Search Result
Results for "
α7nAChR
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-N2332A
-
|
MLA citrate
|
nAChR
|
Neurological Disease
|
|
Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .
|
-
-
- HY-14564A
-
|
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 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist .
|
-
-
- HY-B0567
-
|
|
Potassium Channel
nAChR
Apoptosis
Bacterial
Parasite
|
Infection
Cancer
|
|
Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
|
-
-
- HY-12152
-
|
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-172236
-
|
BNC210; IW-2143
|
nAChR
|
Neurological Disease
|
|
Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 (HY-12560A) with IC50 values in the range of 1.2 to 3 μM. Soclenicant can be used in studies of anxiety, trauma, and stressor-related disorders .
|
-
-
- HY-19490
-
|
AQW-051
|
nAChR
|
Neurological Disease
|
|
VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pKD value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety .
|
-
-
- HY-N2255
-
|
|
Akt
Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
p38 MAPK
ERK
Interleukin Related
TNF Receptor
NO Synthase
nAChR
Bacterial
|
Cancer
|
|
Crebanine is an isoquinoline-like alkaloid that can be derived from Stephania. Crebanine is an antagonist of the α7-nAChR with an IC50 of 19.1 μM. Crebanine suppresses the proliferation, migration, and invasion of cancer cells, triggers reactive oxygen species (ROS) burst, and promotes apoptosis. Crebanine inhibits the AKT/FoxO3a, NF-κB and MAPK signaling pathways. Crebanine attenuates NOX2 hyperactivation, exhibits antioxidant properties by reducing reactive oxygen species and peroxidation in microglia cells. Crebanine inhibits voltage-dependent Na + current in guinea-pig ventricular myocytes. Crebanine has high inhibitory activity against gram-positive animal pathogenic bacteria. Crebanine ameliorates ischemia-reperfusion brain damage in middle cerebral artery occlusion and reperfusion (MCAO/R) rats. Crebanine significantly improves Scopolamine (HY-N0296)-induced cognitive deficits in ICR mice. Crebanine can be used for the study of hepatocellular carcinoma (HCC), cerebral ischemia and Alzheimer's disease .
|
-
-
- HY-12150
-
CCMI
1 Publications Verification
AVL-3288; UCI-4083
|
nAChR
|
Neurological Disease
|
|
CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .
|
-
-
- HY-105670
-
|
|
nAChR
|
Neurological Disease
|
|
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 .
|
-
-
- HY-12151
-
|
NSC 213859
|
nAChR
|
Neurological Disease
|
|
NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
|
-
-
- HY-146066
-
|
|
nAChR
JAK
STAT
NO Synthase
Interleukin Related
|
Inflammation/Immunology
|
|
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
|
-
-
- HY-18060
-
|
TC-5619
|
nAChR
|
Neurological Disease
|
|
Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
-
- HY-106901A
-
|
HI-6
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Asoxime dichloride (HI-6) is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system .
|
-
-
- HY-114269
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
(-)-(S)-B-973B is an allosteric activator of α7 nicotinic acetylcholine receptor (α7 nAChR). (-)-(S)-B-973B alleviates pain behaviors. (-)-(S)-B-973B can be used for the research of inflammatory pain .
|
-
-
- HY-N8249
-
|
|
nAChR
Interleukin Related
|
Inflammation/Immunology
|
|
Cynandione A is an acetophenone that can be isolated from Cynanchum Wilfordii Radix. Cynandione A protects hepatocytes and cortical neurons from toxicity and improves neurological deficits in a rat model of cerebral ischemia. On the other hand, cynandione A has significant anti-inflammatory effects and inhibits inflammation by activating macrophage α7 nAChR and IL-10 expression .
|
-
-
- HY-110160
-
|
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki 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 Ki of 17 nM while binding to α7 nAChR is insignificant .
|
-
-
- HY-W698871
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Others
|
|
(±) Anabasine-d4 is the deuterium labeled (±) Anabasine (HY-W052144). (±) Anabasine is the racemate of Anabasine (HY-B1532). Anabasine is an agonist of α7nAChR and exhibits anti-inflammatory and insecticidal activities .
