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Catalog No.
Product Name
Application
Product Information
Citations
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Angiotensin Receptor Inhibitor
H-Val-Pro-Pro-OH TFA is an inhibitor of Angiotensin I converting enzyme (ACE), demonstrating an IC50 of 9 μM. This milk-derived proline peptide derivative is utilized in research applications focused on cardiovascular biology and hypertension. Its role in modulating the renin-angiotensin system makes it a valuable tool for studying the effects of ACE inhibition in various physiological and pathological contexts. -
CXCR Inhibitor
ALX 40-4C is a small peptide inhibitor targeting the chemokine receptor CXCR4. It effectively prevents the binding of SDF-1 to CXCR4 with a Ki of 1 μM, thereby inhibiting the replication of X4 strains of HIV-1. Additionally, ALX 40-4C Trifluoroacetate serves as an antagonist of the APJ receptor, exhibiting an IC50 value of 2.9 μM. This dual activity makes ALX 40-4C a valuable tool for research in HIV-1 studies and chemokine receptor signaling pathways. -
CXCR Receptor Inhibitor
SCH-900875 is a selective inhibitor of the CXCR3 receptor, known for its oral bioavailability and ability to penetrate the blood-brain barrier. By binding to CXCR3, it effectively prevents the interaction of ligands CXCL9, CXCL10, and CXCL11, thereby inhibiting downstream G protein and β-arrestin signaling pathways, which reduces inflammatory cell migration. This compound holds potential for investigating various autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis, as well as inflammatory conditions like psoriasis and inflammatory bowel disease. -
PDK Inhibitor, CB1/CB2 Agonist
Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor, demonstrating an IC50 value of 9.5 μM. It effectively lowers blood glucose levels in diabetic mouse models. Additionally, Leelamine acts as a weak agonist of cannabinoid receptors CB1 and CB2. Its biological activity includes a reduction in mitotic activity and prostate-specific antigen expression, as well as the induction of apoptosis in cancer cells, making it a valuable tool for cancer research and metabolic studies. -
Cannabinoid Receptor Inhibitor
2-Linoleoyl glycerol is a monoacylglycerol that serves as an antagonist and partial agonist at the cannabinoid receptor type 1 (CB1). It effectively modulates the activity of cannabinoids such as anandamide (AEA) and 2-arachidonoylglycerol (2-AG) by attenuating their effects without enhancing them. This compound has significant implications in cannabinoid research, particularly in studies focused on the endocannabinoid system and potential therapeutic targets for various conditions. Additionally, its potency can be influenced by the inhibition of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). -
CB1 Inhibitor
ANEB-001 is an orally active inhibitor of the cannabinoid receptor type 1 (CB1). This compound is primarily utilized in research focused on acute cannabinoid intoxication, providing insights into the physiological effects and potential therapeutic approaches related to CB1 modulation. Its selective inhibition of CB1 makes it a valuable tool for studies investigating cannabinoid-related pathways and their implications in various biological contexts. -
DAGLα Inhibitor
O-7460 is a selective inhibitor of diacylglycerol lipase alpha (DAGLα), exhibiting an IC50 value of 0.69 μM. This compound demonstrates selectivity against monoacylglycerol lipase (MAGL) and both human CB1 and CB2 cannabinoid receptors. O-7460 has been shown to effectively reduce elevated 2-arachidonoylglycerol (2-AG) levels associated with high-fat diet conditions, making it a valuable tool for studying endocannabinoid signaling and its implications in metabolic disorders. -
CB/FAAH Inhibitor
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is a potent inhibitor of the central cannabinoid receptor (CB1) and fatty acid amide hydrolase (FAAH), exhibiting similar inhibitory activities with IC50 values around 2 nM. It serves as a valuable tool for investigating cannabinoid signaling pathways and lipid metabolism in various biological contexts. Researchers utilize IDEFP to explore the therapeutic potential of modulating endocannabinoid systems in pain, inflammation, and neuroprotection studies. -
BChE Inhibitor/CB2R Agonist
hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation. -
CETP Inhibitor/CB1 Agonist
