Catalog No.
Product Name
Application
Product Information
Citations
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Endothelin ETA Receptor Antagonist
S-1255 is a highly selective endothelin ETA receptor antagonist with a dissociation constant (Kd) of 0.39 nM. This compound effectively inhibits vasoconstriction, leading to sustained hypotensive effects in hypertensive animal models. S-1255 serves as a valuable tool in the study of hypertension and related cardiovascular disorders, providing insights into the endothelin signaling pathway and its role in vascular regulation. -
Endothelin-A Antagonist
BMS-187308 is an orally active antagonist of the endothelin-A (ETA) receptor, exhibiting a Ki of 4.7 nM for ETA and a Ki of 1.7 μM for ETB. This compound effectively inhibits the pressor response to endothelin-1 (ET-1) with an ED25 value of 1.2 µmol/kg when administered intravenously. BMS-187308 serves as a valuable tool for research focused on the physiological and pathophysiological roles of endothelin in various biological systems. -
Endothelin Receptor Agonist
Sarafotoxin S6b is a potent vasoconstrictor peptide and a non-selective agonist of endothelin receptors. This compound effectively induces contraction in isolated human coronary arteries, exhibiting Ki values of 0.27 nM, 0.55 nM, and 19.5 nM for the coronary artery, saphenous vein, and coronary artery, respectively. Sarafotoxin S6b is valuable for research applications focused on cardiovascular physiology and the roles of endothelin signaling in vascular constriction. -
Endothelin (ETA) Receptor Antagonist
CI-1020 is a selective antagonist of the endothelin (ETA) receptor, exhibiting an IC50 value of 0.3 nM. This compound effectively inhibits intimal hyperplasia in human saphenous vein organ culture. Furthermore, CI-1020 demonstrates potential in the treatment of hypoxic pulmonary hypertension by blocking ET-1-induced pressor responses following oral administration, making it a valuable tool for research in vascular biology and cardiovascular diseases. -
Endothelin A Receptor Antagonist
Fandosentan potassium is a selective antagonist of the endothelin A receptor (ETAR). It effectively reverses hypoxic pulmonary vasoconstriction in perinatal lamb models, making it a valuable tool for investigating pulmonary hypertension. Additionally, Fandosentan potassium inhibits the activities of CYP2C9 and CYP3A4 with IC50 values of 39.6 μM and 21.6 μM, respectively, supporting its application in exploring drug metabolism and interactions. -
ETB Receptor Agonist
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist known for its ability to displace [125I] ET-1 binding at ETB receptors, exhibiting an IC50 of 0.2 nM. This compound induces vasoconstriction in the rabbit pulmonary artery and promotes relaxation of the pig urinary bladder neck. BQ-3020 is valuable for research in cardiovascular diseases, providing insights into endothelin signaling pathways and their physiological implications. -
ETA Receptor Antagonist
PD 155080 is a selective antagonist of the endothelin A (ETA) receptor. It effectively reduces coronary resistance in isolated rat heart models and enhances both systolic and diastolic myocardial function in ischemia/reperfusion studies. This reagent is valuable for research focused on cardiovascular diseases, including the investigation of endothelin's role in cardiac function and pathology. -
Endothelin converting enzyme inhibitor
Daglutril targets the endothelin receptor, exhibiting the ability to modulate cytokine-induced endothelin-1 production in astrocytes. Its inhibitory effects on endothelin-1 generation make it a valuable research tool for screening compounds that regulate this peptide's synthesis in glial cells. This compound is particularly relevant for studies investigating the role of endothelin-1 in neuroinflammation and related neurological disorders. -
Endothelin Receptor Antagonist
TAK 044 is an antagonist of the Endothelin Receptor, exhibiting potent inhibitory effects on endothelin-induced pathological changes in various animal models. This compound is valuable for exploring the role of endothelin in diseases such as acute myocardial infarction, acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage. Researchers can leverage TAK 044 to investigate therapeutic strategies targeting endothelin-related conditions. -
Endothelin Antagonist
