Catalog No.
Product Name
Application
Product Information
Citations
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A1 Adenosine Receptor Agonist
CCPA (2-Chloro-N6-cyclopentyladenosine) is a highly selective agonist for A1 adenosine receptors, demonstrating a Ki value of 0.4 nM. This compound effectively inhibits adenylate cyclase, with an IC50 of 33 nM. CCPA is relevant in studies investigating anti-seizure and cardioprotective effects, making it a valuable tool for research related to seizures and myocardial infarction. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Adrenergic Receptor Antagonist
Aaptamine is an alkaloid derived from the marine sponge Aaptos suberitoides, functioning primarily as a competitive antagonist of the α-adrenergic receptor. This compound exhibits significant cytotoxicity against tumor cells, inducing apoptosis and cell cycle arrest while promoting p21 expression through a p53-independent mechanism. Aaptamine also demonstrates a variety of biological activities, including anti-tumor, antioxidant, antibacterial, and analgesic effects, making it a valuable tool for cancer research and therapeutic applications. -
α-1A Adrenergic Receptor Agonist
Dabuzalgron is a selective α-1A adrenergic receptor agonist primarily utilized for the treatment of urinary incontinence. This compound exhibits key biological activity by enhancing bladder function, thereby mitigating symptoms associated with overactive bladder. Additionally, Dabuzalgron has been shown to provide protection against Doxorubicin-induced cardiotoxicity through the preservation of mitochondrial function, making it relevant in cardiovascular research. -
S1PR1 Antagonist
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 value of 398 nM. This compound is instrumental in studying the role of S1PR1 in various biological processes, including immune modulation and cardiovascular function. W146 TFA is valuable for research applications involving cytokine signaling and cellular proliferation pathways. -
ICMT Inhibitor
UCM-1336 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), exhibiting an IC50 of 2 μM. This compound effectively induces mislocalization of endogenous Ras, resulting in decreased Ras activation. UCM-1336 has shown the ability to trigger cell death through autophagy and apoptosis, making it a valuable tool for research in cancer biology and signal transduction pathways. -
5-HT2/D1/D2 Antagonist
Olanzapine-d3 is a deuterated form of olanzapine, targeting multiple receptors, including serotonin receptors 5-HT2A, 5-HT2C, and dopamine receptors D1 to D4. This selective and orally active monoaminergic antagonist exhibits high affinity binding with Ki values ranging from 4 to 57 nM for relevant targets. It is primarily utilized in research related to psychopharmacology and the treatment of schizophrenia and bipolar disorder, enabling detailed pharmacokinetic studies and investigation of receptor interactions. -
mGlu1 Antagonist
LY456236 is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), exhibiting an IC50 of 0.145 μM for the inhibition of phosphatidylinositol hydrolysis. Additionally, it demonstrates inhibitory activity against EGFR with an IC50 of 0.918 μM. By targeting the MAPK pathway, LY456236 effectively blocks cell proliferation and reverses the anti-apoptotic effects of DHPG. This reagent is suitable for investigations in epilepsy and related neurological research. -
Stable Isotope
Thioridazine-d3 hydrochloride is a deuterium-labeled derivative of Thioridazine, an antagonist of dopamine receptor D2 family proteins. It demonstrates significant anti-psychotic and anti-anxiety effects while also inhibiting the PI3K-Akt-mTOR signaling pathway, contributing to anti-angiogenic activity. Additionally, Thioridazine exhibits antiproliferative properties and induces apoptosis in various cancer cell types, with particular efficacy against cancer stem cells (CSCs). This stable isotope is valuable for pharmacokinetic studies and elucidating mechanisms of action in related research applications. -
ETA/ETB Antagonist
