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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
Platelet Aggregation Inhibitor
U-51605 is a platelet aggregation inhibitor that targets thromboxane synthesis. It also functions as a prostaglandin I2 synthase inhibitor and has been shown to block retinal vasodilation responses induced by nitric oxide donors like NOR3. This reagent is valuable for research applications focusing on cardiovascular health and vascular biology. -
RGS Protein Inhibitor
CCG 203769 is a selective inhibitor of the regulator of G protein signaling (RGS4), effectively disrupting the RGS4-Gαo protein-protein interaction with an IC50 of 17 nM. This compound is instrumental for research applications focused on G protein-coupled signaling pathways and the modulation of G protein activity. CCG 203769 may be utilized in studies exploring the role of RGS proteins in various physiological processes and disease states. -
RGS14 Inhibitor
Z55660043 is a selective inhibitor of Regulator of G protein Signaling-14 (RGS14) with an IC50 of 2.3 μM. This compound acts by non-covalently inhibiting the GTPase-accelerating protein (GAP) activity of RGS14, demonstrating a favorable safety profile without significant cytotoxic effects. Z55660043 is suitable for research focused on central nervous system and metabolic disorders, contributing to the understanding of RGS14's role in these biological processes. -
RGS4 Inhibitor
CCG-2046 is a selective inhibitor of the regulator of G-protein signaling 4 (RGS4), demonstrating an IC50 value of 4.3 μM for inhibiting the RGS4-Gαo interaction. This compound modulates G-protein signaling pathways, making it a valuable tool for studying their role in various physiological processes. CCG-2046 is suitable for research applications focused on neurobiology, cardiac function, and potential therapeutic interventions for related disorders. -
RGS Protein Inhibitor
CCG-4986 is a selective RGS protein inhibitor that covalently modifies the Cys-132 residue of RGS4, thereby inhibiting its activity. This compound is valuable for studying the implications of altered G protein-coupled receptor (GPCR) signaling in various pathological conditions, including Parkinson's disease and opioid addiction. CCG-4986 is a useful tool for researchers investigating the role of RGS proteins in cellular signaling pathways. -
MMP Inhibitor
Sucrose octasulfate is a matrix metalloproteinase (MMP) inhibitor that modulates cellular activities by regulating the extracellular matrix. It promotes the release of somatostatin-like immunoreactivity from gastric D cells, facilitating ulcer healing through increased endogenous somatostatin levels. This compound has demonstrated efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers, making it pertinent for research in chronic wound healing and gastrointestinal disorders. Additionally, sucrose octasulfate serves as a valuable pharmaceutical excipient in various therapeutic applications. -
MMP Inhibitor
Sucrose octasulfate sodium is a potent matrix metalloproteinase (MMP) inhibitor that enhances the release of somatostatin-like immunoreactivity (SLI) from gastric D cells. This compound promotes ulcer healing by increasing endogenous gastric somatostatin levels. Sucrose octasulfate sodium is utilized in research related to chronic wound healing and has shown significant efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers. Additionally, it serves as a useful pharmaceutical excipient in various applications. -
Somatostatin Receptor Inhibitor
SRA880 free base is a somatostatin receptor inhibitor, specifically targeting the somatostatin-1 autoreceptor. This compound exhibits antidepressant-modulating effects and has been shown to enhance the efficacy of imipramine, resulting in antidepressant-like outcomes. Additionally, SRA880 influences brain-derived neurotrophic factor (BDNF) mRNA expression and modulates the phosphorylation of associated proteins, making it a valuable tool in neurobiological research focusing on mood disorders and related pathways. -
Somatostatin Receptor Inhibitor
Des-threoninol-octreotide is a potent somatostatin receptor inhibitor, primarily targeting the mSSTR2b, rSSTR5, and hSSTR5 receptor subtypes. This compound demonstrates high inhibitory activity with IC50 values of 13.62 nM, 10.63 nM, and 10.95 nM, respectively. It is valuable for research applications exploring neuroendocrine regulation, peptide hormone signaling, and potential therapeutic interventions involving somatostatin pathways. -
platelet aggregation inhibitor
Trifenagrel is an orally active platelet aggregation inhibitor that targets the pathways induced by arachidonic acid and collagen. It demonstrates significant biological activity, with ED50 values of 1.4 mg/kg and 9.4 mg/kg for the inhibition of AA- and collagen-induced platelet aggregation in guinea pigs, respectively. This compound serves as a valuable tool in cardiovascular research and the study of thrombotic disorders. -
