Catalog No.
Product Name
Application
Product Information
Citations
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benzodiazepine receptor antagonist
Sarmazenil is a benzodiazepine receptor antagonist. -
muscarinic agonist
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes. - Valnoctamide (MI-181) is discontinued (DEA controlled substance). It is a chiral constitutional isomer of valproic acid. It is a mild tranquilizer endowed with anticonvulsant properties, suggesting it may be an alternative treatment for epilepsy and bipolar disorder.
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P2X7 receptor antagonist
JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively. -
BuChE inhibitor
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. -
β-amyloid (Aβ) inhibitor
ALZ-801 is an oral, small-molecule inhibitor of beta amyloid (Aβ) oligomer formation for Alzheimer's disease (AD). ALZ-801 is a prodrug of tramiprosate with improved pharmacokinetic properties and gastrointestinal tolerability. -
α7 nAChR modulator
-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity. -
BACE-1 inhibitor
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. - Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm.
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COX/LOX inhibitor
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 ?M?? - Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.
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AChE inhibitor
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines. - Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1.
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BACE1 inhibitor
BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM. -
BACE-1 inhibitor
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor for the treatment of Alzheimer's disease (AD). -
P2X3R antagonist
Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. - Dexetimide ((+)-Benzetimide) is a high-affinity muscarinic receptor antagonist and a potent and persistent anticholinergic agent used to treat neuroleptic-induced parkinsonism.
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partial M1 agonist and M2/M3 antagonist
Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist. -
GABAA receptor modulator
Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors. -
CaMK antagonist
Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to CaMK with a Kd of 3 nM. -
GlyT1 inhibitor
GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC50 of 38 nM for rGlyT1. Antipsychotic activity. -
NMDA channel blocker
Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a binding (Ki) of 0.56-2.1?μM. -
COX-1/COX-2 inhibitor
(-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively. - (+)-Corynoline is an acetylcholinesterase inhibitor isolated from Corydalis incisa.
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BACE1 Inhibitor
Timosaponin B-II is a major active component of Anemarrhena asphodeloides Bunge (Liliaceae, rhizome) that has protective effects against cerebral ischaemic damage. - 4-Aminobutyric acid is the chief inhibitory neurotransmitter in the mammalian central nervous system.
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Glycine reuptake inhibitor
RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1). -
Glycine reuptake inhibitor
RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1). -
M1 agonist
Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome. -
Anxiolytic anticonvulsant
Etifoxine hydrochloride is potentiator of GABAA receptor function in cultured neurons. -
nAChR Inhibitor
EVP-6124 is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs); shows selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs.
