AChE Acetylcholinesterase Acetylcholinesterase (AChE or acetylhydrolase) is a hydrolase that hydrolyzes the neurotransmitter acetylcholine. AChE is found at mainly neuromuscular junctions and cholinergic brain synapses, where its activity serves to terminate synaptic transmission. It belongs tocarboxylesterase family of enzymes. It is the primary target of inhibition by organophosphorus compounds such as nerve agents and pesticides. AChE has a very high catalytic activity - each molecule of AChE degrades about 25000 molecules ofacetylcholine (ACh) per second, approaching the limit allowed by diffusion of the substrate. ACh is released from the nerve into the synaptic cleft and binds to ACh receptors on the post-synaptic membrane, relaying the signal from the nerve. AChE, also located on the post-synaptic membrane, terminates the signal transmission by hydrolyzing ACh. The liberated choline is taken up again by the pre-synaptic nerve and ACh is synthetized by combining with acetyl-CoA through the action of choline acetyltransferase. www.MedChemExpress.com 1 AChE Inhibitors & Activators (+)-Phenserine (-)-Corynoxidine Cat. No.: HY-16009 Cat. No.: HY-N7010 (+)-Phenserine is a novel selective cholinesterase (-)-Corynoxidine is an acetylcholinesterase noncompetitive inhibitor with an IC50 of 45.3 μM. inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa. (-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. Purity: 98.09% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg (-)-Huperzine A (R)-Rivastigmine D6 tartrate (Huperzine A) Cat. No.: HY-17387 Cat. No.: HY-11017AS (-)-Huperzine A (Huperzine A) is an alkaloid (R)-Rivastigmine D6 tartrate is the deuterium isolated from a Chinese club moss, with labeled (R)-Rivastigmine, which is an neuroprotective activity. cholinesterase inhibitor. Purity: ≥98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg Size: 1 mg, 5 mg (±)-Huperzine A 1-Naphthyl acetate Cat. No.: HY-17388 Cat. No.: HY-W016188 (±)-Huperzine A, an active Lycopodium alkaloid 1-Naphthyl acetate is an attractive chromogenic extracted from traditional Chinese herb, is a substrate for the detection of erythrocyte potent, selective and reversible acetylcholinesterase (AChE) activity. 1-Naphthyl acetylcholinesterase (AChE) inhibitor and has been acetate has the potential to detect widely used in China for the treatment of organophosphorus pesticide (OP) poisoning. Alzheimer's disease (AD). Purity: ≥98.0% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 500 mg 4-Methylbenzylidene camphor Acephate (4-MBC; Enzacamene) Cat. No.: HY-17587 Cat. No.: HY-B0841 4-Methylbenzylidene camphor(4-MBC; Enzacamene)is Acephate is an anticholinesterase insecticide that an organic camphor derivative that is used in the produces cholinotoxicity. Acephate displays weak cosmetic industry for its ability to protect the inhibition of rat AChE but potently inhibits skin against UV, specifically UV B radiation. cockroach AChE. Purity: 99.86% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 50 mg, 100 mg Acetylshikonin AChE/BChE-IN-1 Cat. No.: HY-N2181 Cat. No.: HY-131971 Acetylshikonin, derived from the root of AChE/BChE-IN-1 is a potent and brain-penetrant Lithospermum erythrorhizon, has anti-cancer and dual inhibitor of Acetylcholinesterase and antiinflammation activity. Acetylshikonin is a Butyrylcholinesterase, with IC50s of 1.06 and 7.3 non-selective cytochrome P450 inhibitor nM for hAChE and hBChE, respectively. against all P450s (IC50 values range from 1.4-4.0 AChE/BChE-IN-1 also has antioxidant activity. μM). Purity: 98.06% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Acotiamide monohydrochloride trihydrate Ajmalicine Cat. No.: HY-B2155 (Raubasine) Cat. No.: HY-N1919 Acotiamide monohydrochloride trihydrate is an Ajmalicine (Raubasine) is found in herbs of orally active and first-in-class gastroprokinetic Catharanthus roseus, is an antihypertensive drug agent for the treatment of functional dyspepsia. used in the treatment of high blood pressure, decreases peripheral resistance and blood pressure. Purity: 99.28% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg Aldicarb sulfone