BI-5756 is a selective CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It promotes a significant increase in HDL-C levels while reducing LDL-C levels, thereby improving lipid profiles. Additionally, BI-5756 enhances the function of regulatory T cells and preserves T cell-mediated anti-tumor activity, exhibiting direct anti-proliferative effects on tumor cells. This compound also upregulates the expression of MHC I, MHC II, and CD80 on tumor cells and demonstrates protective effects in graft-versus-host disease. BI-5756 is applicable in research related to oncology, graft-versus-host disease, and metabolic disorders. -
CB1/2 Inhibitor
AM12814 is a potent and selective inhibitor of cannabinoid receptors CB1 and CB2, demonstrating Ki values of 0.7 nM and 3.4 nM, respectively. This compound effectively inhibits cAMP accumulation and promotes β-arrestin 2 recruitment, mimicking cannabimimetic effects. AM12814 is suitable for research applications related to neurological diseases, including studies on catalepsy. -
CB2R Agonist/FAAH Inhibitor
CB2R/FAAH modulator-1 is a potent full agonist of the cannabinoid type 2 receptor (CB2R), exhibiting a binding affinity with a Ki of 14.8 nM for CB2R and 241.3 nM for CB1R. This compound also serves as an inhibitor of fatty acid amide hydrolase (FAAH), demonstrating an IC50 of 4 μM. CB2R/FAAH modulator-1 is effective in modulating cytokine production by decreasing pro-inflammatory cytokines while enhancing anti-inflammatory cytokine levels, making it valuable for research in inflammation and pain modulation. -
Anandamide Transport Inhibitor
N-(3-Hydroxyphenyl)-arachidonoyl amide is an anandamide transport inhibitor, exhibiting an IC50 of 21.3 μM. This compound serves as a valuable tool in understanding endocannabinoid signaling and lipid metabolism. It can be utilized in research applications focusing on cannabinoid receptors and the modulation of neuronal activity. -
CB1 Inhibitor
CB1-IN-2 is a selective CB1 receptor inhibitor, characterized by an IC50 of 0.644 μM. This compound effectively penetrates the blood-brain barrier, making it suitable for studies exploring its potential central nervous system effects. CB1-IN-2 can be applied in research focused on cannabinoid receptor modulation and its implications in various neurological and psychological conditions. -
Adenosine Receptor Inhibitor
CVT-2759 is a potent inhibitor of the A1 adenosine receptor, exhibiting IC50 values of 0.18 μM and 9.5 μM to antagonize [3H]CPX binding in the absence and presence of 1 mM GTP, respectively. This compound is essential for assessing the modulation of AV nodal conduction, facilitating a reduction in ventricular rate without inducing AV block, bradycardia, atrial arrhythmias, or vasodilation. It serves as a valuable reagent for research on cardiovascular physiology and pharmacological modulation of adenosine receptor pathways. -
Adenosine Receptor Inhibitor
KF21213 is a selective adenosine A2A receptor inhibitor, demonstrating a high affinity with a Ki value of 3.0 nM. This compound is essential for research involving central nervous system (CNS) functions and disorders, providing valuable insights into adenosine receptor signaling pathways. Its precision in targeting A2A receptors makes it a suitable tool for studying their role in neuropharmacology and related therapeutic applications. -
Adenylate Cyclase Inhibitor
KUM 32 is a potent inhibitor of adenylate cyclase that functions by antagonizing epinephrine-induced platelet aggregation. By selectively binding to the alpha-2 adrenergic receptor on human platelets, KUM 32 modulates platelet activation and aggregation pathways. This compound is utilized in research focused on cardiovascular disease and hemostasis, providing insights into the mechanisms of platelet function. -
AR Inhibitor
Adenosine receptor inhibitor 1 is a highly selective antagonist of adenosine receptors, demonstrating Ki values of >1000 nM for A1AR, A2BAR, and A3AR, and 68.5 nM for A2AAR. This compound exhibits significant antinociceptive and anti-inflammatory properties, contributing to its potential as a peripheral analgesic. Research applications include the investigation of mechanisms underlying cancer and neurodegenerative diseases, making it a valuable tool for advancing scientific understanding in these areas. -
AR Inhibitor
Adenosine receptor inhibitor 2 (compound 14b) is a selective antagonist of adenosine receptors, primarily targeting A1 and A2A subtypes. This compound exhibits a higher affinity for A1AR, with a Ki value of 52.2 nM, compared to 167 nM for A2AAR. Its potent inhibitory effects make it valuable for research exploring adenosine signaling pathways, and its applications may extend to studies in cardiovascular disease, cancer, and neurobiology. -
Adenosine Receptors Inhibitor
