Catalog No.
Product Name
Application
Product Information
Product Citation
- Methoctramine hydrate is a selective M2 muscarinic receptor antagonist at nM concentrations
- Lingyu Wang, .et al. , Gut Microbes, 2020, 12(1): 1-20 PMID: 33006494
- Darifenacin works by blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions.
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COX-1 inhibitor
(-)-Epicatechin is a natural product from green tea. (-)Epicatechin is an inhibitor of Cox-1- Grace Northrop, .et al. , Food Funct, 2022, Apr 4;13(7):3894-3904 PMID: 35285840
- A S D'Costa, .et al. , Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Mihaela Tudorache, .et al. , Food Hydrocoll, 2019, 97, Dec, 105193
- Md Shajedul Islam, .et al. , Innovative food science & emerging technologies, 2016, v.34 pp. 344-351
- Islam MS, .et al. , J Agric Food Chem, 2016, Oct 10 PMID: 27632812
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GABAA α5 receptor agonist
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA?α1β3γ2, GABAA?α2β3γ2, GABAA?α3β3γ2, and GABAA?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS. -
COX-2 inhibitor
Gallic acid is a trihydroxybenzoic acid found in many plants as either the free acid or in the esterified form of gallotannins and ellagitannins. Gallic acid is an antioxidant which can inhibit both COX-2. - Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.
- Catharanthine sulfate is a vinblastine-type alkaloid precursor with antitumor activity. It inhibits AChR by ion channel blocking and desensitization.
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BACE1 inhibitor
BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively. -
COX-1 inhibitor
Catechin is a polyphenolic flavonoid which has been isolated from a variety of natural sources including tea leaves, grape seeds, and the wood and bark of trees such as acacia and mahogany. -
nAChR agonist
(±)-Epibatidine is a nicotinic agonist. (±)-Epibatidine is a neuronal nAChR agonist. -
BACE1 inhibitor
Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. -
muscarinic receptor inhibitor
Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1. -
acetylcholine receptor antagonist
Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93. -
Glucosylceramide synthase inhibitor
Eliglustat is a specific and potent inhibitor of glucosylceramide synthase. -
P2X3 and P2X2/3 receptor antagonist
A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. -
PKD inhibitor
CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). -
PKD inhibitor
kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 respectively). -
NMDA receptor antagonist
SDZ 220-581 is a competitive NMDA receptor antagonist (pKi = 7.7). -
COX inhibitor
(S)-(+)-Flurbiprofen is a non-selective Cox-1 and Cox-2 inhibitor.- Xing Jin, .et al. , Microchemical Journal, 2018, 143: 280-285
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γ-secretase inhibitor
BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.- Chao Liu, .et al. , Cell Death Differ, 2018, Apr; 25(4): 661-676 PMID: 29238071
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AChE inhibitor
Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM. -
COX inhibitor
Meclofenamate Sodium is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM. -
Benzodiazepine receptor agonist
Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity. -
GABAA antagonist
(+)-Bicuculline is a classical GABAA antagonist.- Maryam Adenike Salaudeen, .et al. , J Pharmacy and Drug Innovations, 2022, 3(4)
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P2X7 receptor antagonist
A-438079 HCl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 >> 10 uM). - Smilagenin (SMI) is a lipid-soluble small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases.
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muscarinic antagonist
Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic. -
amyloid β42 inhibitor
Ro 90-7501 is an inhibitor of amyloid β42 (Aβ42) fibril assembly; reduces Aβ42-induced toxicity (EC50 = 2 μM). - Methyllycaconitine citrate is a potent antagonist for α7-containing neuronal nicotinic receptors (Ki = 1.4 nM). Interacts with α4β2 and α6β2 receptors at concentrations > 40 nM.
- Phenazepam is a benzodiazepine agonist of the ??-aminobutyric acid A (GABAA)-benzodiazepine receptor chloride channel complex.
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NMDA receptor antagonist
(+)-MK 801 is a potent antagonist of NMDA with Ki value of 30.5nM. - Miglustat hydrochloride is an orally active α-glucosidase I and II and ceramide-specific glycosyltransferase inhibitor.
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GABA transport inhibitor
(S)-SNAP5114 is a selective GABA transport inhibitor, with IC50 values of 5 μM and 21 μM for hGAT-3 and rGAT-2, respectively. (S)-SNAP5114 is an anticonvulsant drug.
