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Results for "

α4β2 nAChR partial agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	nAChR (24) ERK (2) Isotope-Labeled Compounds (5) p38 MAPK (2)
By Research Areas:	Cancer (12) Inflammation/Immunology (10) Metabolic Disease (2) Neurological Disease (21)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: nAChR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10019

Varenicline 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 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-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-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 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-10021

Varenicline Tartrate 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-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-107680

3-Pyr-Cytisine 3-Pyr-Cyt	nAChR	Neurological Disease
3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak **α4β2 nAChR** partial agonist that has been studied as an antidepressant .

HY-110142

Thermopsidine CC4	nAChR	Neurological Disease
Thermopsidine (CC4) is a selective partial agonist at α4β2/α6β2 nAChR with EC₅₀ values of 2.2 μM target α4β2 .

HY-10021R

Varenicline (Tartrate) (Standard)	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-10019R

Varenicline (Standard) CP 526555 (Standard)	nAChR	Neurological Disease Inflammation/Immunology Cancer
Varenicline (Standard) is the analytical standard of Varenicline. 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[1][2][3][4][5].

HY-10019AR

Varenicline dihydrochloride (Standard) CP 526555 dihydrochloride (Standard)	nAChR	Neurological Disease Inflammation/Immunology Cancer
Varenicline (dihydrochloride) (Standard) is the analytical standard of Varenicline (dihydrochloride). This product is intended for research and analytical applications. 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 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[1][2][3][4][5].

HY-10020R

Varenicline Hydrochloride (Standard) CP 526555 hydrochloride (Standard)	nAChR	Neurological Disease Inflammation/Immunology Cancer
Varenicline (Hydrochloride) (Standard) is the analytical standard of Varenicline (Hydrochloride). 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[1][2][3][4][5].

HY-107671

DMAB-anabaseine dihydrochloride	nAChR	Neurological Disease
DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an **α4β2 nAChR** antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects .

HY-10019S2

Varenicline-13C15N CP 526555-¹³C_,¹⁵N	Isotope-Labeled Compounds nAChR	Neurological Disease Inflammation/Immunology Cancer
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 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-10019S1

Varenicline-15N,13C,d2 CP 526555-15N,13C,d2	nAChR Isotope-Labeled Compounds	Neurological Disease Inflammation/Immunology Cancer
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 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-10020S

Varenicline-15N3 hydrochloride CP 526555-¹⁵N₃ Hydrochloride	nAChR Isotope-Labeled Compounds	Neurological Disease Inflammation/Immunology Cancer
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-115766

Anabaseine	nAChR	Neurological Disease
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-N0175R

Cytisinicline (Standard)	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-138879

CP-601927	nAChR	Neurological Disease
CP-601927 is a selective *α4β2* nicotinic acetylcholine receptor (nAChR) partial agonist (K_i=1.2 nM; EC₅₀=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .

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-10019S

Varenicline-d4 CP 526555-d₄	Isotope-Labeled Compounds nAChR	Neurological Disease
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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].

HY-10019AS1

Varenicline-d4 hydrochloride	Isotope-Labeled Compounds nAChR	Inflammation/Immunology
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 .

HY-14565

Pozanicline ABT-089	nAChR	Neurological Disease
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (K_i=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (K_i, rat) for Pozanicline to [ ³H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .

HY-138879B

CP-601932 (1S,5R)-CP-601927	nAChR	Neurological Disease
CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (K_i=21 nM; EC₅₀=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (K_i=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0175

Cytisinicline 1 Publications Verification Cytisine; Sophorine; Baptitoxine	Alkaloids Structural Classification Classification of Application Fields Leguminosae Source classification Pyridine Alkaloids Metabolic Disease Plants Thermopsis lanceolala R.Br. Disease Research Fields	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-N0175R

Cytisinicline (Standard)	Alkaloids Structural Classification Leguminosae Source classification Pyridine Alkaloids Plants Thermopsis lanceolala R.Br.	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 .

Cat. No.	Product Name	Chemical Structure

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 .

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 .

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 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 .

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 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-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 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 .

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 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-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 .

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-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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].

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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].

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