8-Chloro caffeine is an adenosine receptor inhibitor that binds with a Ki of 30 µM. This compound is known to potentiate UV-induced chromosomal aberrations in Cl-I Chinese hamster embryonic lung cells, making it relevant for studies in genotoxicity. As a derivative of the methylxanthine alkaloid caffeine, 8-Chloro caffeine serves as a useful tool for investigating the role of adenosine receptors in cellular responses and stress mechanisms. -
A2AAR/hMAO-B Inhibitor
A2AAR/hMAO-B-IN-1 is a non-xanthine dual-target inhibitor that selectively inhibits the A2A adenosine receptor (A2AAR) with an IC50 of 34.9 nM, and human monoamine oxidase B (MAO-B) with a Ki of 39.5 nM. The compound effectively disrupts A2AAR-mediated cAMP accumulation and demonstrates competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 is suitable for research applications in neurodegenerative diseases, particularly in the study of Parkinson's disease (PD). -
hA3AR Inhibitor
PSB-10 hydrochloride is a highly selective antagonist of the human adenosine A3 receptor (hA3AR), demonstrating a Ki value of 0.44 nM. It exhibits over 800-fold selectivity for hA3AR compared to other adenosine receptor subtypes, including rA1, rA2A, hA1, hA2A, and hA2B, with respective Ki values of 805, 6040, 1700, 2700, and 30000 nM. This compound has been shown to induce thermal hyperalgesia in mouse models, making it valuable for exploring pain pathways and adenosine receptor signaling in research. -
Gαi Inhibitor
0990CL is a selective inhibitor of the heterotrimeric Gαi subunit, functioning through direct interaction with Gαi. This compound effectively inhibits α2 adrenergic receptor-mediated regulation of cyclic AMP (cAMP), making it a valuable tool for studying Gαi signaling pathways. It is particularly useful in research related to neurotransmission and cardiovascular physiology, aiding in the exploration of GPCR-mediated processes. -
β3-adrenergic Receptor Inhibitor
Vemtoberant is a selective β3-adrenergic receptor inhibitor with a human Ki of 8.2 nM, demonstrating a significant selectivity of 400- to 600-fold over the human β1- and β2-adrenergic receptors. This compound effectively attenuates β3-AR-mediated cardiac inhibition, making it a valuable tool for studying mechanisms underlying systolic heart failure. Researchers can utilize Vemtoberant to investigate therapeutic strategies aimed at modulating β3-adrenergic signaling in cardiac contexts. -
Adrenergic Receptor Inhibitor
Todralazine hydrochloride is a selective β2 adrenergic receptor inhibitor primarily used in the treatment of hypertension. Its mechanism involves blocking β2 adrenergic receptors, contributing to its effectiveness as an antihypertensive agent. In addition to its receptor inhibition, Todralazine hydrochloride exhibits antioxidant properties, providing potential benefits in research focused on oxidative stress and cardiovascular health. -
α1/β1-Adrenergic Receptor Inhibitor
Amosulalol is a dual inhibitor of the α1 and β1-adrenergic receptors, demonstrating significant antihypertensive activity. By selectively inhibiting the α1-adrenergic receptor, Amosulalol effectively reduces blood pressure, while its β1-adrenergic receptor blockade leads to decreased reflex-induced heart rate and plasma renin activity in spontaneously hypertensive rats. This compound is valuable for research applications focused on cardiovascular physiology and the pharmacological modulation of blood pressure. -
β-AR inhibitor
β-AR antagonist 2 functions as a selective antagonist of β-adrenergic receptors, exhibiting an IC50 value of 0.17 μM. This compound has demonstrated significant inhibitory effects on the growth of mouse A549 xenograft tumors and exhibits cardioprotective properties in a model of doxorubicin-induced heart failure in C57 mice. Its applications in cancer research and cardiovascular studies make it a valuable tool for investigating β-AR signaling pathways. -
Adrenergic Receptor Inhibitor
Napitane is an adrenergic receptor inhibitor that primarily targets α-adrenergic receptors, leading to enhanced catecholamine availability. This compound has demonstrated significant potential in antidepressant research, highlighting its efficacy in modulating neurochemical pathways associated with mood regulation. Napitane serves as a valuable tool for investigating mechanisms underlying depression and exploring novel therapeutic approaches for mood disorders. -
α1 Adrenergic Receptor Inhibitor
Conopeptide rho-TIA is a peptide originating from the venom of the predatory sea snail Conus tulipa, serving as a highly selective noncompetitive inhibitor of the human α1B-adrenergic receptor. It also acts as a competitive inhibitor for both the α1A- and α1D-adrenergic receptors. By selectively binding to these receptor subtypes, conopeptide rho-TIA offers valuable insights for the development of novel, subtype-selective α1-adrenergic receptor therapies. Its unique mechanism of action makes it a potent tool for cardiovascular and pharmacological research. -
