Catalog No.
Product Name
Application
Product Information
Citations
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nAChR Inhibitor
EVP-6124 hydrochloride is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs). EVP-6124 showed selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs. -
gamma-secretase modulator
gamma-secretase modulator 3 is a gamma-secretase modulator. -
CaMKII inhibitor
KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). -
NMDA receptor antagonist
SDZ 220-581 ammonium salt is a potent, competitive antagonist at the NMDA glutamate receptor subtype(pKi= 7.7). -
Muscarinic receptor antagonist
Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD). -
GABA-transaminase inhibitor
Vigabatrin is a structural analog of the inhibitory neurotransmitter ??-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase. -
Gamma-secretase modulator
Compound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25. -
γ-secretase inhibitor
MRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo. - Amyloid b-peptide (42-1) (human), inactive control for Amyloid b (1-42) peptide.
- Amyloid b-Peptide (10-20) (human), soluble amyloid b-peptide fragment that is a substrate for gelatinase A/type IV collagenase/MMP-2 and APP secretase; cleaved between Lys16 and Leu17.
- Amyloid b-peptide (25-35) (human), fragment of human amyloid beta-peptide, functionally required for the neurotrophic and neurotoxic effects associated with Alzheimer's disease.
- Amyloid b-Peptide (12-28) (human), amyloid b-peptide fragment; minimum section required to bind to brain proteins.
- Amyloid b-Peptide (1-40) (human) is a peptide processed from the amyloid precursor protein (APP).
- Amyloid b-Peptide (1-43) (human), amyloid β peptide fragment. Highly toxic, showing higher neurotoxicity compared to Aβ40 and Aβ42.
- Beta-amyloid (1-11) (Abeta) is a peptide with the sequence H-{Asp}{Ala}{Glu}{Phe}{Arg}{His}{Asp}{Ser}{Gly}{Tyr}{Glu}-OH,which is processed from the Amyloid precursor protein.
- Beta-amyloid protein (A beta), a 39-43 amino acid peptide composed of a portion of the transmembrane domain and the extracellular domain of the amyloid precursor protein (APP), is also the principal component of amyloid.
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glutamate receptors agonist
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). -
M3 receptors inhibitor
Imidafenacin is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). -
anti-cancer agent
Ginsenoside Rc, isolated from Panax ginseng, may exert various activities including anti-cancer, anti-inflammatory, antiobesity, and anti-diabetic effects. -
hepatoprotective agent
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. -
CaMK Substrate
Syntide 2 is a substrate peptide for calcium/calmodulin-dependent protein kinase II (CaMKII) that demonstrates selective inhibition of the gibberellin (GA) signaling pathway. By targeting this pathway, Syntide 2 facilitates the investigation of mechanisms underlying plant hormone responses while preserving the activity of other regulatory events, such as those mediated by abscisic acid. This reagent is valuable for studies related to cellular signaling and hormone regulation in plant biology. -
CaMKII Inhibitor
Autocamtide-2-related inhibitory peptide is a selective inhibitor of Calcium/Calmodulin-dependent protein kinase II (CaMKII), exhibiting an IC50 value of 40 nM. This peptide effectively modulates CaMKII activity, making it a valuable tool for studying calcium signaling pathways and their implications in various physiological and pathological processes. Its high specificity and potency simplify the investigation of CaMKII-related mechanisms in cellular signaling research. -
COX Inhibitor
Indomethacin farnesil is a prodrug of indomethacin, primarily targeting cyclooxygenase (COX) enzymes. This potent, blood-brain barrier-permeable inhibitor exhibits nonselective activity against COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. Indomethacin farnesil has been shown to disrupt autophagic flux by impairing lysosomal function, making it useful for investigating inflammatory pathways and autophagy-related processes in research applications. -
Tau ATTEC
MRL828 is a Tau pathology-binding compound that employs the ATTEC technology to selectively target aggregated tau proteins for degradation via the autophagic lysosomal pathway. This reagent effectively decreases intracellular tau aggregates while promoting the secretion of tau from cells. Its unique mechanism makes MRL828 a valuable tool for research on tau-related pathologies and neurodegenerative diseases. -
Sesquiterpene Lactone