|
-
-
- HY-107672
-
|
Stilonium iodide
|
nAChR
|
Neurological Disease
|
|
MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM .
|
-
-
- HY-161671
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice .
|
-
-
- HY-19411
-
|
|
nAChR
|
Neurological Disease
|
|
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 .
|
-
-
- HY-128575
-
|
|
nAChR
|
Neurological Disease
|
|
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-agent like properties and clinical candidate potential. .
|
-
-
- HY-10063
-
|
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 (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
|
-
-
- HY-105670B
-
|
|
nAChR
|
Neurological Disease
|
|
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 .
|
-
-
- HY-110087
-
|
|
nAChR
|
Neurological Disease
|
|
4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site .
|
-
-
- HY-129674
-
|
|
nAChR
|
Neurological Disease
|
|
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation .
|
-
-
- HY-16748
-
|
ABT-126
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease .
|
-
-
- HY-148325
-
|
|
nAChR
|
Neurological Disease
|
|
α7 Nicotinic receptor agonist-1 (Preparation 5) is an α7 nAChR agonist. α7 Nicotinic receptor agonist-1 can be used in studies of psychiatric disorders (such as schizophrenia, manic or hypomanic depression and anxiety disorders) and intellectual disorders (such as alzheimer's disease, learning deficits, cognitive deficits, attention deficits, memory loss, lewy body dementia and attention deficit hyperactivity disorder) .
|
-
-
- HY-W052144
-
|
|
Endogenous Metabolite
|
Others
|
|
(±) Anabasine is the racemate of Anabasine (HY-B1532). Anabasine is an agonist of α7nAChR and exhibits anti-inflammatory and insecticidal activities .
|
-
-
- HY-146066A
-
|
|
nAChR
JAK
STAT
NO Synthase
|
Others
|
|
(R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
|
-
-
- HY-11053
-
|
|
nAChR
|
Neurological Disease
|
|
S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the research of aging-related memory disturbances .
|
-
-
- HY-107678
-
|
WAY-317538
|
nAChR
|
Neurological Disease
|
|
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca 2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research .
|
-
-
- HY-133011
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR agonist 1 is a potent, blood-brain-barrier-permeable, and orally active allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 μM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease .
|
-
-
- HY-14564
-
|
|
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 (Ki=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-12560D
-
|
|
nAChR
|
Others
|
|
PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
|
-
-
- HY-P5823
-
|
|
nAChR
|
Neurological Disease
|
|
Azemiopsin is a potent nicotinic acetylcholine receptor (nAChR) inhibitor with IC50s of 0.18 μM and 22 μM against T. californica nAChR and human α7 nAChR, respectively. Azemiopsin blocks acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR .
|
-
-
- HY-137231B
-
|
|
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-126049
-
|
(S)-(-)-Oxiracetam; (S)-ISF2522
|
Apoptosis
|
Neurological Disease
|
|
(S)-oxiracetam (S-ORC) is an inhibitor targeting apoptosis. S-ORC reduces brain infarct size and lessens neurological dysfunction in middle cerebral artery occlusion/reperfusion (MCAO/R) models. S-ORC prevents neuronal apoptosis via activating PI3K/Akt/GSK3β signaling pathway via α7 nAChR after ischemic stroke. S-ORC can prevent neuronal death after ischemic stroke .
|
-
-
- HY-106901AS
-
|
HI-6-d4
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Asoxime-d4 dichloride (HI-6-d4) is the deuterium labeled Asoxime dichloride. Asoxime dichloride is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system.
|
-
-
- HY-W052144R
-
-
-
- HY-W052144S
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Others
|
|
(±) Anabasine-d4 dihydrochloride is deuterium labeled (±) Anabasine dihydrochloride. (±) Anabasine dihydrochloride is the racemate of Anabasine dihydrochloride. Anabasine dihydrochloride is an agonist of α7nAChR and exhibits anti-inflammatory and insecticidal activities .