Adrenergic Receptor Inhibitor
(+)-Amosulalol is an adrenergic receptor inhibitor that serves as an orally active dual blocker of α1 and β1-adrenergic receptors. This compound demonstrates significant antihypertensive activity by selectively inhibiting α1-adrenergic receptors, while also reducing reflex tachycardia and plasma renin activity in spontaneously hypertensive rats through β1-adrenergic receptor inhibition. As a valuable research tool, (+)-Amosulalol can be employed in studies related to cardiovascular physiology and pharmacology. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
Adrenergic Receptor Inhibitor
Moprolol is a beta-adrenergic receptor inhibitor that primarily targets beta-adrenergic receptors to modulate cardiovascular responses. This compound is useful in research related to essential hypertension studies, enabling investigations into its effects on blood pressure regulation and heart rate modulation. Its properties make it a valuable tool for exploring the role of adrenergic signaling in hypertensive conditions. -
Adrenergic Receptor Inhibitor
JNJ-7925476 hydrochloride is a triple monoamine uptake inhibitor that targets adrenergic receptors to modulate neurotransmitter availability. It demonstrates significant antidepressant activity, as evidenced by increased extracellular levels of serotonin, dopamine, and norepinephrine in the rat cerebral cortex. This compound is applicable in preclinical research to investigate the mechanisms underlying mood disorders and therapeutic interventions. Additionally, its rapid absorption and higher concentration in the brain support its potential for effective neurological studies. -
α2A/α2B AR Inhibitor
BRL-44408 is a selective antagonist of the α2A and α2B adrenergic receptors. It effectively inhibits the actions of norepinephrine and the agonist Clonidine on the release of [3H]norepinephrine and [3H]5-hydroxytryptamine in K+-stimulated conditions. With a higher affinity for α2A-adrenoceptors in human platelet membranes compared to other antagonists, BRL-44408 may play a significant role in modulating neurotransmitter release, making it a valuable tool for research in adrenergic signaling and related pharmacological studies. -
NET Inhibitor
XEN-2174 is a selective noradrenaline transporter (NET) inhibitor that functions through non-competitive inhibition of noradrenaline reuptake. By increasing the synaptic concentration of noradrenaline, it activates α2-adrenergic receptors at the spinal level, leading to pronounced analgesic effects. This compound demonstrates sustained analgesia in various models of neuropathic and postoperative pain in rats, making it a valuable tool for pain research applications. -
Adrenergic Receptor Inhibitor
(-)-Amosulalol is a selective inhibitor of α1/β1-adrenergic receptors, demonstrating dual action in pharmacological studies. It exhibits antihypertensive properties primarily through the blockade of α1-adrenergic receptors, effectively reducing peripheral vascular resistance. Additionally, (-)-Amosulalol decreases reflex tachycardia and plasma renin activity in models of hypertension, making it valuable for research in cardiovascular diseases and hypertension management. -
Adrenergic Receptor Inhibitor
IMTPPE is an adrenergic receptor inhibitor that selectively targets the androgen receptor (AR) in prostate cancer cells. It effectively inhibits AR transcriptional activity and reduces protein levels, leading to decreased proliferation of AR-positive prostate cancer cells, while showing no effect on AR-negative cells. Additionally, IMTPPE demonstrates significant anti-tumor activity against enzalutamide-resistant 22Rv1 xenograft tumors, making it a valuable tool for studying AR signaling pathways and developing therapeutic strategies for resistant prostate cancer. -
5-HT Receptor Inhibitor
Metrenperone is a selective inhibitor of the 5-HT2 receptor, exhibiting significant antagonist activity on α1 and α2 adrenergic receptors, as well as anti-H1 and anti-dopaminergic effects. It demonstrates notable biological activities, including the reduction of blood pressure, enhancement of bradycardia during peripheral ischemia, and inhibition of serotonin-induced platelet aggregation. Additionally, Metrenperone antagonizes serotonin-mediated vasoconstriction and is involved in promoting the repair of acutely damaged collagen tissue, making it valuable for various research applications in cardiovascular and vascular biology. -