Lactupicrin, a sesquiterpene lactone, primarily targets acetylcholinesterase (AChE), exhibiting an inhibitory activity with an IC50 of 150.3 μM. This compound demonstrates notable analgesic, sedative, and antimalarial effects, alongside its atheroprotective properties. Lactupicrin is an orally active bitter compound, making it valuable for research applications focused on neuropharmacology and cardiovascular health. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate (DHEA sulfate) functions as a GABA(A) receptor antagonist and a σ1 receptor agonist. This neurosteroid, primarily secreted by the adrenal gland, is capable of partially penetrating the blood-brain barrier. It inhibits GABA(A) receptor-mediated chloride influx while enhancing NMDA receptor activity via σ1 receptor interaction, displaying anti-inflammatory and antidepressant properties. DHEA sulfate is relevant for research in neuroprotection, depression, post-traumatic stress disorder (PTSD), and Alzheimer’s disease, and may serve as a biomarker for cardiovascular disease mortality due to its correlation with mortality rates. -
GABA(A) Receptor Antagonist/σ1 Receptor Agonist
Dehydroepiandrosterone sulfate sodium (DHEA sulfate) primarily acts as a non-competitive GABA(A) receptor antagonist and σ1 receptor agonist. This neurosteroid, predominantly secreted by the adrenal gland, has demonstrated significant biological activities, including enhancing NMDA receptor function and exerting anti-inflammatory and antidepressant effects. DHEA sulfate sodium can penetrate the blood-brain barrier, making it valuable in research applications related to neuroprotection, neurite growth regulation, and neuropsychiatric disorders such as depression, post-traumatic stress disorder (PTSD), and Alzheimer's disease. Additionally, it may serve as a biomarker for cardiovascular disease mortality, with its levels inversely correlated with mortality rates. -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
AChE/BChE Inhibitor
Epiberberine chloride is an alkaloid derived from Coptis chinensis, functioning primarily as a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 1.07 μM and 6.03 μM, respectively. This compound also serves as a non-competitive inhibitor of BACE1, with an IC50 of 8.55 μM. In addition to its cholinesterase inhibition, Epiberberine chloride exhibits antioxidant properties, demonstrated by its ability to scavenge peroxynitrite (IC50 of 16.83 μM), suggesting a potential protective role in Alzheimer’s disease research. Furthermore, it inhibits the early differentiation of 3T3-L1 preadipocytes and downregulates key signaling pathways, indicating its relevance in studies on diabetes. -
COX-2 Inhibitor
Hexahydrocurcumin is a selective, orally active inhibitor of cyclooxygenase-2 (COX-2), demonstrating significant potential in anti-inflammatory applications. As one of the primary metabolites of curcumin, it exhibits antioxidant and anticancer properties, making it relevant for research in various therapeutic areas. Its selectivity towards COX-2 over COX-1 highlights its potential for minimizing gastrointestinal side effects often associated with non-steroidal anti-inflammatory drugs (NSAIDs). -
Aβ/tau Aggregation Inhibitor
Aβ/tau aggregation-IN-4 is a potent inhibitor of amyloid-beta (Aβ) and tau aggregation. It effectively promotes the degradation of Aβ40 and Aβ42 with IC50 values of 2.151 μM and 3.622 μM, respectively. Additionally, Aβ/tau aggregation-IN-4 exhibits selective inhibition of acetylcholinesterase (AChE) with an IC50 of 5.56 μM, and inhibits monoamine oxidase A (MAO-A) and B (MAO-B) with IC50 values of 0.59 μM and 0.09 μM, respectively. This compound also reduces intracellular reactive oxygen species (ROS) levels, making it a valuable tool in Alzheimer's disease research. -
COX-2 Inhibitor
COX-2-IN-65 is a selective inhibitor of cyclooxygenase-2 (COX-2) with a reported IC50 of 10.24 μM. This compound exhibits antibacterial activity against Staphylococcus aureus and Escherichia coli, while also scavenging reactive oxygen species (ROS). COX-2-IN-65 is valuable for research applications focused on bacterial infections and inflammation pathways. -
MAO-B Inhibitor
MAO-B-IN-7 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE), demonstrating IC50 values of 41 nM for human AChE, 87 nM for electric eel AChE, and 0.3 μM for MAO-B. This compound is notable for its ability to penetrate the blood-brain barrier, making it suitable for central nervous system research. MAO-B-IN-7 has been shown to mitigate oxidative stress and neuroinflammation, supporting its potential applications in neurodegenerative disease studies. -
Insecticide
Methiocarb is an orally active carbamate insecticide primarily targeting acetylcholinesterase to induce cholinergic excitation. It exhibits dose-dependent toxic effects on various organisms, including notable oxidative stress through lipid peroxidation in liver, kidney, brain, and testicular tissues, while also altering reduced glutathione levels via reactive oxygen species generation. This compound is utilized for agricultural pest control and serves as a valuable research tool for studying oxidative stress-related cellular damage in mammalian models. -
