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Tacrine

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) ATP Citrate Lyase (1) CDK (2) Cholinesterase (ChE) (16) Free Fatty Acid Receptor (1) GABA Receptor (1) iGluR (3) Isotope-Labeled Compounds (1) NO Synthase (1) Potassium Channel (4) Reactive Oxygen Species (ROS) (1) Reference Standards (5) Sodium Channel (4) Tyrosinase (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Endocrinology (1) Metabolic Disease (5) Neurological Disease (14)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1488

Tacrine hydrochloride Maximum Cited Publications 8 Publications Verification	Cholinesterase (ChE) iGluR	Neurological Disease
Tacrine hydrochloride is a potent brain-penetrant inhibitor of both AChE and BChE, with IC₅₀s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC₅₀ of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease .

HY-111338

*Tacrine* Maximum Cited Publications 8 Publications Verification	Cholinesterase (ChE)	Neurological Disease
Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC₅₀ = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .

HY-B2244

Tacrine hydrochloride hydrate Maximum Cited Publications 8 Publications Verification	Cholinesterase (ChE)	Neurological Disease
Tacrine hydrochloride (hydrate) is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC₅₀s of 31 nM and 25.6 nM, respectively.

HY-W027553

Ipidacrine NIK-247 free base; Amiridine free base	Cholinesterase (ChE) Potassium Channel Sodium Channel	Neurological Disease Metabolic Disease
Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K ⁺ and Na ⁺-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .

HY-120970

*Bis(7)-tacrine* dihydrochloride**	Cholinesterase (ChE) GABA Receptor iGluR	Neurological Disease
Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABA_Areceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .

HY-151436

ZLMT-12	CDK Cholinesterase (ChE) Apoptosis	Cancer
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC₅₀ values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC₅₀=19.023 μM) and BChE (IC₅₀=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .

HY-B1488R

Tacrine hydrochloride (Standard)	Reference Standards Cholinesterase (ChE) iGluR	Neurological Disease
Tacrine (hydrochloride) (Standard) is the analytical standard of Tacrine (hydrochloride). This product is intended for research and analytical applications. Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease .

HY-111338R

Tacrine (Standard)	Cholinesterase (ChE) Reference Standards	Neurological Disease
Tacrine (Standard) is the analytical standard of Tacrine. This product is intended for research and analytical applications. Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .

HY-B2244R

Tacrine hydrochloride hydrate (Standard)	Reference Standards Cholinesterase (ChE)	Neurological Disease
Tacrine (hydrochloride) (hydrate) (Standard) is the analytical standard of Tacrine (hydrochloride) (hydrate). This product is intended for research and analytical applications. Tacrine hydrochloride (hydrate) is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC₅₀s of 31 nM and 25.6 nM, respectively.

HY-W027553R

Ipidacrine (Standard) NIK-247 free base (Standard); Amiridine free base (Standard)	Reference Standards Cholinesterase (ChE) Potassium Channel Sodium Channel	Neurological Disease Metabolic Disease
Ipidacrine (Standard) is the analytical reference standard of Ipidacrine. This product is used for research and analytical applications. Ipidacrine is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K ⁺ and Na ⁺-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .

HY-143291

AChE-IN-9	Cholinesterase (ChE)	Neurological Disease
AChE-IN-9 is a Tacrine (HY-111338) glycoconjugate tethered with acetylated β-Glucose. AChE-IN-9 is also an AChE inhibitor with an IC₅₀ value of 0.4 μM, with lower hepatotoxicity on healthy cells. Tacrine is used in Alzheimer's research .

HY-P1123R

MEDICA16 (Standard)	Reference Standards ATP Citrate Lyase Free Fatty Acid Receptor	Metabolic Disease
Tacrine (hydrochloride) (Standard) is the analytical standard of Tacrine (hydrochloride). This product is intended for research and analytical applications. Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease .

HY-135006A

Octahydroaminoacridine	Cholinesterase (ChE)	Neurological Disease
Octahydroaminoacridine, a Tacrine analogue, is an acetylcholinesterse (AChE) and butyrylcholinesterase (BChE) inhibitor. Octahydroaminoacridine can be used for Alzheimer's disease (AD) research .

HY-135006

Octahydroaminoacridine succinate	Cholinesterase (ChE)	Neurological Disease
Octahydroaminoacridine succinate, a Tacrine analogue, is an acetylcholinesterse (AChE) and butyrylcholinesterase (BChE) inhibitor. Octahydroaminoacridine succinate can be used for Alzheimer's disease (AD) research .