|
-
-
- HY-160529
-
|
|
nAChR
|
Neurological Disease
|
|
α7 nAChR Modulator-2 (Compound 7b) is a α7 nAChR positive allosteric modulator (PAM) with an EC50 of 2.1 μM. α7 nAChR Modulator-2 can be used for the research of cognitive disorders .
|
-
-
- HY-157958
-
|
|
nAChR
|
Neurological Disease
|
|
α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC50 value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model .
|
-
-
- HY-10554
-
|
|
nAChR
|
Neurological Disease
|
|
WYE-103914 is an orally active α7 nAChR (EC50 = 0.49 µM for rat α7 nAChR, EC50 = 0.57 µM for human α7 nAChR) agonist. WYE-103914 exhibits the ability to enhance memory in multiple cognitive models. WYE-103914 is used in combination with antipsychotic drugs. WYE-103914 can be used for research on schizophrenia .
|
-
-
- HY-117611
-
-
-
- HY-107683
-
|
|
nAChR
|
Neurological Disease
|
|
LY-2087101 is an allosteric potentiator of α7 nAChRs. LY-2087101 causes potentiation of agonist-evoked α7 responses by binding within the nAChR transmembrane region .
|
-
-
- HY-118646
-
|
|
nAChR
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
NS-6740 is a partial agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 also acts as a potent modulator of the cholinergic anti-inflammatory pathway. NS-6740 alters the signaling pattern of α7 in an ion channel-independent manner, thereby reducing synaptic function. NS-6740 induces the desensitized state of α7 nAChR. NS-6740 generates robust nAChR-mediated currents. NS-6740 reduces LPS (HY-D1056)-induced TNF-α release from microglia. NS-6740 can be used in the research of neuroinflammation and neuropathic pain .
|
-
-
- HY-114791
-
|
|
nAChR
|
Neurological Disease
|
|
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 .
|
-
-
- HY-B0567R
-
|
|
Reference Standards
Potassium Channel
nAChR
Apoptosis
Bacterial
Parasite
|
Infection
Cancer
|
|
Dequalinium (Chloride) (Standard) is the analytical standard of Dequalinium (Chloride). This product is intended for research and analytical applications. Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity .
|
-
-
- HY-138879B
-
|
(1S,5R)-CP-601927
|
nAChR
|
Neurological Disease
|
|
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 .
|
-
-
- HY-59201A
-
|
|
ERK
5-HT Receptor
Epigenetic Reader Domain
nAChR
|
Neurological Disease
Metabolic Disease
|
|
A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
- HY-W209279
-
|
|
Endogenous Metabolite
|
Others
|
|
(±) Anabasine hydrochloride is the racemate of Anabasine (HY-B1532). Anabasine hydrochloride is an agonist of α7nAChR and exhibits anti-inflammatory and insecticidal activities .
|
-
- HY-182694
-
|
|
nAChR
|
Neurological Disease
|
|
α7 nAChR Modulator-4 is a positive allosteric modulator of α7 nAChR, with an EC50 of 910 nM. α7 nAChR Modulator-4 interacts with α7 nAChR to trigger downstream effects associated with inflammatory regulation. α7 nAChR Modulator-4 can be used in the research of Alzheimer's disease, Parkinson's disease and schizophrenia .
|
-
- HY-107673
-
-
- HY-N18367
-
|
Wgx-50
|
nAChR
Interleukin Related
Akt
|
Neurological Disease
Inflammation/Immunology
|
|
Lemairamin (Wgx-50) is a hydroxylamine compound. Lemairamin can be isolated from the pericarps of the Zanthoxylum plants. Lemairamin activates α7nAChR, stimulates the expression of IL-10 and POMC. Lemairamin shows a decrease in Akt. Lemairamin attenuates DSS-induced intestinal inflammation. Lemairamin alleviates pain hypersensitivity .
|
-
- HY-N2332
-
|
MLA
|
nAChR
|
Neurological Disease
|
|
Methyllycaconitine (MLA) is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine can be used for neurological disease research, such as Alzheimer’s disease .
|
-
- HY-10814
-
|
|
nAChR
|
Neurological Disease
|
|
CP-810123 is a brain-permeable agonist of α7 nAChR for the research of cognitive impairment associated with psychiatric or neurological disorders such as schizophrenia and Alzheimer's disease .