Macitentan-d4 is a deuterated analog of the dual ETA and ETB endothelin receptor antagonist, Macitentan. This compound exhibits significant biological activity by blocking the effects of endothelin-1, which is implicated in conditions such as pulmonary arterial hypertension (PAH) and idiopathic pulmonary fibrosis (IPF). Macitentan-d4 serves as a valuable tool for research into the underlying mechanisms of endothelin signaling and its role in cardiovascular and pulmonary disorders. -
Endocannabinoid
Arachidonoyl ethanolamide phosphate functions as an endogenous ligand for cannabinoid receptors, primarily targeting the CB1 subtype in the central nervous system and the CB2 subtype in peripheral immune cells. This compound is involved in modulating various physiological processes, including pain perception, mood regulation, and immune response. Its unique action profile makes it useful for research in neurobiology and immunology, particularly in studies focusing on the endocannabinoid system and its implications in various diseases. -
Stable Isotope
N-(Phenylacetyl-d5)glycine is a deuterated form of phenylacetylglycine, functioning as a stable isotope. This compound serves as a gut microbial metabolite that can activate the beta-2 adrenergic receptor (β2AR). Its biological activity includes providing protective effects against cardiac injury induced by ischemia and reperfusion, making it valuable for research in cardiac health and metabolic studies. -
Stable Isotope
D-Mannitol-13C6 is a stable isotope-labeled form of D-Mannitol, targeting metabolic pathways through its role as an osmotic agent. This compound is utilized in various research applications, including studies on calcium and magnesium absorption, cecal fermentation, and the modulation of insulin sensitivity. D-Mannitol has been shown to promote the browning of white adipose tissue by activating the β3-adrenergic receptor, which can lead to enhanced thermogenesis and potential reductions in blood glucose levels. Additionally, it is employed in plant cell culture to maintain osmotic balance and protect cellular integrity. -
Stable Isotope
D-Mannitol-13C is a stable isotope-labeled derivative of D-Mannitol. This compound serves as a valuable osmotic diuretic and is utilized in various research applications, including the study of calcium and magnesium absorption and retention through cecal fermentation. D-Mannitol is known to promote brown adipose tissue formation, enhance insulin sensitivity, and lower blood glucose levels by activating the β3-adrenergic receptor, leading to the conversion of white fat cells into brown fat cells. Additionally, it is employed to maintain osmotic pressure in plant cell cultures, aiding in cellular protection during physiological manipulation. -
Stable Isotope
Perphenazine-d4 is a deuterated derivative of Perphenazine, a typical antipsychotic agent primarily inhibiting the 5-HT2A receptor, alpha-1A adrenergic receptor, dopamine receptor D2/D3, D2L receptor, and histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, allowing for the precise tracking of Perphenazine metabolism and distribution in biological systems. Perphenazine-d4 is essential for researchers focusing on neuropharmacology and drug interaction studies involving antipsychotic medications. -
Antihistamine Agent
Meclizine is an antihistamine that reversibly inhibits the binding of histamine to H1 receptors, making it effective as an anti-motion sickness agent. As a piperazine derivative, it can cross the blood-brain barrier, enabling its use in neurological research. Additionally, Meclizine acts as an agonist for the mouse constitutive androstane receptor (CAR) and serves as an inverse agonist for the human equivalent. This compound is also relevant for studying polyglutamine (polyQ) toxicity disorders, including Huntington's disease. -
Stable Isotope
D-Mannitol-2-13C is a stable isotope-labeled derivative of D-Mannitol. This 13C-labeled compound plays a critical role in metabolic studies, particularly in understanding carbohydrate metabolism and energy homeostasis. D-Mannitol serves as an osmotic diuretic, promotes the absorption of minerals, enhances brown adipose tissue formation, and demonstrates potential for reducing blood glucose levels through β3-adrenergic receptor activation. It is frequently employed in cell culture applications to maintain osmotic pressure and protect cells, particularly when cell walls are compromised. -
