mechanisms such as inhibition of DNA synthesis and induction of apoptosis, making it valuable for research applications in cancer therapy. -
S1P1 Receptor Agonist
(S)-FTY-720 Vinylphosphonate is a chiral phosphonate analogue of Fingolimod that functions as an S1P1 receptor agonist. It demonstrates significant biological activity, activating the S1P1 receptor with an EC50 of 75 nM and effectively inhibiting Camptothecin-induced apoptosis in IEC-6 cells. This reagent is relevant for research into autoimmune diseases, providing insights into therapeutic mechanisms and potential interventions. -
mGlu1 Antagonist
LY456236 free base is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), showing an IC50 for phosphatidylinositol hydrolysis of 0.145 μM. Additionally, it inhibits epidermal growth factor receptor (EGFR) activity with an IC50 of 0.918 μM. This compound effectively blocks cell proliferation by targeting the MAPK signaling pathway, counteracting the anti-apoptotic effects of DHPG. LY456236 free base is a valuable tool for research into epilepsy and other neurological disorders. -
Stable Isotope
Cyproheptadine-d3 is a deuterium-labeled derivative of the antihistamine Cyproheptadine, serving as a stable isotope for research applications. It primarily acts as a serotonin and histamine receptor antagonist, making it useful in studies investigating receptor interactions and pharmacokinetics. This reagent is valuable for tracing and quantifying Cyproheptadine in various biological samples, facilitating research in pharmacology and toxicology. -
β2AR Activator
Phenylacetylglycine is a gut microbial metabolite that acts as a β2-adrenergic receptor (β2AR) activator. It has demonstrated protective effects against cardiac injury resulting from ischemia/reperfusion. This compound is significant for research into cardiovascular health and the role of microbiota in modulating cardiac responses. -
Dopaminergic Neurotoxin
MPTP (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is a potent dopaminergic neurotoxin that readily penetrates the blood-brain barrier. It is primarily utilized to create animal models of Parkinson’s Disease, enabling the study of neurodegenerative processes. MPTP acts by converting into MPP+, which induces apoptosis in dopaminergic neurons, serving as a valuable tool for investigating therapeutic strategies and the underlying mechanisms of neurodegeneration. -
Platelet Aggregation Inhibitor
Epoprostenol sodium, a synthetic derivative of prostaglandin I2, primarily acts as a potent inhibitor of platelet aggregation. This compound is widely recognized for its role in the management of pulmonary arterial hypertension (PAH) and is utilized in clinical settings such as pulmonary hypertension and organ transplantation. Its ability to modulate vasodilation and inhibit platelet activation makes it a valuable tool in related biomedical research applications. -
Histamine Release Inhibitor
Alginic acid is a natural polysaccharide recognized for its ability to inhibit histamine release, making it a valuable compound for research into allergic reactions and inflammation. Its remarkable water solubility, film-forming properties, and biodegradability enhance its applicability in various biological studies. Alginic acid has been demonstrated to induce oxidative stress-mediated effects, resulting in hormone secretion disorders, apoptosis, and autophagy in mouse granulosa cells and ovaries. This compound is of particular interest in anti-anaphylactic and anti-inflammatory research applications. -
Stable Isotope
Kynurenic acid-d5 is a deuterium-labeled analog of kynurenic acid, an endogenous metabolite of tryptophan. It acts as a broad-spectrum antagonist of NMDA and glutamate receptors, as well as the α7 nicotinic acetylcholine receptor. Additionally, kynurenic acid-d5 serves as an agonist for GPR35/CXCR8, making it valuable in studies related to neuropharmacology and neurotransmitter signaling pathways. This stable isotope is ideal for tracing and characterization studies in metabolic research.