Platelet-activating Factor Receptor (PAFR) Inhibitor
TSI-01 is a selective inhibitor of the Platelet-activating Factor Receptor (PAFR), targeting lysophosphatidylcholine acyltransferase (LPCAT)2. This compound exhibits a potent inhibitory effect with an IC50 of 0.47 μM for human LPCAT2, significantly more effective than its activity on LPCAT1 (IC50 = 3.02 μM). TSI-01 effectively suppresses PAF biosynthesis in mouse peritoneal macrophages when stimulated with a calcium ionophore at a concentration of 60 μM. This makes TSI-01 a valuable tool for investigating inflammatory processes and related conditions in research applications. -
Platelet Aggregation Inhibitor
2-Acetylbenzoic acid is a derivative of benzoic acid that functions as a weak inhibitor of platelet aggregation. It specifically inhibits adenosine 5'-diphosphate (ADP)-induced platelet aggregation, making it valuable for research in cardiovascular biology and thrombotic disorders. This compound can be utilized to study the role of platelet activation in various disease models and therapeutic interventions. -
PAFR Inhibitor
Cryptomeridiol is an inhibitor of the platelet-activating factor (PAF) receptor. It demonstrates significant melanogenesis inhibitory activity in α-MSH-stimulated B16 melanoma cells, making it a valuable tool for research into pigmentation processes and potential therapeutic applications in melanoma. Its mechanisms may contribute to a better understanding of PAF signaling in various biological contexts. -
Platelet Aggregation Inhibitor
Preschisanartanin O is a potent platelet aggregation inhibitor derived from Schisandra lancifolia. It effectively inhibits platelet aggregation induced by platelet-activating factor (PAF), highlighting its potential role in cardiovascular research. This compound is valuable for studies investigating thrombus formation and related pathological conditions, providing insight into therapeutic strategies for managing platelet-related disorders. -
Platelet Aggregation-related Pathway Inhibitor
MKC-963 is a potent, orally active inhibitor targeting platelet aggregation-related pathways. This compound exhibits significant antithrombotic activity by disrupting platelet aggregation mechanisms. Additionally, MKC-963 induces autoinduction of CYP3A4, leading to enhanced metabolism in vivo. It is a valuable tool for research into platelet aggregation-related diseases, such as thrombosis. -
Platelet Aggregation Inhibitor
(R,R)-MK 287 is a potent platelet aggregation inhibitor targeting platelet-activating factor (PAF) pathways. It demonstrates strong inhibition of PAF binding to human platelets, polymorphonuclear leukocytes, and lung membranes, with Ki values of 6.1, 3.2, and 5.49 nM, respectively. (R,R)-MK 287 effectively prevents PAF-induced platelet aggregation and elastase release from PMNs, with ED50 values of 56 nM and 4.4 nM, respectively. Additionally, it reduces PAF-induced lethality in murine models and bronchospasm in guinea pigs, showcasing its potential applications in inflammatory and cardiovascular research. -
Arachidonic Acid Metabolism/Platelet Aggregation Inhibitor
Rhazimine is an indole alkaloid that serves as a dual inhibitor of arachidonic acid metabolism and platelet aggregation induced by platelet activating factor. This compound demonstrates significant biological activity by modulating inflammatory pathways and inhibiting platelet aggregation, making it valuable for research in cardiovascular diseases and related pharmacological studies. Rhazimine's mechanism may provide insights into the development of therapeutic strategies targeting vascular inflammation and thrombotic conditions. -
Platelet-activating Factor Receptor (PAFR) Inhibitor
Dersalazine is a selective inhibitor of the platelet-activating factor receptor (PAFR), demonstrating significant intestinal anti-inflammatory properties. This compound shows potential efficacy in the treatment of ulcerative colitis, making it a valuable tool for research into inflammatory bowel diseases. Its ability to modulate PAFR-mediated signaling pathways makes Dersalazine a pertinent candidate for exploring therapeutic strategies targeting inflammation and related gastrointestinal disorders. -
PAF Inhibitor
CV 3988 is a selective inhibitor of platelet-activating factor (PAF), a lipid mediator involved in various inflammatory processes. By blocking PAF activity, CV 3988 demonstrates potential in mitigating inflammation-related pathways and may be valuable in studying conditions influenced by PAF. This compound is suitable for research applications in inflammation, cardiovascular diseases, and related areas of biochemical investigation. -
PAFR Inhibitor
