Search Result
Results for "
α3β4
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P1264
-
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nAChR
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Neurological Disease
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α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
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- HY-A0106
-
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(-)-Tetramisole
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nAChR
Parasite
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Infection
Inflammation/Immunology
Cancer
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Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
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- HY-12152
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NSC 216666
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nAChR
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-A0009
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Galantamine hydrobromide
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Cholinesterase (ChE)
nAChR
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Neurological Disease
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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) .
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- HY-B0379A
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nAChR
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Neurological Disease
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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 .
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- HY-135783
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AT 1001
1 Publications Verification
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nAChR
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
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- HY-147428
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MM-110; (±)-18-Methoxycoronaridine
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nAChR
Parasite
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Infection
Neurological Disease
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Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse . Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis .
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- HY-105670
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nAChR
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Neurological Disease
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PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki 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 .
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- HY-110121A
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NS3861
1 Publications Verification
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nAChR
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Neurological Disease
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NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
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- HY-10063
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TC-1734; ACD3480
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nAChR
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Neurological Disease
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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 (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
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- HY-136207
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nAChR
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Neurological Disease
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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 .
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- HY-171746
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4,5,6,7-Tetrafluoro-L-tryptophan
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nAChR
|
Neurological Disease
|
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F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a ligand targeting the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). F4-Trp is promising for research of neurotransmission, addiction, and related diseases, such as neurological diseases .
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- HY-19411
-
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nAChR
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Neurological Disease
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SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus .
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- HY-110121
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nAChR
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Neurological Disease
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NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
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- HY-138879A
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nAChR
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Neurological Disease
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(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 .
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- HY-105670B
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nAChR
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Neurological Disease
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PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki 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 .
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- HY-114791
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nAChR
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Neurological Disease
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Lobelanidine is an antagonist for nicotinic acetylcholine receptor (nAChR), which inhibits α7 nAChR response and α3β2/α3β4 nAChR responses, with IC50 of 2.8 and 8.2 μM .
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- HY-168824
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nAChR
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Neurological Disease
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Cypenamine hydrochloride is an antidepressant agent. Cypenamine binds to the human nAchR subtypes, α2β4, α3β4 and α4β4, with Ki values of 4.65 μM, 2.69 and 4.11 μM, respectively .
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- HY-169870
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(+)-Mecamylamine; TC-5214
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nAChR
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Neurological Disease
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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 .
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- HY-138953
-
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nAChR
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Neurological Disease
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Epiboxidine is a potent and selective neural nAChR agonist with Kis 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 .
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- HY-A0009R
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Galantamine hydrobromide (Standard)
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nAChR
Cholinesterase (ChE)
Reference Standards
|
Neurological Disease
|
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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) .
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- HY-138879B
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(1S,5R)-CP-601927
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nAChR
|
Neurological Disease
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CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=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 .
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- HY-171807
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nAChR
STAT
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Neurological Disease
Inflammation/Immunology
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TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .
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- HY-107679
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- HY-N12511
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nAChR
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Neurological Disease
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Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity .
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- HY-N10132
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nAChR
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Infection
Neurological Disease
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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 .
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- HY-121141
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nAChR
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Neurological Disease
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Adiphenine 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 has anticonvulsant effects .
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- HY-105670A
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nAChR
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Neurological Disease
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PHA-543613 hydrochloride is an oral or active α7 nAChR agonist with brain permeability, For α3β4, α1β1γδ, α4β2 and 5-HT3 receptors selective. PHA-543613 hydrochloride affects sensory gating and memory in an in vivo model of schizophrenia .
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- HY-A0106R
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(-)-Tetramisole (Standard)
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Reference Standards
nAChR
Parasite
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Infection
Inflammation/Immunology
Cancer
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Levamisole (Standard) is the analytical standard of Levamisole. This product is intended for research and analytical applications. Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
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- HY-10019S
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CP 526555-d4
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Isotope-Labeled Compounds
nAChR
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Neurological Disease
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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 .
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- HY-A0009S
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Galantamine-d3 hydrobromide
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Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
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Neurological Disease
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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) .
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- HY-B0379AR
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Reference Standards
nAChR
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Neurological Disease
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Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. 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 .
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- HY-10019AS1
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Isotope-Labeled Compounds
nAChR
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Inflammation/Immunology
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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 .
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- HY-N11477
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Glycosidase
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Metabolic Disease
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(2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid is a saponin that can be isolated from Rubus ellipticus var. obcordatus. (2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid inhibits α-Glucosidase with an IC50 of 1.68 mM .
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- HY-W680961
-
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nAChR
|
Neurological Disease
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Hydrohydrastinine is a selective α4β2 nicotinic acetylcholine receptor antagonist with an IC50 of 2.6 μM and a Ki of 17 μM. Hydrohydrastinine exhibits weak activity at α4β4 and α3β4 nicotinic acetylcholine receptors. Hydrohydrastinine can be used for the research of depression .
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- HY-14318
-
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SIB-1508Y free base
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nAChR
|
Neurological Disease
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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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- HY-138953A
-
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nAChR
|
Neurological Disease
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Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .
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- HY-105670R
-
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Reference Standards
nAChR
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Neurological Disease
|
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PHA-543613 (Standard) is the analytical standard of PHA-543613 (HY-105670). This product is intended for research and analytical applications. PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki 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 .
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- HY-46286
-
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N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide
|
5-HT Receptor
nAChR
GABA Receptor
Glycine Receptor (GlyR)
|
Neurological Disease
|
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TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel (ZAC) antagonist. TTFB inhibits Zn 2+- and H +-induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
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- HY-182010
-
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nAChR
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Neurological Disease
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nAChR antagonist 3 is a selective α7 nAChR antagonist with an IC50 of 0.86 μM. nAChR antagonist 3 exerts a protective effect against paraoxon-induced toxicity. nAChR antagonist 3 can be used for the research of organophosphate poisoning .
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- HY-182707
-
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nAChR
Interleukin Related
TNF Receptor
NF-κB
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Neurological Disease
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JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease .
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- HY-183666
-
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nAChR
Serotonin Transporter
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Neurological Disease
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NS3956 is a blood-brain barrier-permeable human α4β2-nicotinic acetylcholine receptor (nAChR) agonist (Ki = 0.36 nM). NS3956 induces dopamine release, produces analgesic effects, modulates rotational behavior in 6-OHDA-lesioned rats, and potentiates the effects of SSRI/SNRI in the forced swim test in mice. NS3956 can be used in research related to depression, Parkinson's disease, and acute pain .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1264
-
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nAChR
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Neurological Disease
|
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α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
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- HY-171746
-
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4,5,6,7-Tetrafluoro-L-tryptophan
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nAChR
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Neurological Disease
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F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a ligand targeting the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). F4-Trp is promising for research of neurotransmission, addiction, and related diseases, such as neurological diseases .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-A0009
-
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Galantamine hydrobromide
|
Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
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Cholinesterase (ChE)
nAChR
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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) .
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- HY-114791
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- HY-A0009R
-
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Galantamine hydrobromide (Standard)
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Structural Classification
Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
Source Classification
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nAChR
Cholinesterase (ChE)
Reference Standards
|
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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) .
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- HY-N12511
-
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- HY-N10132
-
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- HY-N11477
-
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Triterpenes
Terpenoids
Rosaceae
Plants
Source Classification
Rubus ellipticus Smith
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Glycosidase
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(2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid is a saponin that can be isolated from Rubus ellipticus var. obcordatus. (2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid inhibits α-Glucosidase with an IC50 of 1.68 mM .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-10019S
-
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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 .
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- HY-A0009S
-
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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) .
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- HY-10019AS1
-
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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 .
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| Cat. No. |
Product Name |
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Classification |
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- HY-14318
-
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SIB-1508Y free base
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Alkynes
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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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