PD 156252 is a highly potent endothelin antagonist, primarily targeting the ETA and ETB receptor subtypes. It exhibits enhanced binding affinity with IC50 values of 1.0 nM for rabbit ETA receptors and 40 nM for rat ETB receptors. This compound is valuable for research applications focusing on the endothelin system, cardiovascular studies, and investigations into related pathophysiological conditions. -
ETA Receptor Antagonist
BQ-610 is a selective antagonist of the endothelin A receptor (ETA), functioning as a competitive inhibitor of endothelin-1 (ET-1) binding. This inhibition leads to the attenuation of vascular smooth muscle contraction, reduction in cell mitosis, and diminished hormone secretion. BQ-610 has demonstrated efficacy in alleviating cerebral vasospasm in animal models, inhibiting bronchial epithelial and pulmonary vascular cell proliferation induced by cigarette smoke, and delaying natural luteal regression in bovine reproduction. This reagent is valuable for research focusing on vasospasm, abnormal cellular proliferation, and reproductive endocrine disorders. -
Macitentan Metabolite
ACT-373898 is the inactive carboxylic acid metabolite of Macitentan, a non-peptide dual antagonist of ETA and ETB endothelin receptors. This compound serves as a valuable reference for studies examining the pharmacokinetics and metabolic pathways of Macitentan. Its characterization is essential for understanding the therapeutic efficacy and safety profiles associated with endothelin receptor modulation in cardiovascular research. -
Endothelin Receptor Antagonist
TA-0201 is a competitive, non-peptide antagonist targeting endothelin receptors. It effectively inhibits the binding of [125I]ET-1 to cloned human ETA and ETB receptors, demonstrating Ki values of 15 pM and 41 nM, respectively. TA-0201 further reduces the pressor response induced by exogenous big ET-1, making it a valuable tool for studies aimed at understanding endothelin-mediated pathways and potential therapeutic interventions in cardiovascular research. -
Histamine Methylated Product
3-Methylhistamine dihydrochloride is a methylated derivative of histamine that serves as a significant biomarker in the study of immune responses. This compound has been shown to be upregulated in vaccinated murine models, making it useful for research applications focused on immunological studies and histamine-related pathways. Its role in the modulation of immune activity positions it as a valuable reagent in exploring allergic reactions and other histamine-mediated processes. -
PGF2α Analog
Fenprostalene is a potent analog of prostaglandin F2α (PGF2α) that primarily targets the prostaglandin pathway. This compound is effective in veterinary medicine for inducing corpus luteum regression and lowering blood progesterone levels in dogs. Its primary applications include the treatment of pyometra and the induction of abortion, making it a critical reagent in reproductive health studies and veterinary practices. -
Amino Acid Derivatives
H-Lys(Fmoc)-OH hydrochloride is an amino acid derivative featuring an Fmoc protecting group. This compound serves as a key intermediate for the synthesis of diacylated GLP-1 derivatives, which possess antidiabetic properties. Its utility in peptide synthesis makes it an important reagent in chemical biology and drug development. -
Amino Acid Derivatives
Boc-Leu-OH hydrate (N-Boc-L-leucine monohydrate) is a protected form of the amino acid leucine, featuring a Boc protecting group. It serves as a useful intermediate in peptide synthesis, particularly for the generation of L-prolyl-L-leucyl-glycinamide, a peptide mimetic known for its modulatory effects on dopamine receptors. This compound is valuable in research focused on neuropharmacology and peptide therapeutics. -
PROTAC Linker
2-[4-(Aminomethyl)triazol-1-yl]ethanamine is a specialized PROTAC linker that serves as a crucial component in targeted protein degradation strategies. This compound facilitates the synthesis of PROTAC CB1R Degrader-1, enabling the effective modulation of cannabinoid receptor 1 (CB1R) levels. Its application in research supports investigations into protein homeostasis and therapeutic approaches for various diseases. -
Ligand for Target Protein for PROTAC
Rimonabant carboxylic acid is a ligand used for the targeted protein degradation (PROTAC) approach by engaging with the target protein. This compound plays a crucial role in synthesizing PROTAC CB1R Degrader-1, facilitating the study of cannabinoid receptor biology and influencing metabolic processes. It serves as a valuable tool for researchers investigating innovative therapeutic strategies for conditions related to the endocannabinoid system. -
PN-1 Agonist