Piperulin A is a selective inhibitor of the platelet-activating factor receptor (PAFR). It effectively disrupts the specific binding of PAFR on isolated rabbit platelet plasma membranes, demonstrating an IC50 value of 7.3 μM. This compound is valuable for research applications focused on understanding PAFR-related signaling pathways and their implications in various physiological and pathological processes. -
PAF Inhibitor
Pinusolidic acid is an inhibitor of platelet-activating factor (PAF), demonstrating an IC50 value of 23 μM. This compound is primarily utilized in research to study the roles of PAF in various biological processes and diseases, including inflammation and thrombosis. Its inhibitory properties make it a valuable tool for investigating PAF-related pathways and potential therapeutic applications. -
Platelet Aggregation Inhibitor
Aggreceride A is a potent platelet aggregation inhibitor that targets multiple pathways involved in thrombosis. It exhibits significant inhibitory activity against platelet aggregation induced by Adenosine 5'-diphosphate (ADP), arachidonic acid, and platelet-activating factor (PAF), making it valuable for cardiovascular research. However, it demonstrates reduced efficacy against collagen-induced aggregation. This compound is suitable for studying mechanisms of platelet function and the effects of aggregation inhibitors in various therapeutic contexts. -
PAF Inhibitor
BN 52111 is a potent platelet-activating factor (PAF) receptor antagonist. It inhibits PAF signaling, which plays a crucial role in various physiological processes, including inflammation and thrombosis. BN 52111 is primarily utilized in research applications to investigate the role of PAF in disease models and to explore potential therapeutic interventions. -
Platelet Aggregation Inhibitor
Aggreceride B is a potent platelet aggregation inhibitor targeting pathways involved in thrombus formation. It effectively inhibits platelet aggregation induced by Adenosine 5'-diphosphate (ADP), arachidonic acid, and platelet activating factor (PAF), while demonstrating reduced activity against collagen-induced aggregation. This compound is valuable in studies focused on thromboembolic diseases and platelet function analysis. -
Platelet Aggregation Inhibitor
Aggreceride C is a potent platelet aggregation inhibitor targeting multiple pathways involved in platelet activation. It effectively inhibits aggregation induced by Adenosine 5'-diphosphate (ADP), arachidonic acid, and platelet activating factor (PAF) while demonstrating reduced activity against collagen-induced aggregation. This compound is valuable for research applications focused on thrombosis and vascular biology. -
PGDS Inhibitor
2-Benzoylthiophene is a selective inhibitor of human hematopoietic prostaglandin D2 synthase (H-PGDS), exhibiting an IC50 value of 11.4 μM. This compound is valuable for investigating the role of prostaglandin D2 in inflammatory diseases and related research applications. Its inhibitory action on H-PGDS provides a useful tool for exploring therapeutic strategies targeting inflammatory pathways. -
Prostaglandin Receptor Inhibitor
p-Hydroxycinnamic acid is a prostaglandin receptor inhibitor that functions as a dietary phenolic compound. It demonstrates significant biological activity by inhibiting platelet activity, with IC50 values of 371 μM for thromboxane B2 production and 126 μM for lipopolysaccharide-induced prostaglandin E2 generation. This compound is often utilized in research related to inflammation, cardiovascular diseases, and platelet function studies. -
Dual Thromboxane Synthase Inhibitor and Receptor Antagonist
Ridogrel is a dual thromboxane A2 synthase inhibitor and receptor antagonist. This compound exhibits potent antiplatelet activity, making it useful in research focused on cardiovascular diseases and thrombotic disorders. Additionally, Ridogrel displays anti-inflammatory properties, providing a valuable tool for studying inflammation-related pathways in various biological contexts. -
Prostaglandin Receptor Inhibitor
Ascorbyl tetra-2-hexyldecanoate is a lipophilic derivative of L-ascorbic acid that functions as a prostaglandin receptor inhibitor. This compound demonstrates protective effects on HaCaT keratinocytes, maintaining cell viability against UVB and oxidative stress while decreasing the production of inflammatory mediators IL-1α and prostaglandin E2 (PGE2). In vivo studies show that topical application enhances epidermal thickness, increases stratum corneum hydration, and improves skin texture, highlighting its potential for formulating skin whitening agents in cosmetic applications. -
TxA2 Synthase/Receptor Inhibitor
Picotamide is a dual inhibitor of thromboxane A2 (TxA2) synthase and its receptor, exhibiting significant antiplatelet activity. This compound is effective in reducing microalbuminuria and inhibiting the growth of carotid plaques, particularly in diabetic models. Picotamide is a valuable tool for investigating both acute and chronic cardiovascular diseases, aiding research into therapeutic interventions for these conditions. -