Azamethiphos Cat. No.: HY-17530 Cat. No.: HY-114899 Aldicarb sulfone(Temik sulfone) is a carbamate Azamethiphos is an organophosphate insecticide and insecticide; is a cholinesterase inhibitor which a neurotoxic agent, causing acetylcholinesterase prevents the breakdown of acetylcholine in the (AChE) inhibition. synapse. Purity: 99.24% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg Benactyzine hydrochloride BuChE-IN-TM-10 Cat. No.: HY-B1542A (TM-10) Cat. No.: HY-114320 Benactyzine hydrochloride is a BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BChE) inhibitor with a Ki butyrylcholinesterase (BuChE) inhibitor, with an of 0.010 mM. IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Purity: 99.69% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg Chlorpyrifos Chlorpyrifos-oxon Cat. No.: HY-B0815 Cat. No.: HY-136610 Chlorpyrifos is an organophosphate insecticide Chlorpyrifos-oxon, an active metabolite of that is classified as a phosphorothionate. The Chlorpyrifos, is a potent phosphorylating agent oxon metabolite of Chlorpyrifos is an inhibitor of that potently inhibits AChE. Chlorpyrifos-oxon acetylcholinesterase (AChE), affecting can induce cross-linking between subunits of neurological function in insects, humans, and tubulin and disrupt microtubule function. other animals. Purity: ≥98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 50 mg, 100 mg Size: 1 mg, 5 mg Corydaline Corynoline ((+)-Corydaline; Corydalin) Cat. No.: HY-N0923 Cat. No.: HY-N0826 Corydaline ((+)-Corydaline), an isoquinoline Corynoline, isolated from Corydalis incise alkaloid isolated from Corydalis yanhusuo, is an (Papaveraceae), is a reversible and noncompetitive AChE inhibitor with an IC50 of 226 µM. Corydaline acetylcholinesterase (AChE) inhibitor with an is a μ-opioid receptor (Ki of 1.23 µM) agonist and IC50 of 30.6 μM. Corynoline exhibits inhibits enterovirus 71 (EV71) replication (IC50 anti-inflammatory activity by activating Nrf2. of 25.23 µM). Purity: 96.17% Purity: 98.06% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 20 mg www.MedChemExpress.com 3 Coumaran Cyanidin-3-O-galactoside chloride (2,3-Dihydrobenzofuran) Cat. No.: HY-75247 (Ideain chloride) Cat. No.: HY-N4142 Coumaran (2,3-Dihydrobenzofuran) is an Cyanidin-3-O-galactoside chloride (Ideain acetylcholinesterase (AChE) inhibitor isolated chloride) is a component from extract peel of from leaves of L. camara. Coumaran can be used hawthorn fruit (EPHF) with the value of 179.4 as a biopesticide. mg/g. EPHF exhibits strong AChE inhibitory activity. Purity: 99.69% Purity: 99.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg Size: 1 mg, 5 mg Dehydronuciferine Demecarium Bromide Cat. No.: HY-N4261 (BC-48) Cat. No.: HY-B1626A Dehydronuciferine is isolated from the leaves of Demecarium Bromide (BC-48) is a potent Nelumbo nucifera Gaertn, a acetylcholinesterase cholinesterase inhibitor, with an apparent affinity (AChE) inhibitor with an IC50 of 25 μg/mL. (Kiapp) of 0.15 μM. Demecarium Bromide (BC-48) is used as a glaucoma agent. Purity: ≥99.0% Purity: ≥95.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Dihydro Donepezil Dihydrowithaferin A (Dihydro E2020) Cat. No.: HY-131252 (2,3-Dihydrowithaferin A) Cat. No.: HY-N5120 Dihydro Donepezil (Dihydro E2020) is a metabolite Dihydrowithaferin A (2, 3-dihydrowithaferin A) is of Donepezil. Donepezil is a specific and potent a withanolide isolated from Withania AChE inhibitor with IC50s of 8.12 nM and 11.6 nM somnifera. Dihydrowithaferin A is active for bAChE and hAChE, respectively. against acetylcholinesterase (AChE). Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg, 5 mg Donepezil Donepezil Hydrochloride (E2020 free base) Cat. No.: HY-14566 (E2020) Cat. No.: HY-B0034 Donepezil (E2020 free base) is a specific and Donepezil (Hydrochloride) (E-2020) is a potent AChE inhibitor with IC50s of 8.12 nM and noncompetitive acetylcholinesterase inhibitor, 11.6 nM for bovine AChE and human AChE, which can readily cross the blood brain barrier respectively. and increases the concentration of cortical acetylcholine. Purity: 99.96% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10