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1), promoting its expression through the cAMP-PKA-Sp1 signaling pathway, which enhances granule biogenesis in endocrine cells. This compound is instrumental in studying the regulation of secretory functions and demonstrates selectivity for β-adrenergic receptors. By interacting with β1-adrenergic receptors, Serpinin activates the AC-cAMP-PKA pathway, crucial for regulating myocardial systolic and diastolic function. Additionally, pGlu-serpinin has been shown to upregulate Bcl2 mRNA transcription, contributing to its neuroprotective effects. -
Anti-platelet Aggregation Agent
Antiplatelet agent 3 is a potent anti-platelet aggregation agent that inhibits platelet aggregation induced by ADP, AA, and COL, with IC50 values of 2.55, 3.22, and 2.09 mg/mL, respectively. This compound demonstrates significant biological activity advantageous for elucidating mechanisms involved in thrombosis and other cardiovascular conditions. Antiplatelet agent 3 is suitable for use in cardiovascular disease research, providing insights into therapeutic strategies for managing platelet-related disorders. -
β-Glucuronidase Inhibitor
β-Glucuronidase-IN-5 is a selective inhibitor of β-glucuronidase with an IC50 value of 39.8 μM. This compound demonstrates low cytotoxicity in PC-3 cells, with an IC50 greater than 30 μM, and shows no affinity for adenosine receptors A₁ and A₂A. β-Glucuronidase-IN-5 is useful for investigating diseases associated with overexpression of β-glucuronidase, including colon cancer, arthritis, and complications related to AIDS. -
PAF C-16 Precursor/Metabolite
Lyso-PAF C-16 is a key precursor and metabolite of 1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine (PAF C-16). It serves as a substrate in the remodeling pathway for the formation of PAF C-16 and is also involved in the selective acylation with arachidonic acid through a CoA-independent transacylase. This compound is beneficial for research into lipid metabolism and the roles of bioactive lipids in various biological processes. -
PAFAH1b2/1b3 Inhibitor
P11 is a selective inhibitor of platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3, demonstrating significant impairment of cancer cell survival. With IC50 values of approximately 40 nM for PAFAH1b2 and 900 nM for PAFAH1b3, P11 is a valuable tool for investigating the role of these enzymes in cancer biology and related research applications, including studies focused on cell proliferation and apoptosis. -
H3 Agonist
Immepip dihydrobromide acts as a selective agonist for the H3 histamine receptor. It is known to attenuate cortical histamine release, thereby influencing neurotransmitter dynamics. This compound is applicable in the study of neurological disorders, providing insights into histaminergic system modulation and its potential therapeutic effects. -
Smoothened Agonist
SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist, with an EC50 of 3 nM and a Kd of 59 nM. This compound effectively activates the Hedgehog signaling pathway, providing a robust mechanism to counteract the inhibitory effects of Cyclopamine. SAG dihydrochloride is valuable for research in developmental biology, cancer biology, and therapeutic strategies targeting Hedgehog-related pathways. -
Smoothened Antagonist
KAAD-Cyclopamine is an antagonist of the Smoothened receptor, a critical component of the Hedgehog signaling pathway. This compound effectively inhibits hedgehog signaling, thereby influencing cell proliferation and differentiation processes. It is widely used in research related to developmental biology, cancer, and regenerative medicine, facilitating the study of signaling cascades and their implications in various diseases. -
hSMOX Inhibitor
JNJ-1289 is a potent and selective inhibitor of human spermine oxidase (hSMOX), exhibiting a competitive and allosteric mechanism of action with an IC50 value of 50 nM. This compound is primarily utilized in research studies focused on polyamine catabolism, inflammation, and various cancer models, providing valuable insights into the role of hSMOX in these biological processes. -
Smo Probe
BODIPY-Cyclopamine is a fluorescent ligand targeting the Smoothened (SMO) receptor, crucial for Hedgehog signaling pathway regulation. Dysregulation of this pathway is linked to tumorigenesis, making BODIPY-Cyclopamine valuable for research related to cancer biology. Utilizing the NanoBRET (Nanofluorescein bioluminescence resonance energy transfer) technique, this compound facilitates the sensitive detection of energy transfer between SMO and the fluorescent probe, enabling high-throughput screening and kinetic studies. Additionally, investigating the binding dynamics of BODIPY-Cyclopamine can assist in the development of SMO-targeted therapeutics. -