Antihistamine Agent
Meclizine dihydrochloride monohydrate is an antihistamine that reversibly inhibits histamine interactions at the H1 receptor. As a member of the piperazine class of H1 antagonists, it is primarily utilized as an effective anti-motion sickness agent. This compound also demonstrates the ability to cross the blood-brain barrier and functions as an agonist for the mouse constitutive androstane receptor (CAR), while acting as an inverse agonist for the human CAR. It has applications in research focusing on polyQ toxicity disorders, including Huntington's disease. -
Somatostatin Receptor Agonist
Octreotide dihydrochloride is a synthetic octapeptide that acts as an agonist for somatostatin receptors, primarily targeting subtypes 2, 3, and 5. By increasing Gi protein activity, it effectively reduces intracellular cAMP levels, contributing to its antitumor effects. Octreotide dihydrochloride is utilized in research applications related to apoptosis and is particularly relevant in studies of acromegaly and other disorders associated with aberrant somatostatin signaling. -
A1 Adenosine Teceptors Agonist
CCPA hemihydrate is a highly selective agonist of the A1 adenosine receptors, exhibiting a Ki value of 0.4 nM. It demonstrates preferential binding to the A1 receptor over the A2 receptor, with a Ki of 3900 nM. As a purine nucleoside analog, CCPA hemihydrate has demonstrated broad antitumor activity, particularly in the context of indolent lymphoid malignancies. Its anticancer effects are mediated through mechanisms such as inhibition of DNA synthesis and induction of apoptosis, making it valuable for research applications in cancer therapy. -
S1P1 Receptor Agonist
(S)-FTY-720 Vinylphosphonate is a chiral phosphonate analogue of Fingolimod that functions as an S1P1 receptor agonist. It demonstrates significant biological activity, activating the S1P1 receptor with an EC50 of 75 nM and effectively inhibiting Camptothecin-induced apoptosis in IEC-6 cells. This reagent is relevant for research into autoimmune diseases, providing insights into therapeutic mechanisms and potential interventions. -
mGlu1 Antagonist
LY456236 free base is a selective, non-competitive antagonist of the metabotropic glutamate receptor 1 (mGlu1), showing an IC50 for phosphatidylinositol hydrolysis of 0.145 μM. Additionally, it inhibits epidermal growth factor receptor (EGFR) activity with an IC50 of 0.918 μM. This compound effectively blocks cell proliferation by targeting the MAPK signaling pathway, counteracting the anti-apoptotic effects of DHPG. LY456236 free base is a valuable tool for research into epilepsy and other neurological disorders. -
Stable Isotope
Cyproheptadine-d3 is a deuterium-labeled derivative of the antihistamine Cyproheptadine, serving as a stable isotope for research applications. It primarily acts as a serotonin and histamine receptor antagonist, making it useful in studies investigating receptor interactions and pharmacokinetics. This reagent is valuable for tracing and quantifying Cyproheptadine in various biological samples, facilitating research in pharmacology and toxicology. -
β2AR Activator
Phenylacetylglycine is a gut microbial metabolite that acts as a β2-adrenergic receptor (β2AR) activator. It has demonstrated protective effects against cardiac injury resulting from ischemia/reperfusion. This compound is significant for research into cardiovascular health and the role of microbiota in modulating cardiac responses. -
Dopaminergic Neurotoxin
MPTP (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is a potent dopaminergic neurotoxin that readily penetrates the blood-brain barrier. It is primarily utilized to create animal models of Parkinson’s Disease, enabling the study of neurodegenerative processes. MPTP acts by converting into MPP+, which induces apoptosis in dopaminergic neurons, serving as a valuable tool for investigating therapeutic strategies and the underlying mechanisms of neurodegeneration. -
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. -
Stable Isotope
