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TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases .
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's 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)2β2EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit .
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice .
Zaurategrast ethyl ester (CDP323), the ethyl ester proagent of CT7758 , is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders .
Zaurategrast ethyl ester sulfate (CDP323 sulfate), the ethyl ester proagent of CT7758 , is a α4β1/α4β7 integrin antagonist used for the treatment of inflammatory and autoimmune disorders .
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity .
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 .
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM .
REDV is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV can be used for the research of cell adhesion .
REDV TFA is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV TFA can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV TFA can be used for the research of cell adhesion .
Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containingnicotinic acetylcholine receptor (nAChR) antagonist .
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 .
Abrilumab is a fully human monoclonal antibody directed against α4β7. Abrilumab selectively binds the α4β7 integrin heterodimer. Abrilumab can be used for the research of inflammatory bowel disease (IBD) .
Valategrast hydrochloride (R-411) is a potent integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast hydrochloride has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment .
Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment .
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2) .
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 .
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 .
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
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 .
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 .
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 .
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 .
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn 2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity .
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .
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 .
Natalizumab is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses .
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 .
PVZB1194 is a biphenyl-type inhibitor of Kinesinspindle proteinEg5 or KIF11. Eg5 is related to the cell cycle, and Eg5 inhibition can lead to cell cycle arrest and apoptosis. PVZB1194 exhibits anticancer potential via inhibiting Eg5 ATPase activity. PVZB1194 binds to the α4/α6 allosteric pocket, and shows ATP competetive activity .
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 .
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 .
(±)-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) .
Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with Ki values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD) .
Natalizumab (Solution) is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses .
Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression .
Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research [4].
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .
EILEVPST is a recombinant human fibronectinderived low-molecular-weight peptide fragment. EILEVPST can promote cell type-specific α4 integrin-mediated adhesion. EILEVPST can be used for the research of thrombogenesis .
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 .
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 [4] .
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 [4] .
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 [4] .
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 .
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 [4] .
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity .
(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 .
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 .
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 .
Tebanicline, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
Benzethonium (chloride) (Standard) is the analytical standard of Benzethonium (chloride). This product is intended for research and analytical applications. Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes.
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 .
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 .
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 .
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 .
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 .
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 .
Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype,Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .
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 .
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease .
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 .
R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful high affinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity .
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
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 .
(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 [4].
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 .
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 .
Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells .
(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 .
(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 .
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) .
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied [4].
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 .
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 .
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
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 [4].
MorHap is a heroin hapten. MorHap conjugated to tetanus toxoid (TT), palm-CV2, and to monophosphoryl lipid A (MPLA)-containing liposomes partially blocks heroin-induced analgesia and hyperlocomotion in mice. MorHap designed conjugates also significantly inhibits HIV-1 binding to α4β7 receptors. MorHap can be used in research to develop vaccines related to heroin addiction and HIV-1 infection .
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].
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].
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 .
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) .
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid agent .
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 .
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 .
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 .
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2 .
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 .
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
PI5P4Ks-IN-2 is a inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ(PI5P4Kγ). PI5P4Ks-IN-2 targets to PI5P4K isoforms with pIC50 values of <4.3 (PI5P4Kα), <4.6 (PI5P4Kβ), 6.2 (PI5P4Kγ), 0.32 (PI5P4Kγ+), respectively .
REDV TFA is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV TFA can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV TFA can be used for the research of cell adhesion .
REDV is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV can be used for the research of cell adhesion .
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn 2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity .
EILEVPST is a recombinant human fibronectinderived low-molecular-weight peptide fragment. EILEVPST can promote cell type-specific α4 integrin-mediated adhesion. EILEVPST can be used for the research of thrombogenesis .
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 .
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 .
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease .
Natalizumab is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses .
Abrilumab is a fully human monoclonal antibody directed against α4β7. Abrilumab selectively binds the α4β7 integrin heterodimer. Abrilumab can be used for the research of inflammatory bowel disease (IBD) .
Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with Ki values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD) .
Natalizumab (Solution) is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses .
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 .
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 .
Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells .
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 .
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) .
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) .
IFN-alpha 4 (IFNA4), belongs to type I interferon family, is produced by macrophages with antiviral activities. IFN-alpha 4 Protein, Cynomolgus (HEK293, Fc) contains 189 a.a. (M1-N189), produced in HEK293 cells with a C-terminal mFc-tag.
IFN-alpha 4 (IFNA4), belongs to type I interferon family, is produced by macrophages with antiviral activities. IFN-alpha 4/IFNA4 Protein, Mouse (HEK293, His) contains 162 a.a. (C25-E186), produced in HEK293 cells with a C-terminal His-tag.
The CNGA4 protein is a regulatory subunit of cation-selective cyclic nucleotide-gated (CNG) channels in olfactory sensory neurons that responds to cAMP to induce depolarization. This critical role in odorant signal transduction and adaptation enhances neural responses to olfactory stimulation. CNGA4 Protein, Human (Cell-Free, His, SUMO) is the recombinant human-derived CNGA4 protein, expressed by E. coli Cell-free , with N-6*His, N-SUMO labeled tag. The total length of CNGA4 Protein, Human (Cell-Free, His, SUMO) is 575 a.a., with molecular weight of 82 kDa.
IFN-alpha 4 (IFNA4), belongs to type I interferon family, is produced by macrophages with antiviral activities. IFN-alpha 4/IFNA4 Protein, Rat (HEK293, Fc) contains 166 a.a. (C24-K189), produced in HEK293 cells with a N-terminal hFc-tag.
IFN-alpha 4 (IFNA4), belongs to type I interferon family, is produced by macrophages with antiviral activities. IFN-alpha 4/IFNA4 Protein, Human (HEK293, Fc) contains 166 a.a. (C24-D189), produced in HEK293 cells with a N-terminal hFc-tag.
IFN-alpha 4 (IFNA4), belongs to type I interferon family, is produced by macrophages with antiviral activities. IFN-alpha 4/IFNA4 Protein, Human (sf9, His) contains 189 a.a. (M1-D189), produced in Sf9 insect cells cells with a C-terminal His-tag.
IFN-alpha 4 (IFNA4), belongs to type I interferon family, is produced by macrophages with antiviral activities. IFN-alpha 4/IFNA4 Protein, Human (HEK293, His) contains 166 a.a. (C24-D189), produced in HEK293 cells cells with a C-terminal His-tag.
TPM4 protein, binding actin filaments in muscle and non-muscle cells, crucially regulates calcium-dependent muscle contraction, aided by the troponin complex in vertebrates. In smooth muscle cells, TPM4 interacts with caldesmon, contributing to contraction regulation. In non-muscle cells, it stabilizes actin filaments in the cytoskeleton. TPM4's calcium-binding ability, homodimer, and heterodimer formation (with alpha and beta chains) showcase its versatile molecular configurations. TPM4's multifaceted interactions emphasize its essential roles in muscle contraction and cytoskeletal dynamics across diverse cellular contexts. TPM4 Protein, Human (HEK293, His) is the recombinant human-derived TPM4 protein, expressed by HEK293, with N-His, N-6*His labeled tag. The total length of TPM4 Protein, Human (HEK293, His) is 247 a.a., with molecular weight of 35-40 kDa.
Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
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].
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].
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 .
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.