Smo Receptors Antagonist
MRT-81 is a potent antagonist of smoothened (Smo) receptors in both human and rodent models, exhibiting an IC50 value of 41 nM in Shh-light2 cells. This compound effectively inhibits hedgehog signaling pathways, making it a valuable tool in cancer research. Its ability to modulate Smo activity facilitates investigations into Hedgehog pathway-related tumors and their therapeutic interventions. -
Smo Antagonist
IHR-1 is a cell membrane impermeable antagonist of Smoothened (Smo), a key component of the Hedgehog signaling pathway. This compound effectively inhibits Smo activity, making it a valuable tool for studying Hedgehog-related biological processes and disease states, such as cancer and developmental disorders. IHR-1's specificity for Smo allows for targeted research into the mechanistic roles of this pathway in various cellular contexts. -
Smo Inhibitor
MRT-83 hydrochloride is a potent Smoothened (Smo) receptor antagonist. By inhibiting the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo, MRT-83 hydrochloride demonstrates significant biological activity. This compound is particularly relevant for research applications focused on cancer and associated signaling pathways. -
Smo Antagonist
MRT-10 is a smoothened (Smo) antagonist that effectively inhibits Smo activity with an IC50 of 0.65 μM in various Hedgehog (Hh) signaling assays. By binding to the Bodipycyclopamine-binding site on the Smo receptor, MRT-10 serves as a valuable tool for investigating the roles of Hedgehog signaling in cancer biology. Its application may extend to studies focused on tumor growth and progression influenced by aberrant Hedgehog pathway activation. -
Smoothened Inhibitor
Glasdegib maleate is a potent smoothened inhibitor that selectively targets the human Smoothened (SMO) protein. With an IC50 value of 4 nM, this orally bioavailable compound effectively modulates the Hedgehog signaling pathway, making it valuable for research in cancer biology and developmental processes. Glasdegib maleate is primarily used in studies investigating tumor growth and metastasis driven by aberrant Hedgehog signaling. -
Smo Inhibitor
Glasdegib hydrochloride is a potent smoothened (SMO) inhibitor, primarily targeting the Hedgehog signaling pathway. It exhibits high affinity for human SMO, with an IC50 of 4 nM, making it an effective tool for research in cancer biology and developmental processes. This compound is valuable for studies investigating the role of SMO in tumorigenesis and therapeutic resistance in various malignancies. -
SMO Inhibitor
AZD7254 is an orally active Smoothened (SMO) inhibitor with a reported EC50 of 1.0 nM against Sonic Hedgehog (Shh) protein. This compound effectively modulates hedgehog signaling pathways, making it a valuable tool for investigating the role of SMO in various cancers and developmental disorders. Its potent inhibition of SMO activity supports research applications in targeted therapies and pathway analysis. -
Smo Antagonist
MRT-14 is a potent Smoothened (Smo) antagonist, specifically targeting the Hedgehog (Hh) signaling pathway. By inhibiting Smo, MRT-14 disrupts the signal transduction linked to Hh morphogens. This compound demonstrates potential for research applications in various cancers associated with dysregulated Hh signaling. -
Smo Agonist
(Rac)-SAG is a potent agonist of the Smoothened (Smo) receptor, exhibiting an EC50 of 3 nM and a Kd of 59 nM. This compound activates the Hedgehog signaling pathway, making it an invaluable tool in studies focused on Smo-mediated processes. Additionally, (Rac)-SAG can counteract the inhibition of Smo by Cyclopamine, facilitating research into signaling and developmental biology. -
SMO Inhibitor
SMO-IN-1 is an orally active Smoothened (SMO) inhibitor that demonstrates an EC50 of 89 nM for sonic hedgehog (Shh) protein. This compound is effective in disrupting the hedgehog signaling pathway, making it a valuable tool in cancer research and developmental biology studies. It may be particularly relevant for investigating tumors associated with aberrant hedgehog signaling. -
Smoothened Antagonist
SMO-IN-4 is a potent oral antagonist of the Smoothened (SMO) protein, displaying an IC50 of 24 nM. This compound demonstrates significant antitumor activity and is utilized in research focused on hedgehog signaling pathways and cancer therapy. SMO-IN-4 serves as a valuable tool for investigating SMO-related mechanisms in various malignancies. -
