Catalog No.
Product Name
Application
Product Information
Citations
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sst4 Receptor Agonist
L-803087 TFA is a potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. Demonstrating over 280-fold selectivity for the sst4 receptor compared to other somatostatin receptors, L-803087 TFA enhances AMPA-mediated synaptic responses in the hippocampus. This compound is also noted for its role in increasing kainate-induced seizures in murine models, making it valuable for research into neurophysiological processes and receptor signaling mechanisms. -
SST1 Antagonist
SST1 receptor antagonist-2 is a piperazine derivative that selectively inhibits somatostatin receptor 1 (SST1). This compound displays significant potential in the investigation of psychiatric disorders, neurodegenerative diseases, tumors, vascular conditions, and immunological diseases. Its selective antagonism of SST1 may provide insights into various pathological processes and therapeutic strategies. -
SSTR2 Agonist
Branosotine is a potent agonist of the somatostatin receptor subtype 2 (SSTR2), exhibiting an EC50 of less than 0.1 nM. This compound demonstrates significant biological activity in modulating neuroendocrine signaling pathways, making it a valuable tool for research involving neuropsychiatric disorders and hormonal regulation. Its high specificity and efficacy position Branosotine as an important reagent for studying SSTR2-related biological processes. -
Somatostatin Receptor Agonist
Zavolosotine is an orally active agonist of the somatostatin receptor type 5 (SST5), exhibiting a potent EC50 of less than 1 nM. This compound effectively inhibits insulin and glucagon secretion while also elevating glucagon levels in a rat model. Zavolosotine is valuable for research in glucose metabolism and endocrine signaling pathways, making it a key reagent for studies on metabolic disorders and diabetes. -
SSTR4 Agonist
Mazisotine tartrate is a potent SSTR4 agonist that selectively activates the somatostatin receptor subtype 4. This compound is primarily involved in modulating neuroendocrine functions and has potential applications in the study of metabolic disorders, neuroprotection, and cancer therapy. Its biological activity suggests utility in investigating signaling pathways linked to this receptor subtype, making it a valuable tool for research in endocrinology and related fields. -
SSTR5 Antagonist
SSTR5 Antagonist 3 is a potent inhibitor targeting the somatostatin receptor subtype 5 (SSTR5) with IC50 values of 2.8 nM in human tissues and 1.4 nM in mouse models. This orally bioavailable compound exhibits low hERG inhibition, making it suitable for in vivo studies. SSTR5 Antagonist 3 is primarily utilized in research focusing on anti-gallstone therapies and the modulation of related gastrointestinal functions. -
Urotensin II Anague
Urotensin II-related peptide is an analog of human urotensin II, exhibiting high affinity for the urotensin II receptor (UT). This peptide plays a significant role in cardiovascular regulation and may influence vascular smooth muscle contraction. It is commonly utilized in research focused on cardiovascular diseases, neurobiology, and the study of peptide receptor interactions. -
Urotensin Receptor Antagonist
SB-611812 is a selective antagonist of the urotensin II receptor (UTR), which plays a significant role in cardiovascular regulation. This compound is useful in investigating the pathological mechanisms underlying cardiovascular diseases and may aid in the development of novel therapeutic strategies targeting UTR-mediated pathways. Researchers can utilize SB-611812 to explore its effects on vascular function and cardiac remodeling in experimental models. -
Urotensin II Receptor Antagonist
SB-706375 is an antagonist of the Urotensin II (UII) receptor, which plays a key role in renal physiology. By inhibiting this receptor, SB-706375 effectively decreases the kidney's response to UII and Urotensin-related peptide (URP), leading to a significant increase in Glomerular Filtration Rate (GFR). This compound is valuable for research applications focused on kidney diseases and hypertension, facilitating further understanding of renal function and associated pathologies. -
Urotensin-II Receptor Antagonist
GSK 1562590 hydrochloride is a potent and selective antagonist of the urotensin-II receptor (UT), exhibiting pKi values ranging from 9.14 to 9.66 across various mammalian species, including mouse, rat, cat, monkey, and human. This compound demonstrates significant inhibition of UT-mediated signaling pathways, making it valuable for research into cardiovascular and neuroendocrine disorders associated with urotensin-II. Its high affinity and selectivity position GSK 1562590 as an essential tool for studying the role of urotensin-II in physiological and pathological processes. -