Kynurenic acid-d5 is a deuterium-labeled analog of kynurenic acid, an endogenous metabolite of tryptophan. It acts as a broad-spectrum antagonist of NMDA and glutamate receptors, as well as the α7 nicotinic acetylcholine receptor. Additionally, kynurenic acid-d5 serves as an agonist for GPR35/CXCR8, making it valuable in studies related to neuropharmacology and neurotransmitter signaling pathways. This stable isotope is ideal for tracing and characterization studies in metabolic research. -
LPA2 Receptor Antagonist
H2L5186303 is a potent and selective antagonist of the lysophosphatidic acid receptor 2 (LPA2), exhibiting an IC50 of 9 nM. This compound induces apoptosis and effectively inhibits cell proliferation and motility. Additionally, H2L5186303 demonstrates anti-inflammatory properties, making it a valuable reagent for research involving cancer biology and inflammation pathways. -
mGlu4 Agonist
Cinnabarinic acid primarily functions as an orthosteric agonist of the mGlu4 receptor, selectively engaging with residues within its glutamate binding pocket, and exhibiting no significant activity on other mGlu receptors. As an endogenous metabolite of the kynurenine pathway of tryptophan, cinnabarinic acid plays a role in cell apoptosis. This compound is valuable in research exploring mGlu4 receptor signaling and its implications in neurological disorders. -
5-HT2 Receptor Antagonist
Cyproheptadine is a selective antagonist of the 5-HT2A receptor, exhibiting both antidepressant and antiserotonergic properties. In addition to its central nervous system effects, Cyproheptadine demonstrates antiplatelet and thromboprotective activities. This compound is valuable for research applications focused on thromboembolic disorders, contributing to the understanding of related vascular conditions. -
vasopressin agonist
Ornipressin (POR-8) is a vasopressin analog and selective V1 receptor agonist. It is used as a local vasoconstrictor and can effectively reverse hypotension associated with combined general/epidural anesthesia. Ornipressin exhibits antidiuretic activity and, in renal failure models, decreases renal vascular resistance while increasing renal blood flow. -
5-HT antagonist
Pimethixene maleate is a potent antihistamine and antiserotonergic compound used as an antimigraine agent. It exhibits strong antagonistic activity at multiple receptors, including serotonin 5-HT1A (pKi 7.63), 5-HT2A (pKi 10.22), 5-HT2B (pKi 10.44), 5-HT2C (pKi 8.42), histamine H1 (pKi 10.14), dopamine D2 (pKi 8.19), dopamine D4.4 (pKi 7.54), muscarinic M1 (pKi 8.61), and muscarinic M2 (pKi 9.38) receptors. Its broad receptor-binding profile contributes to its therapeutic efficacy in migraine management. - Balixafortide (POL6326) is a potent, selective, and well-tolerated peptidic antagonist of the CXCR4 receptor, with IC50 values below 10 nM. It demonstrates over 1000-fold selectivity for CXCR4 compared to other receptors, including CXCR7. Balixafortide effectively blocks β-arrestin recruitment and calcium flux, and is a strong mobilizer of hematopoietic stem and progenitor cells (HSPCs). It also exhibits anti-cancer activity, making it a promising candidate for oncology and hematology research.
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CXCR1/CXCR2 antagonist
Ladarixin (DF 2156A free base) is an orally active, allosteric, non-competitive antagonist of the chemokine receptors CXCR1 and CXCR2. By blocking these receptors, Ladarixin inhibits neutrophil recruitment and inflammatory responses. It is under investigation for the treatment of inflammatory airway diseases such as chronic obstructive pulmonary disease (COPD) and asthma. -
CXCR antagonist
LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory properties. It binds to CXCL12 with a Ki of 267 nM, thereby preventing its interaction with the CXCR4 receptor. LIT-927 is a valuable tool for studying CXCL12/CXCR4-mediated signaling in inflammatory and immune-related conditions. -
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. -
CaSR agonist
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with a functional affinity (pK\_B) of 5.1. It enhances CaSR activation and is useful for research into disorders related to calcium metabolism, such as hyperparathyroidism and other CaSR-associated diseases. -
CaSR PAM
Calindol hydrochloride is a positive allosteric modulator (PAM) of the calcium-sensing receptor (CaSR), acting as a calcimimetic compound. It enhances CaSR activation with an EC50 of 132 nM, making it a valuable tool for studying calcium homeostasis and related signaling pathways. -