EP2 Inhibitor
TG8-260 is a selective EP2 antagonist designed to mitigate the effects of inflammation in both central nervous system and peripheral diseases. This compound effectively reduces neuroinflammation and gliosis in the hippocampus of rats following pilocarpine-induced status epilepticus. With a plasma half-life of 2.14 hours and an oral bioavailability of 77.3%, TG8-260 also demonstrates potent inhibition of CYP450. Its ability to inhibit EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia makes it a valuable tool for investigating anti-inflammatory pathways in various animal models of peripheral inflammatory conditions. -
Thromboxane Synthase Inhibitor
Dazoxiben hydrochloride is a potent thromboxane synthase inhibitor that exhibits oral bioavailability. It effectively suppresses thromboxane production, a key factor in platelet aggregation and vascular smooth muscle contraction. This compound is utilized in research focused on cardiovascular diseases and conditions related to thrombosis and inflammation. -
Thromboxane Synthase Inhibitor
Furegrelate sodium is a selective thromboxane synthase inhibitor, demonstrating significant inhibition of human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. This compound is being investigated for its potential as an antiplatelet agent, making it a valuable tool for research in cardiovascular diseases and platelet function studies. Its oral availability enhances its applicability in preclinical and clinical settings, contributing to advancements in antiplatelet therapy development. -
PGHS1 Inhibitor
Satigrel is a selective inhibitor of prostaglandin H synthase 1 (PGHS1), primarily targeting platelet aggregation. It effectively inhibits collagen- and arachidonic acid-induced platelet aggregation by blocking thromboxane A2 synthesis. With an IC50 of 0.081 μM for PGHS1 and 5.9 μM for PGHS2, Satigrel also demonstrates inhibitory activity against Type III, Type V, and Type II phosphodiesterases, with IC50 values of 15.7 μM, 39.8 μM, and 62.4 μM, respectively. This compound is valuable for research into platelet function and thrombotic diseases. -
Prostaglandin E2 Inhibitor
Thielavin A is a selective inhibitor of prostaglandin E2 biosynthesis, derived from the fungus Thielavia terricola. It specifically targets the conversion of arachidonic acid to prostaglandin H2, thereby disrupting the prostaglandin synthesis pathway. Despite its inhibition of prostaglandin E2, Thielavin A exhibits minimal anti-inflammatory effects upon intravenous or oral administration, making it a valuable tool for studying prostaglandin-related biological processes and inflammation research. -
sPLA2 Inhibitor
CAY10590 is a potent inhibitor of secreted phospholipase A2 (sPLA2), serving as a valuable tool for investigating the role of sPLA2 in chronic inflammatory kidney diseases. Its mechanism of action enables the modulation of inflammatory pathways, which is critical for understanding disease mechanisms and potential therapeutic interventions. This compound is applicable in preclinical research aimed at elucidating the involvement of sPLA2 in renal pathologies. -
PTGR2 Inhibitor
HHS-0701 is a potent inhibitor of prostaglandin reductase 2 (PTGR2), functioning as a sulfur-triazole exchange (SuTEx) ligand. This compound effectively blocks the metabolism of the lipid substrate 15-Keto-PGE2 by PTGR2, playing a crucial role in modulating prostaglandin levels. HHS-0701 is valuable for research applications involving inflammation and lipid metabolism, providing insights into the enzymatic regulation of prostaglandins. -
Prostaglandin Inhibitor
Ibuprofen guaiacol ester is a potent inhibitor of prostaglandin synthesis, demonstrating significant oral bioactivity. It is primarily utilized in research related to inflammation, edema, and fever modulation. This compound provides valuable insights into the mechanistic pathways of pain and inflammatory responses, making it a useful tool in pharmacological studies. -
Platelet Aggregation Inhibitor
17-Phenyl-18,19,20-trinor-PGD2 is a potent inhibitor of platelet aggregation that primarily targets adenosine diphosphate (ADP) signaling pathways. It demonstrates an IC50 of 8.4 μM, significantly outperforming prostaglandin D2 (PGD2), which has an IC50 of 18.6 nM. Additionally, 17-Phenyl-18,19,20-trinor-PGD2 serves as a weak agonist for cyclic AMP accumulation, making it a valuable tool for research in cardiovascular and hemostatic studies. -
Prostaglandin Metabolism Inhibitor
L11204 is a potent inhibitor of prostaglandin metabolism. It effectively inhibits PMS-induced superovulation, resulting in a reduced number of recoverable ova in the oviducts of hamsters. Additionally, L11204 demonstrates the capability to inhibit chorionic gonadotrophin-induced ovarian hypertrophy and steroidogenesis in rats. This compound shows promise for studying reproductive system disorders and related biological processes.