HY-121174

Alaternin Catharticin	NO Synthase CDK Tyrosinase Reactive Oxygen Species (ROS)	Metabolic Disease
Alaternin (Catharticin) is an anthraquinone compound with antioxidant and hepatoprotective activities. Alaternin has an inhibitory activity against hydroxyl radicals generated in a cell-free chemical system (FeSO₄/H₂O₂) with an IC₅₀ value of 3.05 μM. Alaternin exhibits hepatoprotective activity against Tacrine (HY-111338)-induced toxicity in human hepatic HepG2 cells with an EC₅₀ value of 4.02 μM .

HY-W027553S1

Ipidacrine-d9 NIK-247-d9 free base	Isotope-Labeled Compounds Cholinesterase (ChE) Potassium Channel Sodium Channel	Metabolic Disease
Ipidacrine-d₉ (NIK-247-d₉ (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .

HY-182254

AChE/BChE-IN-35	Cholinesterase (ChE)	Neurological Disease
AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC₅₀ of 123.66 nM, human AChE IC₅₀ of 122.34 nM, and equine BChE IC₅₀ of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease .

HY-19689

Ipidacrine hydrochloride NIK-247; Amiridine	Cholinesterase (ChE) Potassium Channel Sodium Channel	Cardiovascular Disease Neurological Disease Endocrinology
Ipidacrine (NIK-247; Amiridine) hydrochloride is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine hydrochloride has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine hydrochloride is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine hydrochloride is effective in various amnesia models, improves erectile function and inhibits K ⁺ and Na ⁺-channels in the neuronal membrane in diabetic rats. Ipidacrine hydrochloride is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .

Cat. No.	Product Name

HY-L236

Amine Fragment Library	19,532 compounds
Fragment-based drug discovery (FBDD) offers a strategic advantage by categorizing fragment hits according to their functional groups. This approach facilitates both the further optimization of these hits and the rational design of larger compounds through fragment combination. The amine functional group plays a vital role in drug development, as evidenced by its presence in many marketed drugs like Galantamine, Tacrine, and Rivastigmine. It is instrumental in enhancing solubility, improving bioavailability, and ensuring shelf-life stability—all critical factors for drug efficacy. MCE offers a collection of 19,532 amine fragments for drug discovery. All of these compounds adhere to the Rule of Three (RO3) criteria for drug-likeness, which MCE offers a collection of 19,532 amine fragments for drug discovery, all of which stipulates a molecular weight ≤ 300 Da, ≤ 3 hydrogen bond donors, ≤ 3 hydrogen bond acceptors, and a cLogP ≤ 3.

Amine Fragment Library

19,532 compounds

Fragment-based drug discovery (FBDD) offers a strategic advantage by categorizing fragment hits according to their functional groups. This approach facilitates both the further optimization of these hits and the rational design of larger compounds through fragment combination. The amine functional group plays a vital role in drug development, as evidenced by its presence in many marketed drugs like Galantamine, Tacrine, and Rivastigmine. It is instrumental in enhancing solubility, improving bioavailability, and ensuring shelf-life stability—all critical factors for drug efficacy.

MCE offers a collection of 19,532 amine fragments for drug discovery. All of these compounds adhere to the Rule of Three (RO3) criteria for drug-likeness, which MCE offers a collection of 19,532 amine fragments for drug discovery, all of which stipulates a molecular weight ≤ 300 Da, ≤ 3 hydrogen bond donors, ≤ 3 hydrogen bond acceptors, and a cLogP ≤ 3.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-121174

Alaternin Catharticin	Flavonoids Plants Rhamnaceae Rhamnus saxatilis X. H. Song Source Classification	NO Synthase CDK Tyrosinase Reactive Oxygen Species (ROS)
Alaternin (Catharticin) is an anthraquinone compound with antioxidant and hepatoprotective activities. Alaternin has an inhibitory activity against hydroxyl radicals generated in a cell-free chemical system (FeSO₄/H₂O₂) with an IC₅₀ value of 3.05 μM. Alaternin exhibits hepatoprotective activity against Tacrine (HY-111338)-induced toxicity in human hepatic HepG2 cells with an EC₅₀ value of 4.02 μM .

Cat. No.	Product Name	Chemical Structure

HY-W027553S1

Ipidacrine-d9
Ipidacrine-d₉ (NIK-247-d₉ (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .

Ipidacrine-d9

Ipidacrine-d₉ (NIK-247-d₉ (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .

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