NMDA Receptor Inhibitor
MN-05 is a dual neuroprotective and vasodilatory inhibitor of the NMDA receptor. By blocking calcium influx, it reduces free radical production and preserves mitochondrial membrane potential in cortical neurons exposed to glutamate. Additionally, MN-05 exhibits vasodilatory effects by dilating aortic rings in response to phenylephrine-induced contraction. This compound demonstrates protective properties against glutamate-induced neuronal injury in vitro, making it valuable for research in neurodegenerative diseases. -
P2Y Receptor Modulator
Uridine-5'-diphosphate disodium salt functions as an agonist for the P2Y6 receptor, exhibiting high specificity with an EC50 of 300 nM (pEC50=6.52 for the human P2Y6 receptor). This endogenous metabolite plays a crucial role in catalyzing the glucuronidation of various substrates and is also instrumental in RNA biosynthesis. Its modulation of P2Y receptors has significant implications for research in cellular signaling and metabolic processes. -
P2Y Receptor Modulator
Uridine 5'-diphosphate sodium salt is a specific modulator of P2Y receptors, acting as a potent native agonist for the P2Y6 receptor with an EC50 of 300 nM and a pEC50 of 6.52, while also serving as a powerful antagonist at the P2Y14 receptor (pEC50 of 7.28). This endogenous metabolite plays a crucial role in the glucuronidation process of diverse substrates and is integral to nucleic acid biosynthesis, making it a valuable reagent in biochemical and pharmacological research focused on nucleotide signaling pathways and metabolic processes. -
GABAB Receptor Negative Allosteric Modulator
(E/Z)-CLH304a is a negative allosteric modulator of the GABAB receptor, consisting of a mixture of (E)-CLH304a and (Z)-CLH304a. This compound selectively inhibits the GABAB receptor and noncompetitively modulates its activity. Research has demonstrated that (E)-CLH304a is effective in blocking Baclofen-induced ERK1/2 phosphorylation in HEK293 cells that overexpress GABAB receptors, making it a valuable tool for studies investigating GABAB receptor signaling pathways and their implications in neurological disorders. -
P2Y14R Inhibitor
HDB-1 is a selective inhibitor of the P2Y14 receptor (P2Y14R) with an IC50 of 26 pM. This compound effectively blocks the activation of hepatic stellate cells by inhibiting the PKA/Raf1/MEK/ERK signaling pathway associated with P2Y14R, thereby mitigating the progression of liver fibrosis. HDB-1 is valuable for research into the mechanisms underlying liver fibrosis and the development of potential therapeutic strategies. -
Stable Isotope
Propoxur-d3 is the deuterated form of Propoxur, a reversible and competitive acetylcholinesterase (AChE) inhibitor. It crosses the blood-brain barrier and exerts neurotoxic effects by inhibiting AChE activity, leading to increased acetylcholine levels and resultant neurological dysfunction. Additionally, Propoxur-d3 promotes the expression of matrix metalloproteinase-2 (MMP-2) and enhances tumor cell migration and invasion through the generation of intracellular reactive oxygen species (ROS) and the activation of the ERK/Nrf2 signaling pathway. This compound has applications in neurotoxicity studies and cancer research, as well as in assessing pesticide effects in ecological studies. -
α7 nAChR Agonist
A-582941 is a selective α7 nicotinic acetylcholine receptor (nAChR) agonist that effectively crosses the blood-brain barrier. With Ki values of 10.8 nM in rat brain and 17 nM in human frontal cortex, it demonstrates significant biological activity by promoting ERK1/2 and CREB phosphorylation, inhibiting GSK-3β through Ser-9 phosphorylation, and enhancing acetylcholine release. Additionally, A-582941 induces the expression of activity-regulated cytoskeleton-associated protein (Arc) and c-Fos while activating brain regions linked to working memory and attention. This compound is valuable for investigating mechanisms involved in Alzheimer's disease and schizophrenia. -
Stable Isotope
Propoxur-d7 is the deuterium-labeled analog of Propoxur, a reversible and competitive inhibitor of acetylcholinesterase (AChE). This compound exhibits significant neurotoxic effects by inhibiting AChE activity, leading to increased levels of acetylcholine and subsequent neurological dysfunction. Propoxur-d7 also enhances tumor cell migration and invasion through the promotion of matrix metalloproteinase-2 (MMP-2) expression, driven by reactive oxygen species (ROS) generation and activation of the ERK/Nrf2 signaling pathway. Additionally, Propoxur serves as a carbamate insecticide effective against a variety of pests in turf, forestry, and household settings.
