Catalog No.
Product Name
Application
Product Information
Citations
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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. -
BDZ receptor agonist
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for ?CGABA and +GABA respectively. - Xanthocillin X permethyl ether is a natural compound isolated from fungal extracts, with Aβ-42 lowering activity.
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BACE-1 inhibitor
BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC50 of 56 nM. -
β-amyloid PET tracer
4-(6-Bromo-2-benzothiazolyl)benzenamine is a β-amyloid PET (positron emission tomography) tracer that can be used in the diagnosis of neurological diseases, such as Alzheimer's and Down's syndrome. -
amyloid imaging agent
4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent amyloid imaging agent which binds to Amyloid-β (1-40) with a KD of 1.7 nM. -
glutaminyl cyclase inhibitor
Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC50 of 1.23 μM. -
glutaminyl cyclase inhibitor
Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM. -
GluN2B modulator
BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM). -
α4β2 nicotinic acetylcholine receptor partial agonist
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. -
GABAA receptor agonist
Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. - Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
- Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.
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P2X7R antagonist
AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10?nM. -
mAChR M5 positive allosteric modulator
VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM. -
OGT donor substrate
UDP-GlcNAc Disodium Salt (UDP-α-D-N-Acetylglucosamine Disodium Salt) is a donor substrate of O-GlcNAc transferase (OGT). -
Oligomeric aggregation inhibitor
Anle138b is an oligomeric aggregation inhibitor. Anle138b is an oligomer modulator for neurodegenerative diseases such Parkinson's disease. -
GABAA α5 inverse agonist
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively). -
COX2 inhibitor
COX-2-IN-2 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX-2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities. -
BACE1 inhibitor
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay. -
NMDA receptor partial agonist
Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist.