CaSR Antagonist
Encaleret (CLTX-305) is an orally active and highly potent antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 0.012 μM. It promotes the secretion of parathyroid hormone (PTH) by inhibiting CaSR activity and is being investigated for the treatment of conditions such as osteoporosis and autosomal dominant hypocalcemia type 1 (ADH1). -
CaSR agonist
Lycoperodine-1 (Cyclomethyltryptophan) is a bioactive compound isolated from tomato fruits (*Lycopersicon esculentum*). It functions as an agonist of calcium-sensing receptors (CaSR), making it a useful molecule for studying CaSR-mediated signaling pathways and calcium homeostasis. -
CaSR antagonist
Ronacaleret hydrochloride (SB 751689A) is an orally active, potent, and selective antagonist of the calcium-sensing receptor (CaSR). It stimulates the endogenous release of parathyroid hormone (PTH) from the parathyroid glands, supporting its use in the study of postmenopausal osteoporosis and related metabolic bone disorders. -
CaSR antagonist
Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates the endogenous release of parathyroid hormone (PTH) from the parathyroid glands. By modulating calcium homeostasis and enhancing PTH secretion, Ronacaleret is used in the study of postmenopausal osteoporosis and other bone-related metabolic disorders. -
CaSR Antagonist
TAK-075 is an orally active and highly potent calcium-sensing receptor (CaSR) antagonist with an IC50 of 0.94 nM. It promotes transient parathyroid hormone (PTH) secretion in rats and effectively prevents the sustained suppression of PTH caused by the buildup of active metabolites, thereby preserving normal PTH secretion dynamics. TAK-075 is a valuable compound for research in metabolic bone diseases, including osteoporosis. -
CRHR1 antagonist
Antalarmin hydrochloride is an orally active, non-peptide antagonist of corticotropin-releasing hormone receptor 1 (CRHR1) with a Ki of 1 nM. It effectively suppresses CRH-induced adrenocorticotropic hormone (ACTH) secretion and blocks both CRH- and novelty-induced anxiety-like behaviors in animal models. Antalarmin hydrochloride also exhibits anti-inflammatory activity in arthritis models and alleviates stress-induced gastric ulceration, supporting its potential in research related to irritable bowel syndrome and stress-related inflammatory conditions. -
CRFR1 antagonist
NBI-27914 is a potent and selective antagonist of corticotropin-releasing factor receptor 1 (CRFR1), a member of the G protein-coupled receptor (GPCR) superfamily. By selectively blocking CRFR1, NBI-27914 is useful for studying stress-related pathways and disorders mediated by CRF signaling, such as anxiety and depression. -
CRF2 receptor agonist
Urocortin, human, is a 40-amino acid neuropeptide that functions as a selective agonist of the endogenous corticotropin-releasing factor receptor 2 (CRF₂). It exhibits high binding affinity with Kᵢ values of 0.4 nM for human CRF₁, 0.3 nM for rat CRF₂α, and 0.5 nM for mouse CRF₂β. Urocortin plays a role in modulating stress responses, cardiovascular function, and feeding behavior. -
CRF1 antagonist
JNJ19567470 (R317573) is a selective, non-peptidergic corticotropin-releasing factor type 1 (CRF₁) receptor antagonist. It effectively blocks sodium lactate (NaLac)-induced panic-like behavior and associated cardiovascular responses. JNJ19567470 also reduces regional glucose utilization in the amygdala and attenuates anxiety-related responses -
CRHR1 antagonist
Antalarmin is a selective, nonpeptide antagonist of corticotropin-releasing factor receptor 1 (CRHR1), with a Ki of 2.7 nM. It is capable of crossing the blood–brain barrier, making it a valuable compound for investigating CRHR1-mediated central nervous system functions and stress-related disorders. -
CRF2 receptor antagonist
α-Helical CRF(9-41) is a competitive antagonist of the corticotropin-releasing factor receptor 2 (CRF₂) with a K\_B of approximately 100 nM. It also acts as a partial agonist at the CRF₁ receptor, with an EC₅₀ of 140 nM. This dual activity makes it a useful tool for studying CRF receptor signaling and stress-related physiological responses.