urotensin-II Receptor Antagonist Peptide
Urantide is a selective and competitive antagonist of the urotensin-II (UT) receptor, exhibiting a pKB of 8.3. This peptide effectively inhibits human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide is valuable for investigating the (patho)physiological roles of hU-II in the mammalian cardiovascular system, making it an important tool for related research applications. -
Urotensin Receptor Agonist
Urotensin II (114-124), human, is a peptide comprising 11 amino acids that functions as a potent vasoconstrictor and an agonist for the urotensin receptor (GPR14). This compound is utilized in research to explore cardiovascular function and pathophysiology, particularly regarding its role in regulating vascular tone and blood pressure. Its biological activity makes it a valuable tool for studying urotensin signaling pathways and their implications in various disease states. -
Urotensin II Antagonist
Palosuran hydrochloride is a selective, orally active antagonist of the urotensin II receptor, exhibiting an IC50 of 3.6 nM in CHO cell membranes expressing human recombinant receptors. This compound demonstrates potential to improve pancreatic and renal function in diabetic models, making it a valuable tool for research in metabolic and renal disorders. Its mechanism and target highlight its relevance in studies of urotensin II signaling pathways. -
Urotensin Receptor Agonist
AC-7954 free base is a selective nonpeptidic agonist of the urotensin receptor, demonstrating an EC50 of 300 nM at the human urotensin II receptor. This compound is valuable for research focused on the urotensin signaling pathway and its implications in cardiovascular and metabolic disorders. Its specificity makes it suitable for studies investigating the physiological and pathological roles of urotensin receptors in various biological systems. -
Urotensin Receptor Agonist
AC-7954 is a selective nonpeptidic agonist of the urotensin receptor, exhibiting an EC50 of 300 nM at the human urotensin II receptor. This compound plays a significant role in cardiovascular and metabolic research, with potential applications in the study of hypertension and heart failure. AC-7954 can be utilized to explore urotensin-related signaling pathways and their implications in various physiological processes. -
Urotensin Receptor Antagonist
SB-436811 is a selective antagonist of the urotensin-II receptor, exhibiting a pKi value of 6.7. This compound is primarily utilized in research focused on cardiovascular and metabolic disorders, where the urotensin-II pathway plays a significant role. By inhibiting urotensin-II activity, SB-436811 can aid in the exploration of its physiological effects and potential therapeutic applications. -
Endothelin A Receptor Antagonist
JKC 301 is a selective Endothelin A receptor antagonist that effectively mitigates the pressor effects of nicotine in rat models. This compound is particularly valuable for investigating the cardiovascular diseases associated with smoking. Its targeted mechanism makes JKC 301 a useful tool for researchers studying the pathophysiological effects of nicotine on cardiovascular function. -
Precursor of Endothelin-1
Big Endothelin-1 (1-39), porcine is the precursor peptide of endothelin-1 (ET-1), a potent vasoconstrictor significantly involved in cardiovascular regulation. This reagent exhibits similar pressor effects in vivo, making it valuable for studies investigating vascular function and regulation. It is useful in research applications that aim to elucidate the roles of endothelin peptides in physiological and pathological processes. -
Endogenous Metabolite
8-(3-Chlorostyryl)caffeine is a selective antagonist of the A2a adenosine receptor, demonstrating a significant 520-fold selectivity in radioligand binding assays conducted in rat brain. It effectively inhibits adenylylase with a 22-fold selectivity in rat chromaffin cells. Co-administration with the A1-selective antagonist CPX has been shown to enhance exercise activity. Additionally, 8-(3-Chlorostyryl)caffeine exhibits potent inhibitory activity against MAO-B in primate mitochondrial systems. This compound serves as a valuable tool for studying adenosine receptor signaling and its effects on physiological processes. -
Endogenous Metabolite
Palmitoleoyl ethanolamide (POEA) is an endogenous fatty amide that functions primarily as a signaling molecule through the activation of cannabinoid receptors. It has been shown to exhibit anti-inflammatory and analgesic properties, making it relevant for research in pain management and inflammatory disorders. POEA's involvement in metabolic processes also positions it as a valuable target for studies in obesity and metabolic syndrome. -
Endogenous Metabolite
