Search Result
Results for "
nAChR
" in MedChemExpress (MCE) Product Catalog:
12
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-145299
-
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nAChR
|
Infection
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nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator .
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- HY-145300
-
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nAChR
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Infection
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nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator .
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-
-
- HY-136258
-
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nAChR
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Neurological Disease
|
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity .
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-
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- HY-146405
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nAChR
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Neurological Disease
Inflammation/Immunology
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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 .
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-
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- HY-107669
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nAChR
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Neurological Disease
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nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
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-
-
- HY-151129
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nAChR
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Neurological Disease
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nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
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-
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- HY-133011
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nAChR
|
Neurological Disease
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nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive 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 .
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-
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- HY-115764
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-
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- HY-157958
-
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nAChR
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Neurological Disease
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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 .
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-
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- HY-160529
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nAChR
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Neurological Disease
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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 .
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-
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- HY-P3654
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nAChR
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Neurological Disease
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α-Conotoxin SIA is a selective nicotinic acetylcholine receptor (nAChR) antagonist with high affinity for the muscle nAChR. α-Conotoxin SIA preferentially targets the α/δ interface of the muscle nAChR in mouse muscle. In contrast, for Torpedo nAChR, α-Conotoxin SIA has a much higher affinity for the α/γ than for the α/δ interface .
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-
-
- HY-146066
-
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nAChR
JAK
STAT
NO Synthase
|
Inflammation/Immunology
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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 .
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- HY-107686
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5-I A-85380 dihydrochloride
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nAChR
|
Neurological Disease
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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 Kds of 12 and 14 pM,respectively .
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-
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- HY-P5188A
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-
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- HY-10063
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TC-1734; ACD3480
|
nAChR
|
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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-
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- HY-110131
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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 .
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- HY-N12511
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nAChR
|
Neurological Disease
|
Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity .
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-
-
- HY-W014928
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(S)-Anabasine hydrochloride; (+)-Anabasine hydrochloride
|
nAChR
|
Neurological Disease
|
Anabasine ((S)-Anabasine) hydrochloride is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 µM) .
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- HY-145297
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-
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- HY-P1265
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Vc1.1
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nAChR
|
Neurological Disease
|
ACV1 (Vc1.1), an α-Conotoxin, is a selective α9α10 nAChR antagonist with an IC50 of 19 nM. ACV1 is ~100-fold less potent on human α9α10 vs. rat nAChRs .
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- HY-110087
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nAChR
|
Neurological Disease
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4BP-TQS is a potent allosteric agonist of α7 nAChR. 4BP-TQS activates nAChRs via an allosteric transmembrane site .
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-
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- HY-10019
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CP 526555
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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-
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- HY-10020
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CP 526555 hydrochloride
|
nAChR
|
Neurological Disease
Inflammation/Immunology
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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 .
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- HY-10021
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CP 526555-18
|
nAChR
ERK
p38 MAPK
|
Others
Neurological Disease
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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 .
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-
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- HY-10019A
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CP 526555 dihydrochloride
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nAChR
|
Neurological Disease
Inflammation/Immunology
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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 .
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- HY-138879A
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nAChR
|
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-131001
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nAChR
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Neurological Disease
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DPNB-ABT594 is a nitrobenzyl-caged ABT594 (HY-14316A) and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca 2+ signalling in the MHb .
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- HY-152170
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nAChR
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Neurological Disease
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bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
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-
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- HY-10019S1
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CP 526555-15N,13C,d2
|
nAChR
Isotope-Labeled Compounds
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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 .
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- HY-B1532
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(S)-Anabasine; (+)-Anabasine
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nAChR
|
Neurological Disease
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Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 µM) .
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- HY-B0823
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nAChR
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Neurological Disease
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Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders .
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- HY-105170B
-
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nAChR
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Neurological Disease
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ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease .
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- HY-107680
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3-Pyr-Cyt
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nAChR
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Neurological Disease
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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 .
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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-110121A
-
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nAChR
|
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-124874
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(rel)-Aspergillimide; (rel)-VM55598
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nAChR
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Neurological Disease
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(rel)-Asperparaline A ((rel)-Aspergillimide), an anthelmintic metabolite, is isolated from okara that has been fermented with Aspergillus japonicas JV-23. (rel)-Asperparaline A is also a potent and selective antagonist of nAChR. (rel)-Asperparaline A exhibits paralytic activity in silk worms .
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- HY-B0118A
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ORG NC 45
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nAChR
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Neurological Disease
Cancer
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Vecuronium (ORG NC 45) bromide is a non-depolarizing neuromuscular blocking agent that also acts as a nicotinic acetylcholine receptor (nAChR) inhibitor, a muscle relaxant, and can be used for pre-surgical anesthesia .