|
-
- HY-105670R
-
|
|
Reference Standards
nAChR
|
Neurological Disease
|
|
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 .
|
-
- HY-18060A
-
|
TC-5619 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
- HY-B1178A
-
|
(+)-Cotinine; (R)-Cotinine; (R)-NIH-10498
|
nAChR
|
Neurological Disease
|
|
R-(+)-Cotinine ((+)-Cotinine), a Nicotine metabolite, lacks significant activity across a wide range of pharmacological targets. R-(+)-Cotinine can enhance the Ach-evoked current in human α7 nAChRs .
|
-
- HY-116507
-
|
|
nAChR
|
Neurological Disease
|
|
AZD0328 is a selective α7 nAChR partial agonist. AZD0328 selectively enhances midbrain dopaminergic neuronal activity and enhances cortical dopamine levels in rats. AZD0328 improves cognitive performance .
|
-
- HY-146405
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
nAChR antagonist 1 (compound B15) is an excellent α7 nAChR antagonist with an IC50 value of 3.3 μM. nAChR antagonist 1 can be used for researching schizophrenia, Alzheimer’s disease and inflammatory disorders .
|
-
- HY-107666
-
-
- HY-18039
-
|
SEN15924
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
WAY-361789 (SEN15924) is an orally active agonist for α7 nicotinic acetylcholine receptor (α7 nAChR) with an EC50 of 0.18 μM. WAY-361789 improves the cognitive function, exhibits potential in ameliorating Alzheimer’s Disease and schizophrenia .
|
-
- HY-16748A
-
|
ABT-126 citrate
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease .
|
-
- HY-149776
-
|
|
nAChR
|
Neurological Disease
|
|
RGH-560 (compound 53) shows highly advanced α7 nAChR positive modulator properties and favorable physicochemical features. RGH-560 has robust procognitive in vivo potential. RGH-560 can be used to study Scopolamine (HY-N0296) -induced amnesia in mice .
|
-
- HY-105670A
-
|
|
nAChR
|
Neurological Disease
|
|
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 .
|
-
- HY-137231A
-
|
|
nAChR
|
Neurological Disease
|
|
(S)-UFR2709 is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction .
|
-
- HY-12153
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
JNJ-1930942 is a selective and blood-brain barrier (BBB) penetrant α(7) nAChR positive allosteric modulator.JNJ-1930942 enhances the Choline (HY-B0282)-evoked rise in intracellular Ca 2+ levels and neurotransmission at hippocampal dentate gyrus synapses. JNJ-1930942 reverses the naturally occurring sensory gating deficit in DBA/2 mice .
|
-
- HY-10019S
-
|
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 . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .
|
-
- HY-10019AS1
-
|
|
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-B0072S
-
-
- HY-N0584B
-
|
6-Hydroxyhyoscyamine hydrochloride
|
Adrenergic Receptor
|
Inflammation/Immunology
Cancer
|
|
Anisodamine hydrochloride is an anticholinergic and α1 adrenergic receptor antagonist. Anisodamine hydrochloride can be used for improving blood flow in circulatory disorders such as septic shock, Anisodamine hydrochloride displays a spectrum of pharmacological effects similar to Atropine (HY-B1205) and Sopolamine (HY-B2065) including inhibition of salivation, gastrointestinal and sweat secretion, gastrointestinal motility, respiratory secretion and urinary bladder contraction in vivo .
|
-
- HY-180400
-
|
|
nAChR
Calcium Channel
|
Neurological Disease
|
|
PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain .
|
-
- HY-124057
-
|
|
nAChR
|
Neurological Disease
|
|
RO5126946 is a selective, orally active α7 nAChR allosteric potentiator with EC50 values of 0.06 μM (hα7 nAChR) and 770 nM (α7 nAChR), and it crosses the blood-brain barrier. RO5126946 enhances synaptic transmission and positively modulates GABA-ergic responses by increasing peak current, slowing current decay, and elevating the frequency of spontaneous inhibitory postsynaptic currents, without affecting the recovery of receptors from the desensitized state. RO5126946 not only enhances subthreshold nicotine effects and improves associative learning, but also does not interfere with the original pro-cognitive effects of nicotine. RO5126946 can be used to study cognitive impairments associated with diseases such as Alzheimer's disease and schizophrenia .