Smo Antagonist
PF-5274857 hydrochloride is a potent, selective antagonist of Smoothened (Smo) with an IC50 of 5.8 nM and a Ki of 4.6 nM. Its oral bioavailability and ability to penetrate the blood-brain barrier enhance its utility in research on tumors, particularly brain tumors and brain metastases associated with an activated Hedgehog (Hh) signaling pathway. This compound is valuable for studies aimed at understanding Smo-mediated tumorigenesis and developing targeted therapeutics. -
Smo Activator
7-keto-25-Hydroxycholesterol is an oxysterol that acts as an activator of Smoothened (Smo). This compound interacts specifically with the extracellular cysteine-rich domain (CRD) of Smo, facilitating its activation. Research applications include studies on hedgehog signaling pathways and the exploration of Smo’s role in developmental biology and cancer. -
Smo Inhibitor
Saridegib hydrochloride is a selective inhibitor of Smoothened (Smo), a critical component of the Hedgehog (Hh) signaling pathway. By targeting Smo, this compound effectively disrupts Hh-mediated signaling, which is implicated in various developmental processes and diseases, including cancer. It is utilized in research to explore the role of the Hh pathway in tumorigenesis and as a potential therapeutic approach in Smo-dependent malignancies. -
ARα2c Inhibitor
BAY-2925976 is an α2C adrenergic receptor (ARα2C) inhibitor that selectively blocks receptor activity. This compound is primarily utilized in research related to obstructive sleep apnea (OSA), providing insights into its underlying mechanisms and potential therapeutic approaches. BAY-2925976 aids in elucidating the role of ARα2C in respiratory regulation and sleep disorders. -
β-AR Antagonist
Lubabegron fumarate is a selectiveβ-adrenergic receptor (β-AR) modulator, exhibiting antagonistic properties at both β1 and β2 receptor subtypes while acting as an agonist at the β3 subtype in bovine species. This compound effectively reduces ammonia (NH3) gas emissions from livestock and their waste, making it a valuable tool for improving environmental sustainability in agricultural practices. Lubabegron fumarate is primarily used in research applications focused on animal health and emissions management. -
Sigma Receptor Ligand
Caprospinol is a potent σ-1 receptor ligand that exhibits neuroprotective properties through multiple mechanisms. It effectively binds to β-amyloid protein (Aβ(42)), interacts with the mitochondrial respiratory chain, and facilitates the clearance of Aβ(42) monomers. Caprospinol is capable of crossing the blood-brain barrier, thereby showing promise in restoring cognitive function and inhibiting the progression of Alzheimer's disease. Its diverse biological activities make it a valuable tool for research in neurodegenerative disorders. -
Anticholinergic
Piperilate is an anticholinergic agent that functions primarily as a PAF antagonist through its hetrazepine derivatives. This compound exhibits significant biological activity in the treatment of bronchial asthma and demonstrates hypotensive effects. Additionally, Piperilate has been shown to effectively rescue mice from organophosphate poisoning, making it a valuable reagent for research into respiratory conditions and toxicology. -
DA/NE/5-HT Inhibitor
Tesofensine is a triple monoamine reuptake inhibitor targeting dopamine (DA), norepinephrine (NE), and serotonin (5-HT). It effectively inhibits the reuptake of these neurotransmitters in the synaptic cleft, exhibiting IC50 values of 6.5 nM for DA, 1.7 nM for NE, and 11 nM for 5-HT. Tesofensine is primarily studied for its potential as an anti-obesity agent and may be useful in related central nervous system research applications. -
MAO-A And 5-HT-uptake Inhibitor
Sercloremine hydrochloride is a selective and reversible inhibitor of monoamine oxidase A (MAO-A) and serotonin (5-HT) uptake. This compound is primarily utilized in research related to depression, offering insights into the modulation of serotonin levels and its effects on mood regulation. Its dual mechanism of action makes it valuable for exploring therapeutic approaches in depressive disorders. -
5-HT Reuptake Inhibitor
Clomipramine is a potent 5-HT reuptake inhibitor with an IC50 value of 1.5 nM. As a tricyclic antidepressant, it is primarily utilized in research investigating the mechanisms of depression and obsessive-compulsive disorder (OCD). Its ability to influence serotonin levels makes it a valuable tool for studying various neuropsychiatric conditions.