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-
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- HY-10019AS1
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Isotope-Labeled Compounds
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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-P5306
-
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nAChR
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Neurological Disease
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α-Conotoxin TxID is a potent α3β4 nAChR antagonist with an IC50 value of 12.5 nM. α-Conotoxin TxID has weak inhibition activity of closely related α6/α3β4 nAChR (IC50= 94 nM). α-Conotoxin TxID has the potential for novel smoking cessation drug development .
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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-145295
-
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nAChR
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Infection
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Flupyradifurone is a systemic nAChR agonist that interferes with signal transduction in the central nervous system of sucking pests. Flupyradifurone can be used as a butenolide insecticide .
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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-135483A
-
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nAChR
|
Neurological Disease
|
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis 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 .
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-
-
- HY-105670A
-
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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 .
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-
-
- HY-P1271
-
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nAChR
|
Cardiovascular Disease
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
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-
-
- HY-59201A
-
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nAChR
5-HT Receptor
|
Neurological Disease
|
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
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-
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- HY-P1271A
-
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nAChR
|
Cardiovascular Disease
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
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-
-
- HY-128575
-
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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. .
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-
-
- HY-P5823
-
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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 .
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-
-
- HY-138953
-
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nAChR
|
Neurological Disease
|
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-138953A
-
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nAChR
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Neurological Disease
|
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-110160
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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 .
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-
- HY-19490
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AQW-051
|
|
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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 .
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-
- HY-14316A
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Ebanicline dihydrochloride; ABT-594 dihydrochloride
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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 Ki of 37 pM .
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-
- HY-14316B
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Ebanicline hydrochloride; ABT-594 hydrochloride
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nAChR
|
Neurological Disease
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Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
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-
- HY-12150
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AVL-3288; UCI-4083
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nAChR
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Neurological Disease
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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 .
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- HY-118504
-
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nAChR
|
Neurological Disease
|
Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens .
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-
- HY-107683
-
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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 .
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-
- HY-107676
-
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nAChR
|
Neurological Disease
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders .
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- HY-P5839
-
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nAChR
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Neurological Disease
|
α-Conotoxin MrIC is an α7nAChR biased agonist. α-Conotoxin MrIC exclusively activates α7nAChR regulated by type II positive allosteric modulators, including PNU120596. α-Conotoxin MrIC can be used to study neurological diseases and also to probe the pharmacological properties of α7nAChR .
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- HY-12151
-
NSC 213859
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nAChR
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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).
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-
- HY-137231B
-
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nAChR
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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 .
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-
- HY-137231A
-
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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 .
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-
- HY-18060
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TC-5619
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nAChR
|
Neurological Disease
|
Bradanicline is a highly selective α7 nicotinic acetylcholine receptor (nAChR) agonist (humanα7 nAChR: EC50=17 nM; Ki= 1.4 nM). Bradanicline is used for the research of cognitive disorders .
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- HY-U00139
-
-
- HY-P5849
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αA-OIVA
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nAChR
|
Neurological Disease
|
αA-Conotoxin OIVA (αA-OIVA) is a selective nAChR antagonist with an IC50 of 56 nM against mammalian fetal muscle nAChR. αA-Conotoxin OIVA is a peptide that can be derived from conotoxin. αA-Conotoxin OIVA paralyzes muscles .
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-
- HY-P1269
-
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nAChR
|
Neurological Disease
|
α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM .
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-
- HY-P5149
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αC-PrXA
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nAChR
|
Neurological Disease
|
αC-Conotoxin PrXA is a paralytic peptide neurotoxin and a competitive nAChR antagonist, with IC50s of 1.8 nM (α1β1εδ, adult) and 3.0 nM (α1β1γδ, fetal), respectively. αC-Conotoxin PrXA competes with α-bungarotoxin at the α/δ and α/γ subunit interfaces of the nAChR, shows high specificity against neuromuscular nAChR .
|
-
- HY-P1268
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia 。
|
-
- HY-P1269A
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin AuIB TFA, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM .
|
-
- HY-107674
-
|
nAChR
|
Neurological Disease
|
bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
|
-
- 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-P1268A
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia 。
|
-
- HY-121027
-
(-)-Anagyrine; Monolupine; Rhombinine
|
mAChR
nAChR
|
Neurological Disease
|
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .
|
-
- HY-121027A
-
(-)-Anagyrine hydrochloride; Monolupine hydrochloride; Rhombinine hydrochloride
|
mAChR
nAChR
|
Neurological Disease
|
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR .
|
-
- HY-107672
-
Stilonium iodide
|
nAChR
|
Neurological Disease
|
MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM .
|
-
- HY-B0282S
-
ACh-d4 (chloride)
|
nAChR
Calcium Channel
Endogenous Metabolite
|
Neurological Disease
Cancer
|
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
|
-
- HY-B0282S1
-
ACh-d9(chloride)
|
nAChR
Calcium Channel
Endogenous Metabolite
|
Neurological Disease
Cancer
|
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
|
-
- 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-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-107673
-
-
- HY-146404
-
-
- HY-14565
-
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 (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, 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-15430A
-
EVP-6124 hydrochloride
|
nAChR
|
Neurological Disease
|
Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
|
-
- HY-14774
-
AAD1566
|
nAChR
|
Cancer
|
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-15430
-
EVP-6124
|
nAChR
|
Neurological Disease
|
Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
|
-
- HY-107679
-
-
- HY-107670
-
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-145298
-
|
nAChR
|
Infection
|
Dicloromezotiaz is a potent insecticide acting on nicotinic acetylcholine receptors (nAChRs). Dicloromezotiaz can be used to control a broad range of lepidoptera .
|
-
- HY-B0823S
-
|
nAChR
|
Neurological Disease
|
Acetamiprid-d3 is the deuterium labeled Acetamiprid. Acetamiprid is a neonicotinoid insecticide. Acetamiprid is a nAChR agonist[1].
|
-
- HY-107675
-
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-N3610
-
|
nAChR
|
Neurological Disease
|
Coclaurine is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist .
|
-
- HY-W795027
-
-
- HY-12152
-
NSC 216666
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) 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-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-107682
-
-
- HY-W705106
-
(-)-(S)-Coclaurine hydrochloride; (S)-Coclaurine hydrochloride; l-Coclaurine hydrochloride
|
nAChR
|
Neurological Disease
|
(-)-Coclaurine hydrochloride (compound I) is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum. (-)-Coclaurine hydrochloride is a nicotinic acetylcholine receptor (nAChRs) antagonist .
|
-
- HY-N2332A
-
MLA
|
nAChR
|
Neurological Disease
|
Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR) with blood-brain barrier permeability.
|
-
- HY-114269
-
|
nAChR
|
Neurological Disease
|
(-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity .
|
-
- HY-124540B
-
|
nAChR
|
Neurological Disease
|
(Rac)-ABT-202 dihydrochloride is a racemate of ABT-202. ABT-202 is an agonist of nicotinic acetylcholine receptors (nAChRs) and can be used as an analgesic .
|
-
- HY-136608
-
|
nAChR
|
Neurological Disease
|
5-AAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist .
|
-
- HY-136609
-
|
nAChR
|
Neurological Disease
|
5-AMAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist .
|
-
- 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-108038
-
|
nAChR
|
Neurological Disease
|
ABT-107 is a selective α7 neuronal nicotinic receptor agonist. ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions .
|
-
- HY-14824
-
ABT 894
|
nAChR
|
Neurological Disease
|
Sofiniclin (ABT 894), an agonist of nicotinic acetylcholine receptor (nAChR), is used as a potential non-stimulant research for attention-deficit/hyperactivity disorder (ADHD) .
|
-
- HY-13780
-
Vincaleukoblastine sulfate salt
|
Microtubule/Tubulin
Autophagy
|
Cancer
|
Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
|
-
- 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-W001909
-
|
nAChR
|
Metabolic Disease
|
Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM .
|
-
- HY-B1552B
-
|
|
|
Benzoquinonium dibromide is a nicotinic acetylcholine receptors (nAChRs) antagonist, with an IC50 of 0.46 μM. Benzoquinonium dibromide can block neuromuscular and ganglionic transmission .
|
-
- 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-W099757
-
2-Propylpiperidine hydrochloride
|
nAChR
|
Neurological Disease
|
(±)-Coniine hydrochloride (2-Propylpiperidine hydrochloride) is a potent nAChR agonist with an EC50 value of 0.3 mM. (±)-Coniine hydrochloride shows acute toxicity with an LD50 value of 7.7 mg/kg .
|
-
- HY-P1264F
-
|
nAChR
|
Neurological Disease
|
FITC-α-Bungarotoxin is the FITC labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
|
-
- HY-P1264F1
-
|
nAChR
|
Neurological Disease
|
Biotin-α-Bungarotoxin is the Biotin labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
|
-
- HY-P1267
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease .
|
-
- HY-14774S
-
|
nAChR
|
Cancer
|
(Rac)-Monepantel-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-101347
-
|
nAChR
|
Neurological Disease
|
Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way .
|
-
- HY-N2326
-
|
|
|
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM) .
|
-
- 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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
|
-
- HY-P1270
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin Im-I is a selective α7/α9 nAChR antagonist, blocking α7 nicotinic receptors with the highest apparent affinity, while having an 8-fold lower affinity for homomeric α9 nicotinic receptors. α-Conotoxin Im-I is toxic and induces seizures in rodents. α-Conotoxin Im-I is a tool for studying neuronal nAChR .
|
-
- HY-12149
-
|
nAChR
|
Neurological Disease
|
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM .
|
-
- HY-B0820
-
|
|
|
Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals .
|
-
- HY-P1267A
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease .
|
-
- HY-14774S1
-
|
nAChR
|
Cancer
|
(Rac)-Monepantel sulfone-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-N3359
-
-
- HY-N3359B
-
D-Lupanine hydrochloride
|
nAChR
|
Neurological Disease
|
Lupanine (D-Lupanine) hydrochloride is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine hydrochloride shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM .
|
-
- HY-D1398
-
|
nAChR
|
Neurological Disease
|
LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
|
-
- HY-149483
-
|
nAChR
|
Neurological Disease
|
CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
|
-
- HY-P5148
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin BuIA is a paralytic peptide neurotoxin and a competitive nAChR antagonist, with IC50s of 0.258 nM (α6/α3β2), 1.54 nM (α6/α3β4), 5.72 nM (α3β2), respectively. α-Conotoxin BuIA can be used to distinguish nAChRs containing β2- and β4-subunit, respectively. α-Conotoxin BuIA distinguishes among αxβ2 nAChRs with a rank order potency of α6>α3>α2>α4 .
|
-
- 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-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-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-147360
-
|
nAChR
|
Infection
|
Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type nicotinic acetylcholine receptor (nAChR) agonist .
|
-
- HY-P5844
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin AuIA is a potent and selective α3β4 n-nAChR inhibitor. α-Conotoxin AuIA is a α-conotoxin that can be isolated from Conus aulicus .
|
-
- HY-B0743A
-
|
nAChR
|
Neurological Disease
|
Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM .
|
-
- HY-139582
-
OC-02
|
nAChR
SARS-CoV
|
Infection
|
Simpinicline (OC-02), a highly selective nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC50 of 0.04 µM .
|
-
- HY-B0282
-
ACh chloride
|
nAChR
Calcium Channel
Endogenous Metabolite
|
Neurological Disease
Cancer
|
Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
|
-
- HY-B1395
-
|
|
|
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
|
-
- HY-P1050
-
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM .
|
-
- HY-108069
-
|
Potassium Channel
nAChR
|
Neurological Disease
|
Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist .
|
-
- HY-B1395A
-
|
nAChR
Histamine Receptor
|
Cardiovascular Disease
Neurological Disease
|
Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
|
-
- HY-P5848
-
|
nAChR
|
Neurological Disease
|
αO-Conotoxin GeXIVA is a potent α9α10 nAChR antagonist with an IC50 of 12 nM against rat α9α10. αO-Conotoxin GeXIVA shows analgesic in animal models of pain .
|
-
- HY-P5147
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin GID is a paralytic peptide neurotoxin and a selective antagonist of nAChR, with IC50s of 5 nM (α7), 3 nM (α3β2), 150 nM (α4β2), respectively. α-Conotoxin GID is small disulfide-rich peptide, with potential to inhibit chronic pain. α-Conotoxin GID contains a C-terminal carboxylate, thus substitution with a C-terminal carboxamide results in loss of α4β2 nAChR. α-Conotoxin GID can be isolated from the Conus species .
|
-
- HY-W001909S
-
|
nAChR
|
Metabolic Disease
|
Myosmine-d4 is the deuterium labeled Myosmine. Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM[1][2].
|
-
- HY-B1700A
-
|
nAChR
|
Neurological Disease
|
Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell .
|
-
- HY-125777A
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach .
|
-
- HY-P1050A
-
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM .
|
-
- HY-115766
-
|
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-145296
-
|
nAChR
|
Infection
|
Triflumezopyrim, a mesoionic insecticide, has high efficiency at a low dosage, and is mainly used to control hopper species. Triflumezopyrim mainly acts on the nicotinic acetylcholine receptor (nAChR) inhibition, which is very highly efficient, rapidly effective, and nearly nontoxic to nontarget arthropods .
|
-
- HY-137788
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin GI has high affinity for nAChR.α-Conotoxin GI is a short peptide toxin that can be isolated from the venom of Conus geographus.α-Conotoxin GI has the similar activity with neuromuscular blocking agent .
|
-
- HY-161118
-
|
Others
|
Neurological Disease
|
MB327 is a bipyridine nonoxime compound that restores neuromuscular function. MB327 restores the activity of nicotinamide acetylcholine receptors (nAChRs) for carbachol desensitization in a typical type II PAM manner. MB327 can neutralize nerve agent poisoning .
|
-
- HY-107688A
-
|
nAChR
|
Neurological Disease
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
|
-
- HY-B0827B
-
(S)-MTI-446
|
nAChR
Parasite
|
Infection
|
(S)-Dinotefuran ((S)-MTI-446), a neonicotinoid pesticide, is toxic by binding to α8 subunit of nAChR of honeybee Apis mellifera (Apis mellifera Linnaeus). (S)-Dinotefuran shows more toxic than R-dinotefuran to honeybee Apis mellifera .
|
-
- HY-12641A
-
|
|
|
Pyrantel is an orally active anthelmintic and an agonist of the nicotinic acetylcholine receptor (nAChR). Pyrantel can cause spasmodic muscle paralysis in parasites. Pyrantel can be used in the study of parasitic infections such as ascariasis, hookworm infections, intestinal worms (pinworm infections), trichinosis and trichinosis .
|
-
- HY-107688
-
|
nAChR
|
Neurological Disease
|
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
|
-
- 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-B0820R
-
|
nAChR
Parasite
|
Neurological Disease
|
Nitenpyram (Standard) is the analytical standard of Nitenpyram. This product is intended for research and analytical applications. Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals .
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-
- HY-B0569
-
|
nAChR
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .
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-
- HY-N0175
-
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-P5841
-
|
Liposome
|
Neurological Disease
|
α-Conotoxin LtIA is an α3β2 nAChR blocker (IC50=9.8 nM), that can be obtained from Conus litteratus venom. Alpha-Conotoxin LtIA can be used in the study of neurological diseases (such as Parkinson's disease, pain) .
|
-
- HY-P5845
-
α-RgIA
|
nAChR
|
Neurological Disease
|
α-Conotoxin RgIA (α-RgIA) is a specific α9α10 nAChR antagonist. α-Conotoxin RgIA can be obtained from Conus regius venom. α-Conotoxin RgIA can be used in the study of neurological diseases .
|
-
- 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-12641
-
|
Parasite
nAChR
Antibiotic
|
Infection
|
Pyrantel tartrate is an orally active anthelmintic and an agonist of the nicotinic acetylcholine receptor (nAChR). Pyrantel tartrate can cause spasmodic muscle paralysis in parasites. Pyrantel tartrate can be used in the study of parasitic infections such as ascariasis, hookworm infections, intestinal worms (pinworm infections), trichinosis and trichinosis .
|
-
- HY-N0443
-
Caulophylline
|
nAChR
|
Inflammation/Immunology
|
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia .
|
-
- HY-106901A
-
HI-6
|
nAChR
|
Neurological Disease
|
Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system .
|
-
- 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-107666
-
-
- HY-105858
-
H-Ile-Trp-OH; IW-2143
|
nAChR
|
Neurological Disease
|
BNC210 (H-Ile-Trp-OH) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. BNC210 exhibits acute anxiolytic activity in rodent models of anxiety. BNC210 can be used in studies of generalised anxiety disorders .
|
-
- HY-138879
-
|
nAChR
|
Neurological Disease
|
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .
|
-
- HY-P3653
-
|
mAChR
nAChR
|
Neurological Disease
|
α-Conotoxin M I is a potent and selective inhibitor of mAChR and α1β1γδ nAChR, but has no effect on nicotine-stimulated dopamine release. α-Conotoxins are small, disulfide-rich peptides that competitively inhibit muscle and neuronal nicotinic AChRs .
|
-
- HY-12640
-
Pyrantel embonate
|
Parasite
nAChR
Antibiotic
|
Infection
|
Pyrantel pamoate (Pyrantel embonate) is an orally active anthelmintic and an agonist of the nicotinic acetylcholine receptor (nAChR). Pyrantel pamoate can cause spasmodic muscle paralysis in parasites. Pyrantel pamoate can be used in the study of parasitic infections such as ascariasis, hookworm infections, intestinal worms (pinworm infections), trichinosis and trichinosis .
|
-
- HY-138800
-
|
nAChR
|
Neurological Disease
|
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. Spinosad has an excellent environmental and mammalian toxicological profile. Larvicidal activity .
|
-
- HY-A0106
-
(-)-Tetramisole
|
|
|
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 .
|
-
- HY-19490A
-
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia .
|
-
- HY-12560A
-
|
nAChR
5-HT Receptor
|
Neurological Disease
|
PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems .
|
-
- HY-P1266
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors .
|
-
- HY-P1264
-
|
nAChR
|
Neurological Disease
|
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 .
|
-
- 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-P5852
-
Alpha-conotoxin EIIB
|
nAChR
|
Neurological Disease
|
α-Conotoxin EIIB (Alpha-conotoxin EIIB) is a toxin peptide that can be obtained from Conus ermineus. α-Conotoxin EIIB binds to nAChR (Ki=2.2 nM). α-Conotoxin EIIB can be used in the study of neurological diseases such as schizophrenia, drug addiction, Alzheimer's disease, and Parkinson's disease .
|
-
- HY-B1395S1
-
|
Isotope-Labeled Compounds
nAChR
|
Neurological Disease
|
Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
|
-
- HY-108057A
-
RG3487 hydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
|
-
- HY-12560
-
|
nAChR
5-HT Receptor
|
Neurological Disease
|
PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems .
|
-
- HY-P0099
-
|
|
|
Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
|
-
- HY-P5146
-
-
- HY-107681
-
|
nAChR
|
Neurological Disease
|
SIB-1508Y is an orally active and selective nAChR agonist. SIB-1508Y has the potential to study parkinsonism . SIB-1508Y is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-126047B
-
|
NF-κB
Amyloid-β
nAChR
|
Neurological Disease
Inflammation/Immunology
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
|
-
- HY-106901AS
-
HI-6-d4
|
Isotope-Labeled Compounds
nAChR
|
Neurological Disease
|
Asoxime-d4 (dichloride) is the deuterium labeled Asoxime dichloride. Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system[1].
|
-
- HY-A0009
-
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-12640R
-
Pyrantel embonate (Standard)
|
Parasite
nAChR
Antibiotic
|
Infection
|
Pyrantel (pamoate) (Standard) is the analytical standard of Pyrantel (pamoate). This product is intended for research and analytical applications. Pyrantel pamoate (Pyrantel embonate) is an orally active anthelmintic and an agonist of the nicotinic acetylcholine receptor (nAChR). Pyrantel pamoate can cause spasmodic muscle paralysis in parasites. Pyrantel pamoate can be used in the study of parasitic infections such as ascariasis, hookworm infections, intestinal worms (pinworm infections), trichinosis and trichinosis .
|
-
- HY-19918A
-
|
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-P1365
-
α-CTxMII
|
nAChR
|
Neurological Disease
|
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- 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-105118A
-
CGS-9343B; KW 5617
|
Calmodulin
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
|
-
- HY-P1365A
-
α-CTxMII TFA
|
nAChR
|
Neurological Disease
|
α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-12560C
-
|
nAChR
5-HT Receptor
|
Neurological Disease
|
(S)-PNU-282987 hydrochloride is an isoform of PNU-282987 (HY-12560). PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems .
|
-
- HY-A0009S
-
Galantamine-d3 hydrobromide
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
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)[1][2][3].
|
-
- HY-A0009R
-
Galantamine hydrobromide (Standard)
|
nAChR
Cholinesterase (ChE)
|
Neurological Disease
|
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-136207
-
|
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-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-P5850
-
|
nAChR
|
Neurological Disease
|
α-Conotoxin Bt1.8 is a potent α6/α3β2β3 and α3β2 nAChRs inhibitor with IC50s of 2.1 nM and 9.4 nM against rat α6/α3β2β3 and α3β2, respectively .
|
-
- HY-107684
-
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-15310
-
MK-933
|
Flavivirus
Dengue virus
Parasite
HIV
Mitophagy
HSV
SARS-CoV
Antibiotic
Autophagy
Bacterial
|
Infection
Cancer
|
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
|
-
- HY-103066
-
|
nAChR
|
Neurological Disease
|
Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit .
|
-
-
-
HY-L062
-
|
1785 compounds
|
Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.
In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.
MCE designs a unique collection of 1785 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.
|
-
-
HY-L069
-
|
1374 compounds
|
Alzheimer’s Disease (AD) is a progressive degenerative brain disease which causes mental and physical decline, gradually resulting in death. Despite the significant public health issue that it poses, only few medical treatments have been approved for Alzheimer’s Disease (AD) and these act to control symptoms rather than alter the course of the disease. Discovery of new therapeutic approaches depends on the study of pathology of AD. Recent research findings have led to greater understanding of disease neurobiology in Alzheimer's Disease (AD) and identification of unique targets for drug development. Several important mechanisms have been proposed to explain the underlying pathology of AD, such as Amyloid cascade hypothesis, Tau hypothesis and Cholinergic hypothesis, etc.
MCE offers a unique collection of 1374 compounds with anti-Alzheimer’s Disease activities or targeting the unique targets of AD. MCE Anti-Alzheimer’s Disease Compound Library is a useful tool for exploring the mechanism of AD and discovering new drugs for AD.
|
-
-
HY-L085
-
|
1339 compounds
|
Parkinson’s disease (PD), the second most common age-associated neurodegenerative disorder, is characterized by the loss of dopaminergic (DA) neurons and the presence of α-synuclein-containing aggregates in the substantia nigra pars compacta (SNpc). Motor features such as tremor, rigidity, bradykinesia and postural instability are common traits of PD. To date, there is no treatment to stop or at least slow down the progression of the disease. The etiology and pathogenesis of PD is still elusive, however, a large body of evidence suggests a prominent role of oxidative stress, inflammation, apoptosis, mitochondrial dysfunction and proteasome dysfunction in the pathogenesis of PD.
MCE offers a unique collection of 1339 compounds with anti- Parkinson’s Disease activities or targeting the unique targets of PD. MCE Anti- Parkinson's Disease Compound Library is a useful tool for exploring the mechanism of PD and discovering new drugs for PD.
|
-
-
HY-L086
-
|
2228 compounds
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Neurodegenerative diseases are incurable and life-threatening conditions that result in progressive degeneration and/or death of nerve cells. Some common neurodegenerative diseases include Alzheimer’s Disease (AD), Parkinson’s Disease (PD), Motor Neuron Disease (MND), Huntington’s Disease (HD), Spino-Cerebellar Ataxia (SCA), Spinal Muscular Atrophy (SMA), and Amyotrophic Lateral Sclerosis (ALS). Because the pathophysiology of neurodegenerative disorders is generally poorly understood, it is difficult to identify promising molecular targets and validate them. At the same time, about 85% of the drugs fail in clinical trials. Therefore, validating new targets and discovering new drugs to mitigate neurodegenerative disorders is need of the hour.
MCE offers a unique collection of 2228 compounds with anti-Neurodegenerative Diseases activities or targeting the unique targets of neurodegenerative diseases. MCE Neurodegenerative Disease-related Compound Library is a useful tool for exploring the mechanism of neurodegenerative diseases and discovering new drugs for neurodegenerative diseases.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1271
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nAChR
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Cardiovascular Disease
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Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
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- HY-P3654
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nAChR
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Neurological Disease
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α-Conotoxin SIA is a selective nicotinic acetylcholine receptor (nAChR) antagonist with high affinity for the muscle nAChR. α-Conotoxin SIA preferentially targets the α/δ interface of the muscle nAChR in mouse muscle. In contrast, for Torpedo nAChR, α-Conotoxin SIA has a much higher affinity for the α/γ than for the α/δ interface .
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- HY-P5188A
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- HY-P1265
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Vc1.1
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nAChR
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Neurological Disease
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ACV1 (Vc1.1), an α-Conotoxin, is a selective α9α10 nAChR antagonist with an IC50 of 19 nM. ACV1 is ~100-fold less potent on human α9α10 vs. rat nAChRs .
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- HY-P5306
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nAChR
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Neurological Disease
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α-Conotoxin TxID is a potent α3β4 nAChR antagonist with an IC50 value of 12.5 nM. α-Conotoxin TxID has weak inhibition activity of closely related α6/α3β4 nAChR (IC50= 94 nM). α-Conotoxin TxID has the potential for novel smoking cessation drug development .
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- HY-P1271A
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nAChR
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Cardiovascular Disease
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Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
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- HY-P5823
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nAChR
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Neurological Disease
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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 .
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- HY-P5839
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nAChR
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Neurological Disease
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α-Conotoxin MrIC is an α7nAChR biased agonist. α-Conotoxin MrIC exclusively activates α7nAChR regulated by type II positive allosteric modulators, including PNU120596. α-Conotoxin MrIC can be used to study neurological diseases and also to probe the pharmacological properties of α7nAChR .
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- HY-P5849
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αA-OIVA
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nAChR
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Neurological Disease
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αA-Conotoxin OIVA (αA-OIVA) is a selective nAChR antagonist with an IC50 of 56 nM against mammalian fetal muscle nAChR. αA-Conotoxin OIVA is a peptide that can be derived from conotoxin. αA-Conotoxin OIVA paralyzes muscles .
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- HY-P1269
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nAChR
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Neurological Disease
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α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM .
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- HY-P5149
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αC-PrXA
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nAChR
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Neurological Disease
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αC-Conotoxin PrXA is a paralytic peptide neurotoxin and a competitive nAChR antagonist, with IC50s of 1.8 nM (α1β1εδ, adult) and 3.0 nM (α1β1γδ, fetal), respectively. αC-Conotoxin PrXA competes with α-bungarotoxin at the α/δ and α/γ subunit interfaces of the nAChR, shows high specificity against neuromuscular nAChR .
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- HY-P1268
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nAChR
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Neurological Disease
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α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia 。
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- HY-P1269A
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nAChR
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Neurological Disease
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α-Conotoxin AuIB TFA, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM .
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- HY-P1268A
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nAChR
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Neurological Disease
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α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia 。
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- HY-P1264F
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nAChR
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Neurological Disease
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FITC-α-Bungarotoxin is the FITC labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
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- HY-P1264F1
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nAChR
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Neurological Disease
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Biotin-α-Bungarotoxin is the Biotin labelled α-Bungarotoxin (HY-P1264). α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs) .
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- HY-P1267
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nAChR
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Neurological Disease
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α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease .
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- HY-P1270
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nAChR
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Neurological Disease
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α-Conotoxin Im-I is a selective α7/α9 nAChR antagonist, blocking α7 nicotinic receptors with the highest apparent affinity, while having an 8-fold lower affinity for homomeric α9 nicotinic receptors. α-Conotoxin Im-I is toxic and induces seizures in rodents. α-Conotoxin Im-I is a tool for studying neuronal nAChR .
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- HY-P1267A
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nAChR
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Neurological Disease
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α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease .
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- HY-P5148
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nAChR
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Neurological Disease
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α-Conotoxin BuIA is a paralytic peptide neurotoxin and a competitive nAChR antagonist, with IC50s of 0.258 nM (α6/α3β2), 1.54 nM (α6/α3β4), 5.72 nM (α3β2), respectively. α-Conotoxin BuIA can be used to distinguish nAChRs containing β2- and β4-subunit, respectively. α-Conotoxin BuIA distinguishes among αxβ2 nAChRs with a rank order potency of α6>α3>α2>α4 .
