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Catalog No.
Product Name
Application
Product Information
Citations
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CXCR4 Inhibitor
CXCR4-IN-1 is a selective inhibitor of the CXCR4 chemokine receptor, with an IC50 of 20 nM. This compound exhibits potential biological activity in modulating cellular responses associated with cancer progression, HIV infection, diabetic retinopathy, and inflammatory conditions. CXCR4-IN-1 is suitable for use in research applications focused on these disease processes, providing valuable insights into therapeutic targeting of the CXCR4 signaling pathway. -
CXCR2 Inhibitor
NVP CXCR2 20 is a selective inhibitor of the CXCR2 receptor, primarily involved in modulating pain pathways. It exhibits significant analgesic and antinociceptive effects, effectively reducing mechanical and thermal hypersensitivity in rat models of chronic constriction injury (CCI). Additionally, NVP CXCR2 20 diminishes CXCL3-induced hypersensitivity in naive mice and lowers CXCL3 protein levels in the spinal cord and dorsal root ganglia of CCI-exposed rats. This compound is valuable for research into neuropathic pain and chronic obstructive pulmonary disease (COPD). -
CXCL12 Inhibitor
4-Amino-D-phenylalanine is a potent CXCL12 inhibitor that targets the CXCR4 receptor. With an IC50 value of 0.1 μM, it effectively inhibits the binding of CXCL12 to its receptor. This compound is valuable for research applications focused on understanding CXCR4-related pathways and their implications in cancer, inflammation, and various other diseases. -
CXCR4 Inhibitor
vMIP-II (1-21) is a selective inhibitor of the chemokine receptor CXCR4. By competing with 125I-SDF-1R for binding sites, vMIP-II (1-21) effectively disrupts CXCR4 signaling, with an IC50 value of 190 nM. This compound is useful for research applications involving the study of chemokine receptors and their role in various biological processes, such as immune response and cancer metastasis. -
CXCR4 Inhibitor
TN14003 is a selective inhibitor of the CXCR4 receptor. It demonstrates significant antitumor activity by disrupting CXCR4-mediated signaling pathways, which are implicated in cancer cell survival, proliferation, and metastasis. This compound is primarily utilized in research focused on cancer treatment and understanding the role of the CXCR4 chemokine receptor in tumor progression. -
Phospholipase D Inhibitor
Halopemide is a potent inhibitor of phospholipase D (PLD), exhibiting IC50 values of 220 nM for human PLD1 and 310 nM for PLD2. In addition to its enzymatic inhibition, Halopemide functions as a dopamine receptor antagonist and exhibits psychotropic properties. This reagent is valuable for research applications exploring PLD-mediated signaling pathways and dopamine receptor interactions in various biological contexts. -
Dopamine Receptor Inhibitor
Clopenthixol is a thiaquinoline compound that acts as an antagonist of D1 and D2 dopamine receptors. It exhibits inhibitory effects comparable to those of phenothiazine antipsychotics, making it valuable in the treatment of schizophrenia and other mental disorders. This compound is primarily utilized in research related to psychiatric conditions and the exploration of dopamine regulation in the central nervous system. -
SR-2A/D2DR Inhibitor
Octoclothepin maleate salt is a dual inhibitor of the SR-2A and D2 dopamine receptors. This compound exhibits significant central depressant activity, demonstrated in various observational and instrumental studies using rodent models. Its properties make it a valuable tool in neuropharmacological research, particularly in the study of neuroleptic effects and dopaminergic signaling pathways. -
CXCR Inhibitor
AMD-3329 is a selective CXCR4 inhibitor that targets the chemokine receptor involved in HIV-1 and HIV-2 entry into host cells. By obstructing CXCR4, AMD-3329 effectively inhibits viral replication, making it a valuable tool in HIV research. This compound is suitable for studies focused on developing therapeutic strategies against X4-tropic HIV strains and understanding the mechanisms of viral entry and infection. -
HIV Inhibitor
KRH-3955 is a potent CXCR4 antagonist that demonstrates significant anti-HIV-1 activity, particularly against X4 strains. It effectively inhibits the replication of various X4 HIV-1 clinical isolates and is active against recombinant strains with resistance mutations in reverse transcriptase, protease, and tyrosinase. KRH-3955 disrupts the binding of SDF-1alpha to CXCR4, thereby interfering with calcium signaling through this receptor, along with inhibiting antibody binding to CXCR4. With an oral bioavailability of 25.6% in rats, KRH-3955 has shown efficacy in vivo, making it a valuable tool for HIV research. -
DAGL-α/DAGL-β Inhibitor
LEI105 is a selective and reversible dual inhibitor of diacylglycerol lipase (DAGL)-α and DAGL-β. This compound effectively decreases levels of 2-arachidonoylglycerol in Neuro2A cells, demonstrating its potential to modulate endocannabinoid signaling. Research applications include investigations into the mechanisms underlying obesity, metabolic disorders, and neuroinflammation, as well as studies of cannabinoid receptor-mediated synaptic plasticity in mouse hippocampal slices. -
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. -
Prostaglandin Receptor Inhibitor
1,2,3-Trilinoelaidoyl glycerol acts as a prostaglandin receptor inhibitor, influencing the biosynthesis of prostaglandins and modulating platelet function. This compound also demonstrates significant effects on the fatty acid composition within rat organs, depending on the dosage administered. It serves as a valuable tool for examining dietary impacts on lipid metabolism and associated physiological parameters in preclinical research involving rodent models. -
Thromboxane Synthase Inhibitor
Furegrelate is a selective thromboxane synthase inhibitor that acts primarily by blocking the synthesis of thromboxane A2 (TxA2) in human platelets, exhibiting an IC50 of 15 nM. Its potent inhibitory action makes Furegrelate a valuable candidate for research applications focused on antiplatelet therapies. This compound is under investigation for its potential to mitigate thrombotic events associated with cardiovascular diseases. -
Thromboxane Synthetase Inhibitor
UK 34787 is a selective thromboxane synthetase inhibitor that exhibits minimal activity against cyclooxygenase and prostacyclin synthetase. This compound is utilized in research to study thromboxane's role in cardiovascular function and various pathophysiological conditions. Its specificity makes it a valuable tool in investigating the therapeutic potential of thromboxane modulation in disease models. -
Thromboxane Synthase Inhibitor
Wy 27569 is a thromboxane synthase inhibitor that modulates prostaglandin balance by decreasing pro-thrombotic thromboxane A2 (TXA2) and increasing anti-thrombotic prostacyclin (PGI2). This compound is known for its vascular selectivity and ability to effectively lower blood pressure. Wy 27569 is utilized in research on cardiovascular diseases, including hypertension and angina, making it valuable for understanding thrombotic processes and vascular health. -
Thromboxane A2 Synthetase Inhibitor
Nafagrel hydrochloride is a potent thromboxane A2 synthetase inhibitor. This compound effectively prevents thrombus formation, demonstrated in a rat model of acute arterial thrombosis. It is valuable for research applications related to cardiovascular disease, thrombosis, and related therapeutic interventions. -
Thromboxane Synthetase Inhibitor
Dazoxiben is an effective thromboxane synthetase inhibitor that functions to reduce thromboxane production, thereby influencing platelet aggregation and vasoconstriction. This compound is particularly relevant in the investigation of vascular conditions, such as Raynaud's syndrome, where thromboxane overproduction may play a critical role. Its oral bioavailability makes it suitable for in vivo studies on thromboxane-related pathologies. -
PGHS-2 Inhibitor
15(S)-HpEPE is a lipoxygenase-derived hydrolysis product of polyunsaturated fatty acids (PUFAs), serving as a potential inhibitor of prostaglandin H synthase 2 (PGHS-2). This compound has been shown to downregulate PGHS-2 expression, making it a valuable tool for research focused on inflammatory pathways and associated diseases. Its biological activity is of interest in studies examining the modulation of prostaglandin synthesis and the regulation of inflammatory responses. -
PTGR2 Inhibitor
RJG-2036 is a potent covalent inhibitor of human prostaglandin reductase 2 (PTGR2) with an IC50 value of 100 nM. This compound effectively inhibits NADPH-dependent reduction, leading to a significant decrease in the secretion of proinflammatory cytokines such as TNF-α and various eicosanoids in LPS-stimulated THP-1 macrophages. RJG-2036 serves as a valuable tool for investigating the molecular mechanisms underlying inflammatory diseases.