|
-
- HY-18060B
-
|
TC-5619 tosylate
|
nAChR
|
Inflammation/Immunology
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline tosylate exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline tosylate possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline tosylate requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline tosylate is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
- HY-116488
-
|
|
nAChR
|
Neurological Disease
|
|
IND8 is a α7 nAChR activator and cognitive enhancer. IND8 mediates cognitive enhancement by activating α7 nAChR . IND8 improves spatial working memory, episodic short-term memory and spatial long-term memory in amnesic mice induced by Scopolamine (HY-N0296). IND8 improves memory function in mice with delayed natural memory decline. IND8 can be used in research related to Alzheimer's disease .
|
-
- HY-107678R
-
|
WAY-317538 (Standard)
|
Reference Standards
nAChR
|
Neurological Disease
|
|
SEN12333 (Standard) is the analytical standard of SEN12333 (HY-107678). This product is intended for research and analytical applications. SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays high affinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research .
|
-
- HY-18176
-
|
|
nAChR
Potassium Channel
|
Neurological Disease
|
|
SEN 78702 is an orally active, selective, full α7 nAChR agonist, with a pEC50 of 6.13. SEN 78702 has an acceptable hERG inhibition (IC50: 15.8 μM). SEN 78702 induces memory enhancement .
|
-
- HY-182010
-
|
|
nAChR
|
Neurological Disease
|
|
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 .
|
-
- HY-P11470
-
|
|
nAChR
SARS-CoV
|
Infection
|
|
Conofurin-Delta is a potent α7 nAChR inhibitor with an IC50 of 177 nM. Conofurin-Delta also inhibits α9α10 nAChR with an IC50 of 98.1 nM. Conofurin-Delta may be used in SARS-CoV-2 infection research .
|
-
- HY-118646A
-
|
|
nAChR
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
NS-6740 hydrochloride is a partial agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC50 of 3 nM. NS-6740 hydrochloride also acts as a potent modulator of the cholinergic anti-inflammatory pathway. NS-6740 hydrochloride alters the signaling pattern of α7 in an ion channel-independent manner, thereby reducing synaptic function. NS-6740 hydrochloride induces the desensitized state of α7 nAChR. NS-6740 hydrochloride generates robust nAChR-mediated currents. NS-6740 hydrochloride reduces LPS (HY-D1056)-induced TNF-α release from microglia. NS-6740 hydrochloride can be used in the research of neuroinflammation and neuropathic pain .
|
-
- HY-179621
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
EQ-04 is a highly selective positive allosteric modulator (PAM) of α7 nAChR. EQ-04 has no direct inhibitory activity on AChE and BChE. EQ-04 inhibits Aβ aggregation. EQ-04 has safe cytotoxicity and potent neuroprotective activity. EQ-04 can be used for the study of Alzheimer's disease.
|
-
- HY-182707
-
|
|
nAChR
Interleukin Related
TNF Receptor
NF-κB
|
Neurological Disease
|
|
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 .
|
-
- HY-106901B
-
|
HI-6 dimesylate
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Asoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system .
|
-
- HY-59201
-
|
|
nAChR
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5823
-
|
|
nAChR
|
Neurological Disease
|
|
Azemiopsin is a potent nicotinic acetylcholine receptor (nAChR) inhibitor with IC50s of 0.18 μM and 22 μM against T. californica nAChR and human α7 nAChR, respectively. Azemiopsin blocks acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR .
|
-
- HY-P11470
-
|
|
nAChR
SARS-CoV
|
Infection
|
|
Conofurin-Delta is a potent α7 nAChR inhibitor with an IC50 of 177 nM. Conofurin-Delta also inhibits α9α10 nAChR with an IC50 of 98.1 nM. Conofurin-Delta may be used in SARS-CoV-2 infection research .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: