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Results for "

alpha4beta2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Amyloid-β (2) Apoptosis (1) Bacterial (2) Calcium Channel (2) Caspase (1) Cholinesterase (ChE) (4) Dopamine Transporter (2) Endogenous Metabolite (1) Environmental Pollutants (1) ERK (2) GABA Receptor (3) Isotope-Labeled Compounds (10) nAChR (100) NF-κB (2) p38 MAPK (2) Potassium Channel (1) Reference Standards (12) Serotonin Transporter (1) Sodium Channel (2) STAT (1)
By Research Areas:	Cancer (13) Infection (2) Inflammation/Immunology (17) Metabolic Disease (6) Neurological Disease (94)
Click Chemistry:	Alkynes (1)

104

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Natural
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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10019

Varenicline 1 Publications Verification CP 526555	nAChR	Neurological Disease Inflammation/Immunology Cancer
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-10021

Varenicline Tartrate 1 Publications Verification CP 526555-18	nAChR ERK p38 MAPK	Others Neurological Disease Cancer
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-N0175

Cytisinicline 1 Publications Verification Cytisine; Sophorine; Baptitoxine	nAChR	Metabolic Disease Cancer
Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-14564A

GTS-21 dihydrochloride 10+ Cited Publications DMXB-A; DMBX-anabaseine	nAChR 5-HT Receptor	Inflammation/Immunology
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor *(α7-nAChR)* agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a *α4β2* (K_i=20 nM for humanα4β2) and 5-HT3A receptor (IC₅₀=3.1 μM) antagonist .

HY-B0942

Benzethonium chloride 1 Publications Verification	Environmental Pollutants nAChR Bacterial Apoptosis Caspase	Infection Neurological Disease Cancer
Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and *α4β2* neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo .

HY-107670

Dihydro-β-erythroidine hydrobromide 1 Publications Verification DHβE hydrobromide	nAChR	Neurological Disease
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC₅₀s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities .

HY-12152

PNU-120596 1 Publications Verification NSC 216666	nAChR	Neurological Disease Inflammation/Immunology
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) that can cross the blood-brain barrier, with an EC₅₀ of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research .

HY-A0009

Galanthamine hydrobromide Maximum Cited Publications 15 Publications Verification Galantamine hydrobromide	Cholinesterase (ChE) nAChR	Neurological Disease
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-B0379A

Adiphenine hydrochloride 3 Publications Verification	nAChR	Neurological Disease
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC₅₀s of 1.9, 1.8, 3.7, and 6.3 μM for α1, *α3β4, α4β2, and α4β4*, respectively. Adiphenine hydrochloride has anticonvulsant effects .

HY-14316A

Tebanicline dihydrochloride Ebanicline dihydrochloride; ABT-594 dihydrochloride	nAChR	Neurological Disease
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a K_i of 37 pM .

HY-10020

Varenicline Hydrochloride CP 526555 hydrochloride	nAChR	Neurological Disease Inflammation/Immunology Cancer
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-B1671

(+)-Kavain	GABA Receptor Sodium Channel Calcium Channel	Neurological Disease Metabolic Disease
(+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na ⁺ and Ca ²⁺ channels . (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-105670

PHA-543613	nAChR	Neurological Disease
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a K_i of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors . PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research .

HY-110160

Pozanicline dihydrochloride ABT-089 dihydrochloride	nAChR	Neurological Disease
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a K_i of 16.7 nM for binding to [ ³H]cytisine sites . Pozanicline is an *α4β2*-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a K_i of 17 nM while binding to α7 nAChR is insignificant .

HY-107675

Desformylflustrabromine hydrochloride Deformylflustrabromine hydrochloride; dFBr hydrochloride	nAChR	Neurological Disease
Desformylflustrabromine hydrochloride is a selective agonist of *α₄β₂* neuronal nicotinic acetylcholine receptor (nAChR) with a pEC₅₀ of 6.48.

HY-10019A

Varenicline dihydrochloride CP 526555 dihydrochloride	nAChR	Neurological Disease Inflammation/Immunology Cancer
Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-136146

SUVN-911	nAChR	Neurological Disease
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a K_i of 1.5 nM. SUVN-911 has antidepressant activity .

HY-P5189A

*His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA*	Endogenous Metabolite Cholinesterase (ChE)	Others
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .

HY-12766S

Bupropion morpholinol-d6	Isotope-Labeled Compounds nAChR Dopamine Transporter	Neurological Disease
Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .

HY-110121A

NS3861 1 Publications Verification	nAChR	Neurological Disease
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding K_i values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .

HY-13225B

Rivanicline hemioxalate 1 Publications Verification RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate	nAChR	Neurological Disease
Rivanicline (RJR-2403) hemioxalate is a neuronal nicotinic receptor agonist. Rivanicline hemioxalate is highly selective for the rat brain cortex nAChRs (K_i = 26 nM, EC₅₀ of 732 nM) and α4β2 subtype (K_i = 26 nM, EC₅₀ = 16 μM). Rivanicline hemioxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hemioxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .

HY-10063

Ispronicline TC-1734; ACD3480	nAChR	Neurological Disease
Ispronicline (TC-1734), an orally active, brain-selective *α4β2* nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (K_i=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .

HY-136207

TC-2559 difumarate	nAChR	Neurological Disease
TC-2559 idifumarate is a CNS-selective, orally active *α4β2* subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC₅₀=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC₅₀s in the range of 10-30 µM. Antinociceptive effect .

HY-110131

A 85380 hydrochloride	nAChR	Neurological Disease
A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .

HY-107686

5-Iodo-A-85380 dihydrochloride 5-I A-85380 dihydrochloride	nAChR	Neurological Disease
5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with K_ds of 12 and 14 pM,respectively .

HY-B0942R

Benzethonium chloride (Standard)	Reference Standards nAChR Bacterial	Neurological Disease
Benzethonium (chloride) (Standard) is the analytical standard of Benzethonium (chloride). This product is intended for research and analytical applications. Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes.

HY-N0175R

Cytisinicline (Standard) Cytisine (Standard); Sophorine (Standard); Baptitoxine (Standard)	Reference Standards nAChR	Metabolic Disease Cancer
Cytisinicline (Standard) is the analytical standard of Cytisinicline. This product is intended for research and analytical applications. Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-108069

Iptakalim hydrochloride	Potassium Channel nAChR	Neurological Disease
Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (K_ATP) opener, as well as an α₄β₂-containing nicotinic acetylcholine receptor (nAChR) antagonist .

HY-107684

3-Bromocytisine 3-Br-cytisine	nAChR	Neurological Disease
3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC₅₀s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC₅₀s are 8 and 50 nM, respectively .

HY-12766

Bupropion morpholinol	Dopamine Transporter nAChR	Neurological Disease
Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .

HY-115766

Anabaseine	nAChR	Neurological Disease
Anabaseine, a brain-penetrant occurring alkaloid toxin, is potent agonist of multiple nicotinic acetylcholine receptors (AChRs). Anabaseine stimulates the neuromuscular α12β1γδ or α12β1γɛ and α7 AChRs. Anabaseine is also a weak partial agonist at α4β2 nAChRs .

HY-135483A

AR-R17779 hydrochloride	nAChR	Neurological Disease
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with K_is of 92 and 16000 nM for α7 and *α4β2* subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .

HY-N2326

(±)-Anatoxin A fumarate	nAChR	Neurological Disease Metabolic Disease
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits K_i values of 1.25 nM and 1.84 μM for binding to α4β2- and α7-type nicotinic receptors in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ ³H]-dopamine release from rat striatal synaptosomes (EC₅₀=134 nM). (±)-Anatoxin A fumarate has toxic effect on fish .

HY-115764

nAChR agonist 2	nAChR	Neurological Disease
nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (K_d=26 nM) .

HY-139581

Ropanicant SUVN-911 free base	nAChR	Neurological Disease
Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active *neuronal nicotinic acetylcholine α4β2* receptor** antagonist for the research of depression .

HY-110241

Dianicline dihydrochloride	nAChR	Neurological Disease
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .

HY-138879A

(Rac)-CP-601927 hydrochloride	nAChR	Neurological Disease
(Rac)-CP-601927 hydrochloride is the racemate of CP-601927. CP-601927 is a nAChR agonist with Ki values 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively .

HY-138953

Epiboxidine	nAChR	Neurological Disease
Epiboxidine is a potent and selective neural nAChR agonist with K_is of 0.46 nM and 1.2 nM for rat and *human α4β2* nAChRs**, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .

HY-110121

NS3861 fumarate 1 Publications Verification	nAChR	Neurological Disease
NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding K_i values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .

HY-137231B

(S)-UFR2709 hydrochloride	nAChR	Neurological Disease
(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist?and displays higher affinity for α₄β₂ nAChRs than for α₇ nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction .

HY-13225A

Rivanicline RJR-2403; (E)-Metanicotine	nAChR	Neurological Disease
Rivanicline (RJR-2403) is a neuronal nicotinic receptor agonist. Rivanicline is highly selective for the rat brain cortex nAChRs (K_i = 26 nM, EC₅₀ of 732 nM) and α4β2 subtype (K_i = 26 nM, EC₅₀ = 16 μM). Rivanicline can significantly restore the learning impairment and cognitive dysfunction. Rivanicline can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .

HY-105670B

PHA-543613 dihydrochloride	nAChR	Neurological Disease
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a K_i value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors . PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research .

HY-N1064

Xanthoplanine	nAChR	Neurological Disease
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC₅₀ ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC₅₀ values of 9 μM (alpha7) and 5 μM (alpha4beta2) .

HY-169870

Dexmecamylamine (+)-Mecamylamine; TC-5214	nAChR	Neurological Disease
Dexmecamylamine ((+)-Mecamylamine) is the antagonist for nicotinic acetylcholine receptor (nAChR), that antagonises the α3β4/α4β2/α7/α1β1γδ receptor with IC₅₀ of micromolare levels. Dexmecamylamine exhibits anxiolytic and antidepressant-like activities .

HY-14564

GTS-21	nAChR 5-HT Receptor	Inflammation/Immunology
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor *(α7-nAChR)* agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a *α4β2* (K_i=20 nM for humanα4β2) and 5-HT3A receptor (IC₅₀=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research .

HY-10021R

Varenicline Tartrate (Standard) CP 526555-18 (Standard)	Reference Standards nAChR ERK p38 MAPK	Others Neurological Disease
Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-115766S

Anabaseine-d4	Isotope-Labeled Compounds nAChR	Neurological Disease
Anabaseine-d₄ is the deuterium labeled Anabaseine (HY-115766). Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .

HY-14319B

Sazetidine A dihydrochloride	nAChR	Neurological Disease
Sazetidine A dihydrochloride is a potent ligand for the α4β2 nAChR, with high binding affinity and selectivity for this subtype. Sazetidine A dihydrochloride exhibits favorable pharmacological properties and may contribute to research targeting nicotinic receptor-related diseases. Sazetidine A dihydrochloride has been mentioned in studies investigating the binding affinity of various analogs, highlighting its importance in understanding the nAChR ligand subtype selectivity .

HY-19918A

Anatabine dicitrate 1 Publications Verification	NF-κB Amyloid-β nAChR	Neurological Disease Inflammation/Immunology
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .

HY-13225

Rivanicline oxalate RJR-2403 oxalate; (E)-Metanicotine oxalate	nAChR	Neurological Disease
Rivanicline (RJR-2403) oxalate is a neuronal nicotinic receptor agonist. Rivanicline oxalate is highly selective for the rat brain cortex nAChRs (K_i = 26 nM, EC₅₀ of 732 nM) and α4β2 subtype (K_i = 26 nM, EC₅₀ = 16 μM). Rivanicline oxalate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline oxalate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease) .

Cat. No.	Product Name	Target	Research Area

HY-P5189A

*His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA*	Endogenous Metabolite Cholinesterase (ChE)	Others
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0175

Cytisinicline 1 Publications Verification Cytisine; Sophorine; Baptitoxine	Alkaloids Classification of Application Fields Leguminosae Pyridine Alkaloids Metabolic Disease Plants Thermopsis lanceolala R.Br. Disease Research Fields Source Classification	nAChR
Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-107670

Dihydro-β-erythroidine hydrobromide 1 Publications Verification DHβE hydrobromide	Alkaloids Piperidine Alkaloids Leguminosae Plants Erythrina Source Classification	nAChR
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC₅₀s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities .

HY-A0009

Galanthamine hydrobromide Maximum Cited Publications 15 Publications Verification Galantamine hydrobromide	Alkaloids Other Alkaloids Plants Amaryllidaceae	Cholinesterase (ChE) nAChR
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-B1671

(+)-Kavain	Structural Classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants Source Classification	GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na ⁺ and Ca ²⁺ channels . (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-N0175R

Cytisinicline (Standard) Cytisine (Standard); Sophorine (Standard); Baptitoxine (Standard)	Alkaloids Structural Classification Leguminosae Pyridine Alkaloids Plants Thermopsis lanceolala R.Br. Source Classification	Reference Standards nAChR
Cytisinicline (Standard) is the analytical standard of Cytisinicline. This product is intended for research and analytical applications. Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-N1064

Xanthoplanine	Alkaloids Monophenols other families Phenols Plants Isoquinoline Alkaloids Source Classification	nAChR
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC₅₀ ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC₅₀ values of 9 μM (alpha7) and 5 μM (alpha4beta2) .

HY-A0009R

Galanthamine hydrobromide (Standard) Galantamine hydrobromide (Standard)	Structural Classification Alkaloids Other Alkaloids Plants Amaryllidaceae Source Classification	nAChR Cholinesterase (ChE) Reference Standards
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-N10132

Microgrewiapine A	Malvaceae Alkaloids Microcos paniculata L. Other Alkaloids Plants Source Classification	nAChR
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC₅₀ of 6.8 μM .

HY-13225E

(E/Z)-Rivanicline (E/Z)-RJR-2403; (E/Z)-Metanicotine	Alkaloids Duboisia hopwoodii (F.Muell.) F.Muell. Quinoline Alkaloids Solanaceae Plants Source Classification	nAChR
(E/Z)-Rivanicline ((E/Z)-RJR-2403, (E/Z)-Metanicotine) is the E/Z mixture of Rivanicline (HY-13225A). Rivanicline is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype, K_i is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .

HY-B1671R

(+)-Kavain (Standard)	Structural Classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants Source Classification	Reference Standards GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

Cat. No.	Product Name	Chemical Structure

HY-12766S

Bupropion morpholinol-d6
Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .

HY-115766S

Anabaseine-d4
Anabaseine-d₄ is the deuterium labeled Anabaseine (HY-115766). Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .

HY-B0942S

Benzethonium-d7 chloride
Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.

HY-10019S2

Varenicline-13C15N

Varenicline- ¹³C ¹⁵N (CP 526555- ¹³C ¹⁵N) is ¹³C and ¹⁵N labeled Varenicline. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-10019S1

Varenicline-15N,13C,d2

Varenicline- ¹⁵N, ¹³C,d₂ is ¹⁵N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-10020S

Varenicline-15N3 hydrochloride

Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the ¹⁵N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-W743727

Cytisine-d4
Cytisine-d₄ is the deuterium labeled Cytisinicline (HY-N0175). Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-10019S

Varenicline-d4

Varenicline-d₄ is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .

HY-A0009S

Galanthamine-d3 hydrobromide

Galanthamine-d₃ (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-10019AS1

Varenicline-d4 hydrochloride

Varenicline-d₄ hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .

Cat. No.	Product Name		Classification

HY-14318

Altinicline SIB-1508Y free base		Alkynes
Altinicline (SIB-1508Y free base) is a selective *α4β2* nicotinic acetylcholine receptor (nAChR) agonist, with no activity against α7 or *α1β1γδ* nAChRs and only extremely low activity against *α3β4* nAChRs. Altinicline reverses escape deficits and increases avoidance responses. Altinicline is applicable to research related to depression .

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