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- HY-P5844
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nAChR
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Neurological Disease
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α-Conotoxin AuIA is a potent and selective α3β4 n-nAChR inhibitor. α-Conotoxin AuIA is a α-conotoxin that can be isolated from Conus aulicus .
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- HY-P5848
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nAChR
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Neurological Disease
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αO-Conotoxin GeXIVA is a potent α9α10 nAChR antagonist with an IC50 of 12 nM against rat α9α10. αO-Conotoxin GeXIVA shows analgesic in animal models of pain .
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- HY-P5147
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nAChR
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Neurological Disease
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α-Conotoxin GID is a paralytic peptide neurotoxin and a selective antagonist of nAChR, with IC50s of 5 nM (α7), 3 nM (α3β2), 150 nM (α4β2), respectively. α-Conotoxin GID is small disulfide-rich peptide, with potential to inhibit chronic pain. α-Conotoxin GID contains a C-terminal carboxylate, thus substitution with a C-terminal carboxamide results in loss of α4β2 nAChR. α-Conotoxin GID can be isolated from the Conus species .
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- HY-125777A
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nAChR
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Neurological Disease
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α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach .
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- HY-P1050A
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nAChR
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Neurological Disease
Inflammation/Immunology
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COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM .
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- HY-137788
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nAChR
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Neurological Disease
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α-Conotoxin GI has high affinity for nAChR.α-Conotoxin GI is a short peptide toxin that can be isolated from the venom of Conus geographus.α-Conotoxin GI has the similar activity with neuromuscular blocking agent .
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- HY-P5841
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Liposome
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Neurological Disease
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α-Conotoxin LtIA is an α3β2 nAChR blocker (IC50=9.8 nM), that can be obtained from Conus litteratus venom. Alpha-Conotoxin LtIA can be used in the study of neurological diseases (such as Parkinson's disease, pain) .
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- HY-P5845
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α-RgIA
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nAChR
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Neurological Disease
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α-Conotoxin RgIA (α-RgIA) is a specific α9α10 nAChR antagonist. α-Conotoxin RgIA can be obtained from Conus regius venom. α-Conotoxin RgIA can be used in the study of neurological diseases .
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- HY-P3653
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mAChR
nAChR
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Neurological Disease
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α-Conotoxin M I is a potent and selective inhibitor of mAChR and α1β1γδ nAChR, but has no effect on nicotine-stimulated dopamine release. α-Conotoxins are small, disulfide-rich peptides that competitively inhibit muscle and neuronal nicotinic AChRs .
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- HY-P1266
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nAChR
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Neurological Disease
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α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors .
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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-P5852
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Alpha-conotoxin EIIB
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nAChR
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Neurological Disease
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α-Conotoxin EIIB (Alpha-conotoxin EIIB) is a toxin peptide that can be obtained from Conus ermineus. α-Conotoxin EIIB binds to nAChR (Ki=2.2 nM). α-Conotoxin EIIB can be used in the study of neurological diseases such as schizophrenia, drug addiction, Alzheimer's disease, and Parkinson's disease .
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- HY-P5146
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- HY-P1365
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α-CTxMII
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nAChR
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Neurological Disease
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α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
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- HY-P1365A
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α-CTxMII TFA
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nAChR
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Neurological Disease
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α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
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- HY-P5850
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nAChR
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Neurological Disease
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α-Conotoxin Bt1.8 is a potent α6/α3β2β3 and α3β2 nAChRs inhibitor with IC50s of 2.1 nM and 9.4 nM against rat α6/α3β2β3 and α3β2, respectively .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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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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- HY-B0282S
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Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
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- HY-10019S1
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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 .
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- HY-B0282S1
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Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
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- HY-B0823S
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Acetamiprid-d3 is the deuterium labeled Acetamiprid. Acetamiprid is a neonicotinoid insecticide. Acetamiprid is a nAChR agonist[1].
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- HY-14774S
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(Rac)-Monepantel-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
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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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
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- HY-14774S1
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(Rac)-Monepantel sulfone-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
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- HY-W001909S
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Myosmine-d4 is the deuterium labeled Myosmine. Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM[1][2].
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- HY-B1395S1
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Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
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- HY-106901AS
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Asoxime-d4 (dichloride) is the deuterium labeled Asoxime dichloride. Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system[1].
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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)[1][2][3].
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Cat. No. |
Product Name |
Application |
Reactivity |
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- HY-P82871
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ACH4; AChR; Acra4; BFNC; CHRNA4; EBN; EBN1; nAChR; NACRA4
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WB, IP
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Human, Mouse, Rat |
Cat. No. |
Product Name |
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Classification |
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- HY-107681
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Alkynes
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SIB-1508Y is an orally active and selective nAChR agonist. SIB-1508Y has the potential to study parkinsonism . SIB-1508Y is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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