5-OAHSA is an endogenous metabolite that functions as a lipid mediator. It is known to lower blood glucose levels, enhance glucose tolerance, and stimulate the secretion of glucagon-like peptide-1 (GLP-1) and insulin. 5-OAHSA is valuable for research applications focused on metabolic regulation and inflammation modulation. -
Endogenous Metabolite
Hydroxy bosentan is an endogenous metabolite derived from Bosentan, primarily processed by the cytochrome P450 system in the liver. This compound retains 10%-20% of Bosentan's pharmacological activity, serving as a significant contributor to the overall therapeutic effects of the parent compound. Hydroxy bosentan is useful in research focused on metabolic pathways and the pharmacokinetics of endothelin receptor antagonists. -
Endogenous Metabolite
AZD-3199 is an ultra-long-acting beta2 adrenergic agonist primarily targeting the beta2 adrenergic receptor. It exhibits significant bronchodilator activity, making it a candidate for therapeutic use in asthma and chronic obstructive pulmonary disease (COPD) research. Its prolonged action facilitates investigations into novel treatment strategies for managing these respiratory conditions. -
Drug Derivative
Bmapn is a drug derivative with impactful interactions on dopamine signaling pathways. It exhibits rewarding and reinforcing properties by decreasing dopamine transporter levels and enhancing dopamine receptor D2 gene expression specifically in the striatum. This compound is valuable for research applications studying addiction, neuropharmacology, and the modulation of dopaminergic systems. -
Stable Isotope
Boc-Leu-OH·H2O-13C is a stable isotope-labeled derivative of N-Boc-L-leucine, featuring a carbon-13 (13C) label. This amino acid derivative, protected with a Boc group, serves as an essential building block for the synthesis of peptides, such as L-prolyl-L-leucyl-glycinamide, which exhibit modulatory activity on dopamine receptors. It is valuable for applications in peptide research, metabolic studies, and tracer experiments utilizing stable isotopes. -
Histamine N-methyltransferase
Histamine N-methyltransferase, rat is a biocatalyst that functions primarily by catalyzing the N-methylation of histamine. This enzyme plays a critical role in the metabolism of histamine, contributing to the regulation of physiological processes such as inflammatory responses and neurochemical signaling. Research applications include enzyme engineering aimed at optimizing reaction kinetics, enhancing substrate specificity, and improving enzyme stability under varying pH conditions, potentially facilitating dynamic control of enzymatic activity for various experimental needs. -
Activation Peptide
Enterostatin (rat) is an activation peptide of procolipase that plays a significant role in modulating fat intake. This peptide selectively reduces body fat consumption and lowers serum cholesterol levels through a cholecystokinin 1 (CCK1) receptor-dependent mechanism. It serves as a valuable tool for research on energy balance, appetite regulation, and metabolic disorders. -
N-acylserinol Compound
Myristoyl ethanolamide, an N-acylserinol compound, functions as a bioactive lipid signaling molecule. It is involved in modulating various biological processes, including inflammation and pain perception. Myristoyl ethanolamide serves as a valuable tool in research applications focused on lipid metabolism, neuromodulation, and the study of cannabinoid receptor interactions. This compound can enhance the understanding of endocannabinoid signaling pathways and their implications in physiological and pathological conditions. -
Blood Platelet Aggregation Inhibitor
Ent-8-Iso-15(S)-prostaglandin F2α is a potent inhibitor of blood platelet aggregation. This compound exhibits superior activity compared to its isomer, 8-Isoprostaglandin F2α, in whole blood assays, making it a valuable tool for studying platelet function and related cardiovascular research. Its mechanism of action can aid in the exploration of therapeutic strategies for conditions associated with abnormal platelet aggregation. -
Endogenous Metabolite
9(R)-HODE is a monohydroxy fatty acid and an endogenous metabolite of linoleic acid, generated through the enzymatic actions of cyclooxygenase (COX) and lipoxygenase (LO). This compound is known to promote chemotaxis and elevate the expression of chemokine receptors CCR9 and CXCR4 in immune cells. Additionally, 9(R)-HODE effectively inhibits interleukin-6 (IL-6) release in primary human monocytes and suppresses CD3α- and CD28-induced proliferation in isolated human peripheral blood lymphocytes at a concentration of 25 μg/mL, making it a valuable tool for studying immune responses and inflammatory processes. -
2-arachidonoylglycerol derivative
1-Monoarachidin is a 2-arachidonoylglycerol derivative that primarily acts as a modulator of cannabinoid receptors. This fatty acid plays a crucial role in the endocannabinoid system, contributing to various biological processes such as inflammation and neuroprotection. It is utilized in research to investigate the physiological effects of endocannabinoids and their potential therapeutic applications in neurological and inflammatory disorders. -
O-Alkyl-N-acyloxy Homologues
Oxy-Arachidonoyl ethanolamide is an O-alkyl-N-acyl oxime derivative that acts on O-Alkyl-N-acyl homologues. This compound exhibits significant biological activity, particularly in the modulation of endocannabinoid systems. It is employed in research applications focusing on cannabinoid receptor signaling, lipid metabolism, and neuroprotective studies, illuminating potential therapeutic pathways for various neurological diseases. -
Endogenous Metabolite
N-Methylarachidonamide is an analog of the endogenous cannabinoid anandamide, primarily targeting the central cannabinoid receptor (CB1). This compound exhibits a binding affinity with a Ki value of 60 nM for CB1, influencing various physiological processes. Additionally, it effectively inhibits rat glial gap junction cell-cell communication by 100% at a concentration of 50 μM. As such, N-Methylarachidonamide is a valuable tool for research exploring cannabinoid receptor signaling and its implications in neurobiology and related fields. -
FAAH Inhibitor
3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone is a potent inhibitor of fatty acid amide hydrolase (FAAH) with a pI50 of 5.89. This compound exhibits significant activity against endocannabinoids and lipid mediators, making it relevant for studies in pain management, inflammation, and cannabinoid signaling pathways. Its limited affinity for cannabinoid receptors CB(1) and CB(2) allows for targeted research into FAAH-related physiological processes without direct receptor modulation. -
NR4A1 Inhibitor
Glycerol kinase, microorganism functions as an NR4A1 inhibitor by directly binding to and inhibiting the transcription factor NR4A1, which plays a critical role in hepatic gluconeogenesis. This inhibition leads to reduced blood glucose levels and positively influences UCP1 expression through the β-adrenergic receptor-cAMP-CREB signaling pathway, promoting the browning of white adipose tissue and enhancing thermogenesis. Additionally, it modulates intracellular fatty acid composition and energy metabolism. Research using glycerol kinase in diabetic mouse models has demonstrated its ability to counteract NR4A1-induced hyperglycemia, indicating its potential applications in diabetes and obesity studies. -
Bile Acid Sequestrant
Colesevelam hydrochloride is a bile acid sequestrant that primarily acts by binding bile acids in the gastrointestinal tract, leading to the formation of nonabsorbable complexes. This action interrupts enterohepatic recirculation and enhances fecal bile acid elimination. In addition to lowering lipids, colesevelam modulates FXR, TGR5, and CYP7A1 activities, which in turn activates cAMP signaling and promotes GLP-1 release. Its applications in research include investigations into type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease, while also influencing hepatic lipid and glucose metabolism. -
Platelet Aggregation Inhibitor
Myrianthic acid is a pentacyclic triterpenoid that functions as a platelet aggregation inhibitor. Isolated from the root wood of Myrianthus arboreus and the leaves of Campsis grandiflora, it effectively inhibits adrenaline-induced platelet aggregation, demonstrating an IC50 of 46.2 μM. This compound is valuable for research applications focused on thrombosis and related cardiovascular disorders. -
NR2B Antagonist
NMDA-IN-1 dihydrochloride is a selective antagonist of the NMDA NR2B receptor, exhibiting a Ki of 0.85 nM and an IC50 of 9.7 nM for NR2B-mediated Ca2+ influx. This compound effectively inhibits Glu/Gly-stimulated Ca2+ flux in Ltk- cells expressing hNR1a/NR2B, demonstrating specificity as it does not interact with NR2A, NR2C, NR2D, hERG channels, or α1-adrenergic receptors. NMDA-IN-1 dihydrochloride displays significant efficacy in mechanical hyperalgesia models in rats and is relevant for investigations into stroke, Parkinson's disease, and neuropathic pain. -
σ Receptor Agonist
threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research. -
IBAT Inhibitor
Elobixibat hydrate is an orally active inhibitor of the intestinal bile acid transporter (IBAT), demonstrating potent activity with IC50 values of 0.53 nM for human IBAT, 0.13 nM for mouse IBAT, and 5.8 nM for canine IBAT. This compound has been shown to effectively lower LDL cholesterol levels, enhance serum GLP-1 concentrations, and promote colonic motility. Elobixibat hydrate is valuable for research applications related to chronic idiopathic constipation (CIC), dyslipidemia, non-alcoholic fatty liver disease, and the study of liver tumors, particularly in elderly populations. -
