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Catalog No.
Product Name
Application
Product Information
Citations
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Histamine Inhibitor
Elbanizine is a potent histamine inhibitor that effectively suppresses histamine and bradykinin release from rat mast cells, demonstrating an IC50 of 0.26 μM. This compound has been shown to inhibit IgE-mediated passive cutaneous anaphylaxis (PCA) reactions. Additionally, Elbanizine exhibits significant antiallergic and antiasthmatic properties in guinea pig models, making it a valuable tool for research in allergy and asthma mechanisms. -
Dopamine Receptor Inhibitor
BL-1020 mesylate is a dopamine receptor inhibitor with high affinity for D2L, D2S, and 5-HT2A receptors, exhibiting Ki values of 0.066, 0.062, and 0.21 nM, respectively. This compound functions as an antipsychotic agent and also acts as an agonist at the GABAA receptor, enhancing GABA release with a Ki of 3.74 μM. Furthermore, BL-1020 mesylate interacts effectively with histamine receptors (Ki of 0.47 nM) and demonstrates the ability to diminish amphetamine-induced hyperactivity while minimizing catalepsy and sedation. It penetrates the blood-brain barrier, making it suitable for neurological research applications. -
Histamine Receptor Inhibitor
D18024 is a potent histamine receptor inhibitor that demonstrates antiallergic and antihistaminic properties. This compound exhibits significant activity in modulating histamine-mediated processes, making it useful for research focused on allergy and inflammation pathways. D18024 can be employed in studies investigating the role of histamine receptors in various biological systems, contributing to the understanding of allergic responses and potential therapeutic interventions. -
Histamine Receptor Inhibitor
CI-949 is a potent histamine receptor inhibitor known for its ability to suppress the release of key allergic mediators. It demonstrates inhibition of histamine, leukotriene C4/D4, and thromboxane B2 with IC50 values of 11.4 μM, 0.5 μM, and 0.1 μM, respectively. This compound is useful for studies focused on allergic reactions and inflammation, providing insights into therapeutic strategies for allergic conditions. -
Histamine Receptor Inhibitor
KP136 is a potent histamine receptor inhibitor that exhibits antiallergic properties. It effectively blocks histamine release with an IC50 of 76.1 μg/mL and degranulation at 63 μg/mL. This compound is valuable for research applications focusing on allergic responses and related inflammation processes. -
CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone. -
noradrenalin re-uptake inhibitor
Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor. -
dopamine beta-hydroxylase inhibitor
Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. -
α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
DDP-4 inhibitor
Sitagliptin phosphate is an anti-diabetic (antihyperglycemic) drug of the dipeptidyl peptidase-4 (DPP-4) class. Inhibition of the enzyme DPP-4 is thought to increase Glucagon-like peptide-1 (GLP-1) which inhibits glucagon release , stimulates the insulin release and lowers blood glucose. -
Serotonin reuptake inhibitor
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%). -
triple reuptake inhibitor
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively. -
SSR inhibitor / 5-HT1A receptor partial agonist
Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. -
DPP4 inhibitor
Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1). -
dopamine reuptake inhibitor
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). -
LTC4 inhibitor
Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2). -
serotonin reuptake inhibitor/5-HT2A receptor antagonist
Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1. -
bovine tubulin oxidation inhibitor
Takeda103A is a potent GRK2-dependent bovine tubulin oxidation inhibitor. -
Pigmentation inhibitor
N,N′-Diferuloylputrescine acts as a pigment inhibitor, showing a 57% reduction in pigmentation. It also considerably diminishes the protein expression of MITF and displays potent antioxidant properties as a radical scavenger against reactive oxygen species.
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prostaglandin synthase inhibitor
Pizuglanstat is a hematopoietic prostaglandin synthase inhibitor. -
norepinephrine reuptake inhibitor
(R)-Viloxazine Hydrochloride is the R-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
norepinephrine reuptake inhibitor
(S)-Viloxazine Hydrochloride is the S-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
Prostaglandin E2 Inhibitor
Thielavin B is an inhibitor of prostaglandin biosynthesis, specifically targeting the synthesis of prostaglandin E2 from endoperoxide precursors. This compound demonstrates significant anti-inflammatory activity, as evidenced by its efficacy in reducing carrageenan-induced edema in rat models following intravenous administration. Thielavin B is valuable for research focused on inflammation and pain pathways. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
L-glutamate Uptake Inhibitor
Evans Blue is a potent inhibitor of L-glutamate uptake through the membrane-bound excitatory amino acid transporter (EAAT). This compound effectively inhibits L-glutamate and kainate receptor-mediated currents, making it valuable for research into neurophysiological processes. Additionally, due to its strong affinity for serum albumin, Evans Blue serves as a high molecular weight protein tracer and is widely used to investigate blood-brain barrier (BBB) permeability. -
Endothelin Receptor Inhibitor
Carperitide is a synthetic analogue of Atrial Natriuretic Peptide (ANP) that acts as an endothelin receptor inhibitor. This 28-amino acid peptide significantly reduces endothelin-1 secretion in a dose-dependent manner, thereby promoting vasodilation and natriuresis. It is primarily used in research applications related to cardiovascular physiology, providing insights into heart failure mechanisms and the regulation of blood pressure. -
Platelet Aggregation Inhibitor
Epoprostenol sodium, a synthetic derivative of prostaglandin I2, primarily acts as a potent inhibitor of platelet aggregation. This compound is widely recognized for its role in the management of pulmonary arterial hypertension (PAH) and is utilized in clinical settings such as pulmonary hypertension and organ transplantation. Its ability to modulate vasodilation and inhibit platelet activation makes it a valuable tool in related biomedical research applications. -
Histamine Release Inhibitor
Alginic acid is a natural polysaccharide recognized for its ability to inhibit histamine release, making it a valuable compound for research into allergic reactions and inflammation. Its remarkable water solubility, film-forming properties, and biodegradability enhance its applicability in various biological studies. Alginic acid has been demonstrated to induce oxidative stress-mediated effects, resulting in hormone secretion disorders, apoptosis, and autophagy in mouse granulosa cells and ovaries. This compound is of particular interest in anti-anaphylactic and anti-inflammatory research applications. -
CaSR inhibitor
Calhex 231 hydrochloride is a potent negative allosteric modulator of the calcium-sensing receptor (CaSR), with an IC50 of 0.39 μM for inhibiting \[³H]inositol phosphate accumulation induced by CaSR activation. It transiently blocks signaling through the human wild-type CaSR and is utilized in research related to traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM), where dysregulated calcium signaling contributes to disease pathology. -
PAR2 inhibitor
I-287 is an orally active and selective protease-activated receptor 2 (PAR2) inhibitor that functions as a negative allosteric modulator, specifically targeting Gαq and Gα12/13 signaling pathways and their downstream effectors. By disrupting PAR2-mediated signaling, I-287 effectively reduces inflammation in preclinical models, including Complete Freund's Adjuvant (CFA)-induced inflammation in mice. -
NSAID/COX inhibitor
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory drug (NSAID) that functions primarily by inhibiting cyclooxygenase (COX) enzymes, thereby reducing the synthesis of pro-inflammatory prostaglandins. In addition to its classical NSAID activity, Fenoprofen has been identified as a positive allosteric modulator (PAM) of melanocortin receptors (MCRs), enhancing MCR-mediated signaling. Fenoprofen also promotes ERK1/2 activation in HEK293T cells, suggesting additional modulation of intracellular signaling pathways involved in inflammation and cellular proliferation. -
NMDAR/TRPM4 inhibitor
Brophenexin (compound 8) is a potent inhibitor of the interaction interface between NMDA receptors (NMDAR) and TRPM4 channels, exhibiting significant neuroprotective activity. It prevents NMDA-induced excitotoxicity, including cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. In vivo, Brophenexin protects against brain damage in mice subjected to middle cerebral artery occlusion (MCAO) and preserves retinal ganglion cells from NMDA-induced degeneration. These findings support its potential as a therapeutic agent for neurodegenerative diseases and ischemic brain injury. -
GRK5 inhibitor
KR-39038 is a potent and orally bioavailable inhibitor of G protein-coupled receptor kinase 5 (GRK5), with an IC₅₀ of 0.02 μM. It effectively suppresses angiotensin II–induced cellular hypertrophy by inhibiting the HDAC5 signaling pathway in neonatal cardiomyocytes. KR-39038 exhibits strong anti-hypertrophic activity and improves cardiac function in preclinical models, making it a promising candidate for research in heart failure and related cardiovascular diseases. -
ErbB2 inhibitor
AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease. -
PDE Inhibitor
Theophylline sodium acetate functions as a potent phosphodiesterase (PDE) inhibitor, specifically targeting PDE3 to promote the relaxation of airway smooth muscle. It also acts as an adenosine receptor antagonist and histone deacetylase (HDAC) activator, contributing to its anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation to the nucleus. Additionally, Theophylline sodium acetate is known to induce apoptosis, making it a valuable reagent for research on asthma and chronic obstructive pulmonary disease (COPD). -
CXCR4 Inhibitor
Hit 14 is a selective inhibitor of C-X-C chemokine receptor type 4 (CXCR4), demonstrating an IC50 value of 254 nM. This compound effectively inhibits the migration and invasion of MDA-MB-231 cells, highlighting its potential in cancer research. Furthermore, Hit 14 modulates Akt phosphorylation and exhibits anti-inflammatory properties, demonstrating efficacy in reducing ear swelling and damage in mouse models. Its diverse biological activities make it a valuable tool for studies related to cancer metastasis and inflammation. -
Angiotensin Receptor Inhibitor
YS-49 monohydrate is a selective angiotensin receptor inhibitor, primarily targeting the angiotensin II pathway. This compound effectively reduces angiotensin II-stimulated proliferation of vascular smooth muscle cells by inducing heme oxygenase-1, offering potential therapeutic insights for cardiovascular research. Additionally, as an isoquinoline alkaloid, YS-49 demonstrates significant positive inotropic effects through the activation of cardiac β-adrenoceptors, making it a valuable reagent for studies involving cardiac function and vascular biology. -
CB1/P-gp Inhibitor
Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR). -
Dopamine β-hydroxylase Inhibitor
Fusaric acid is a potent dopamine β-hydroxylase inhibitor that reduces endogenous levels of norepinephrine and epinephrine in various tissues, including the brain, heart, spleen, and adrenal glands. By inducing oxidative stress and apoptosis, fusaric acid disrupts mitochondrial integrity and activates key apoptosis-related proteases such as Caspase-3/7, -8, and -9. Additionally, fusaric acid regulates pivotal apoptotic proteins, inhibits fibrosis-related signaling pathways including NF-κB and TGF-β1/SMADs, and mitigates collagen deposition. Its applications extend to myocardial fibrosis and cardiac hypertrophy research, as well as studies on esophageal and liver cancers. -
IBAT Inhibitor
(S)-Elobixibat is a selective inhibitor of the intestinal bile acid transporter (IBAT). It effectively lowers LDL cholesterol levels, enhances serum levels of GLP-1, and promotes colonic motility, making it a valuable tool in metabolic syndrome research. This compound is utilized in studies related to constipation, dyslipidemia, non-alcoholic fatty liver disease, and liver tumors. -
A2AAR/HDAC Dual Inhibitor
A2AAR/HDAC-IN-2 is a potent dual inhibitor targeting the adenosine A2A receptor (A2AAR) and histone deacetylase 1 (HDAC1). It demonstrates a strong binding affinity for A2AAR with a Ki value of 10.3 nM and exhibits significant inhibitory activity against HDAC1 with an IC50 of 18.5 nM. This compound is applicable in cancer research, particularly in studies exploring antitumor mechanisms and therapeutic efficacy. -
A2AAR/HDAC Inhibitor
A2AAR/HDAC-IN-1 is a potent dual inhibitor targeting the A2A adenosine receptor (A2AAR) and histone deacetylase 1 (HDAC1), with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. This compound demonstrates significant anticancer activity, making it a valuable reagent for research in cancer therapeutics and epigenetic modulation. Its oral bioavailability enhances its utility in in vivo studies, facilitating investigations into the mechanisms underlying tumor growth and proliferation. -
Histamine Receptor Inhibitor
Levodropropizine is a selective histamine receptor inhibitor primarily used as a peripheral antitussive agent. Its mechanism of action involves the suppression of cough reflexes through its interaction with histamine receptors, making it effective in treating cough associated with colds and allergies. Levodropropizine is noted for its good tolerance profile, facilitating its use in various research applications focused on respiratory physiology and pharmacology. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses.