Adrenergic Receptor Inhibitor
Bamosiran is a small interfering RNA that specifically targets the β-adrenergic receptor 2. This compound is recognized for its ability to significantly reduce intraocular pressure, making it valuable in the study of ocular conditions. Its role as an adrenergic receptor inhibitor aids in investigating therapeutic strategies for glaucoma and other eye disorders. -
Platelet Aggregation Inhibitor
D-RGDW is a synthetic peptide containing the Arg-Gly-Asp (RGD) sequence, which targets the αIIbβ3 integrin. It effectively inhibits platelet aggregation, making it a valuable tool for research into thrombosis and hemostasis. D-RGDW can be utilized in various biochemical studies focused on vascular biology and the mechanisms of platelet activation. -
Glycoprotein IIb-IIIa/Platelet Aggregation Inhibitor
Variabilin is a potent antagonist of glycoprotein IIb-IIIa, functioning primarily as a platelet aggregation inhibitor. Isolated from the hard tick Dermacentor variabilis, Variabilin effectively inhibits platelet aggregation induced by various agonists, including ADP, collagen, and thrombin receptor peptide SFLLRNP. Additionally, it hinders platelet adhesion to immobilized fibrinogen (Fg) and blocks the binding of purified human GPIIb-IIIa to immobilized Fg. This compound is valuable for research applications in hematology and thrombosis. -
Dopamine β-hydroxylase Inhibitor
A32390A is a potent inhibitor of dopamine β-hydroxylase, functioning primarily to decrease norepinephrine synthesis. This reduction can lead to lowered blood pressure, making A32390A valuable in studies related to hypertension, particularly in models such as DOCA hypertensive rats. Additionally, the compound's properties as a copper chelator allow for exploration in the context of bacterial infections and metabolic disorders, providing versatile applications in chemical research. -
AChE/Dopamine 2 Inhibitor
Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies. -
CCR5/CXCR3 Inhibitor
CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial. -
Cholecystokinin Receptor Inhibitor
Gastrazole free acid is a cholecystokinin receptor antagonist that demonstrates potential in inhibiting pancreatic cancer growth. By targeting gastrin receptors, this compound plays a crucial role in the modulation of gastric functions and may aid in the investigation of therapeutic strategies for gastrointestinal malignancies. Its utility in research provides insights into receptor-mediated pathways and cancer biology. -
CCK B Inhibitor
PD-135666 is a potent dipeptide inhibitor of cholecystokinin B (CCK B) receptors, demonstrating an IC50 of 0.1 nM in mouse cerebral cortex. Unlike its enantiomer, PD-140548, which selectively targets CCK A receptors in rat pancreas, PD-135666 primarily interacts with CCK B receptors. This compound has been shown to exhibit anxiolytic effects in various animal models, making it a valuable tool for studying anxiety-related disorders and CCK receptor biology. -
Cholecystokinin Receptor Inhibitor
CCK-A receptor inhibitor 1 is a selective inhibitor of the cholecystokinin A (CCK-A) receptor, exhibiting a binding IC50 of 340 nM. By modulating CCK-A receptor activity, this compound plays a crucial role in studying gastrointestinal physiology and related disorders. Its inhibitory properties make it useful for research applications focused on appetite regulation and the gastrointestinal system. -
ELR+CXCL-CXCR1/2 Inhibitor
CXCL-CXCR1/2-IN-1 is an orally active inhibitor of the ELR+CXCL-CXCR1/2 signaling pathway, exhibiting an EC50 of 42.7 nM for the CXCR2 receptor. This compound demonstrates significant anticancer and antiangiogenic properties, making it a valuable tool for research into tumor progression and vascularization. Its ability to target these pathways underscores its potential application in cancer biology and therapeutic development. -
CXCR4 Inhibitor
CXCR4-IN-3 is a potent inhibitor of the CXCR4 receptor, demonstrating an IC50 of 3.2 nM. It exhibits significant antichemotactic effects, with an inhibition rate of 79.19±2.33%. This compound also displays anti-inflammatory properties, making it a valuable tool for research into inflammatory bowel disease (IBD) and related inflammatory conditions. -
CXCR4 Inhibitor
Peptide R is a cyclic peptide that functions as a specific antagonist of the CXCR4 receptor. It demonstrates significant efficacy in remodeling tumor stroma, making it a valuable tool for tumor research. Its ability to modulate the tumor microenvironment highlights its potential applications in cancer therapy and investigation into tumor progression mechanisms.