P/Q Type Ca2+ Channel Blocker
ω-Agatoxin IVA is a highly selective blocker of P/Q type calcium channels (Cav2.1), with IC50 values of 2 nM and 90 nM. This compound effectively inhibits glutamate exocytosis and calcium influx triggered by elevated potassium levels. Additionally, ω-Agatoxin IVA suppresses capsaicin-induced CGRP release and associated vasodilation. It is valuable for investigations into neurological and cardiovascular diseases, contributing to the understanding of calcium channel modulation in these contexts. -
Racemate of NNC 55-0396
(Rac)-NNC 55-0396 is a racemic mixture that targets the dopamine D2 receptor. This compound is of significant interest in neurological research due to its potential role in modulating dopaminergic signaling pathways. It is commonly utilized in studies investigating the pharmacological effects of dopamine receptor antagonists in various neurological disorders. -
Cholecystokinin
Cholecystokinin-J is a cholecystokinin peptide that primarily targets the cholecystokinin receptor. It is known to stimulate Ca2+ release, playing a significant role in various physiological processes such as digestion and satiety. This reagent is valuable for research applications in gastrointestinal physiology and neurobiology, facilitating studies on CCK-related pathways and functions. -
Stable Isotope
O-Desmethyl carvedilol-d5 is a deuterium-labeled derivative of O-Desmethylcarvedilol, a potent active metabolite of the non-selective β-adrenergic receptor antagonist Carvedilol. This compound exhibits inhibitory effects on store-overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation, with an IC50 of 7.62 μM. Additionally, O-Desmethyl carvedilol-d5 contributes to cardiovascular research by attenuating heart rate increases and stabilizing diastolic blood pressure in response to Isoproterenol in conscious rabbit models, demonstrating ED50 values of 32 and 5 μg/kg, respectively. -
Lipid
DMG-PEG is a lipid compound that enhances the hydrophilicity and electrical neutrality of lPEI/DNA nanoparticles, facilitating improved transport and diffusivity in the gastrointestinal mucus layer. This pegylated lipid is pivotal in formulating liposomes for siRNA delivery, significantly increasing transfection efficiency. In vivo studies demonstrate that nucleic acid nanoparticles coated with DMG-PEG effectively maintain elevated levels of glucagon-like peptide-1 (GLP-1) expression in liver, lung, and intestinal tissues of type II diabetic mouse models, while also regulating blood glucose levels. Additionally, DMG-PEG serves as an effective component in the preparation of lipid nanoparticles for mRNA therapeutics. -
MAGL Inhibitor
OMDM169 is a selective inhibitor of monoacylglycerol lipase (MAGL), effectively increasing the levels of 2-arachidonoylglycerol (2-AG) in biological systems. This compound demonstrates significant analgesic properties through the indirect activation of cannabinoid receptors. OMDM169 exhibits an effective concentration of 0.13 μM, making it a valuable tool for research focused on pain modulation and cannabinoid receptor signaling pathways. -
HIF Inhibitor
Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models. -
P2X1 Receptor Antagonist
NF449 octasodium is a potent antagonist of the P2X1 receptor, exhibiting IC50 values of 0.28 nM, 0.69 nM, and 120 nM for recombinant P2X1, recombinant P2X1 with 5, and P2X2+3 receptors, respectively. It selectively targets the Gsα subunit of G proteins, effectively inhibiting GTP[γS] binding to Gsα-s and reducing adenylyl cyclase activity. NF449 octasodium is useful in research focused on the regulation of P2X1 receptor-mediated signaling pathways and β-adrenergic receptor interactions. -
Somatostatin
Tyr-Somatostatin-28 is a potent somatostatin analog featuring a tyrosine residue at the N-terminus. This modification enhances its stability and bioactivity, making it an important tool for studying somatostatin receptor interactions and signaling pathways. Tyr-Somatostatin-28 has applications in neurobiology and endocrinology research, particularly in the investigation of hormone regulation and therapeutic targets for diseases such as acromegaly and neuroendocrine tumors. -
Potassium Channel Blocker
Besipirdine hydrochloride is a potassium channel blocker that exerts both cholinergic and adrenergic effects. Its cholinergic activity is characterized by stimulation of phosphatidylinositol turnover and a reduction in potassium currents, while its adrenergic activity promotes norepinephrine release through the inhibition of presynaptic α2-adrenergic receptors and the blocking of norepinephrine reuptake. This compound is applicable in research related to Alzheimer's disease, providing insights into potential therapeutic pathways.
