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Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinicacetylcholinereceptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinicM1, M2, and M3receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinicM1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
Biperiden (KL 373) is a non-selective muscarinicreceptor antagonist that competitively binds to M1muscarinicreceptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinicacetylcholinereceptor and a M1receptor agonist (EC50: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
Trihexyphenidyl hydrochloride is a selective and orally active M1muscarinicreceptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1muscarinicreceptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
Biperiden (KL 373) hydrochloride is a non-selective muscarinicreceptor antagonist that competitively binds to M1muscarinicreceptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR(muscarinicacetylcholinereceptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinicacetylcholinereceptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
Pirenzepine (LS 519 free base) is a selective M1 mAChR(muscarinicacetylcholinereceptor) antagonist, with poor penetration of the blood-brain barrier. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinicM1receptor gene expression and muscarinicM1receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
TAK-071 is a novel, potent and highly selective muscarinicacetylcholinereceptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM .
PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1muscarinicacetylcholinereceptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca 2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .
MK-7622 (M1receptor modulator) is an orally active positive allosteric modulator of muscarinicM1acetylcholinereceptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1receptors (EC50 = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD) .
Iperoxo is a potent superagonist of muscarinicacetylcholinereceptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinicreceptors when labeled with tritium .
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1muscarinicacetylcholinereceptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia .
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinicM1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinicM1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline can cross the blood-brain barrier (BBB) .
Aceclidine (Quinuclidin-3-yl acetate) hydrochloride is a modulator of M3 muscarinicacetylcholinereceptor and a M1receptor agonist (EC50: 40 μM). Aceclidine hydrochloride is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine hydrochloride has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .
Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinicacetylcholineM4receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
Tiotropium bromide monohydrate (BA-679 BR monohydrate) is a long-acting anticholinergic bronchodilator. Tiotropium bromide monohydrate blocks the action of acetylcholine at muscarinicM1, M2, and M3receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide monohydrate is applicable to research related to chronic obstructive pulmonary disease and asthma .
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinicM1, M2, and M3receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
Scotanamine D (N1-Dihydrocaffeoyl, N10-caffeoyl spermidine) is a spermidine alkaloid. It can be isolated from S. tangutica. Scotanamine D potently and selectively inhibits the activity of the M1muscarinicacetylcholinereceptor, with an IC50 of 32 nM. It can be used in studies related to Parkinson's disease .
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinicreceptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
VU6008055 (AF98943) is a brain-penetrant, orally active and selective muscarinicacetylcholinereceptor subtype 4 (mAChR4) activator with human EC50 values of 73.4 nM. VU6008055 potentiates mAChR4receptor activity in the presence of acetylcholine, and exhibits no activity at mAChR1, mAChR3, or mAChR5. VU6008055 can be used for the research of schizophrenia, parkinson’s disease, alzheimer’s disease .
AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease .
Isopteropodine is a positive modulator that selectively acts on muscarinicM1 and 5-HT2receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
PF-06764427 is a selective M1muscarinicacetylcholinereceptor positive allosteric modulator. PF-06764427 exhibits robust M1 agonist activity. PF-06764427 can be used in the research of Alzheimer's disease and schizophrenia .
Trihexyphenidyl is a selective and orally active M1muscarinicreceptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1muscarinicreceptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
Cycrimine is an orally active muscarinic cholinergic receptor (mAChR) M1 antagonist, reduces the acetylcholine levels in parkinson model. Cycrimine shows antispasmodic activity, can be used in studies of behavioral and mental disorder .
4-Bromo-2-hydroxypyridine is an intermediate. 4-Bromo-2-hydroxypyridine can be used to synthesize M1muscarinicacetylcholinereceptor(M1 mAChR) positive allosteric modulators. 4-Bromo-2-hydroxypyridine can be used in the research of Alzheimer's disease and schizophrenia .
Biperiden (hydrochloride) (Standard) is the analytical standard of Biperiden (hydrochloride). This product is intended for research and analytical applications. Biperiden (KL 373) hydrochloride is a non-selective muscarinicreceptor antagonist that competitively binds to M1muscarinicreceptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Biperiden (KL 373) lactate is an orally active non-selective muscarinicreceptor antagonist that competitively binds to M1muscarinicreceptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders .
VU0238441 is a pan muscarinicacetylcholinereceptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinicM1, M2, and M3receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinicacetylcholinereceptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
M1 ligand 1 (compound 3b-b) is a muscarinicacetylcholinereceptorM1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer .
HTL-9936 is a selective M1muscarinicacetylcholinereceptor(M1-mAChR) agonist. HTL-9936 is promising for research of neurodegenerative disorders (e.g., Alzheimer’s) .
VU0415248 is a selective muscarinicacetylcholinereceptor 1 (M1) inhibitor. VU0415248 inhibits acetylcholine-induced calcium mobilization in cells expressing human and rat M1muscarinicacetylcholinereceptors, with an IC50 of 0.4 and 0.18 μM, respectively. VU0415248 is applicable to the research of Parkinson's disease, movement disorders and fragile X syndrome .
VU6007678 is a CNS-penetrant muscarinicacetylcholinereceptor (mAChR) modulator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5muscarinicacetylcholinereceptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke .
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinicacetylcholinereceptorsM1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.
VU0090157 is a positive allosteric modulator (PAM) of the M1muscarinicacetylcholinereceptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .
Atropine Oxide (Atropine oxidation) hydrochloride, a derivative of Atropine, acts as a competitive antagonist to the muscarinicacetylcholinereceptorsM1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings .
Trihexyphenidyl-d5 is deuterium labeled Trihexyphenidyl (HY-B1277A). Trihexyphenidyl is a selective and orally active M1muscarinicreceptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1muscarinicreceptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
Trihexyphenidyl-d5 hydrochloride is deuterium labeled Trihexyphenidyl hydrochloride (HY-B1277). Trihexyphenidyl hydrochloride is a selective and orally active M1muscarinicreceptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1muscarinicreceptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
VU0357017 (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1muscarinicacetylcholinereceptor, with an EC50 of 477 nM. VU0357017 is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 can be used for the research of Alzheimer’s disease and schizophrenia .
Trihexyphenidyl hydrochloride (Standard) is the analytical standard of Trihexyphenidyl hydrochloride (HY-B1277). This product is intended for research and analytical applications. Trihexyphenidyl is a selective and orally active M1muscarinicreceptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1muscarinicreceptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
Biperiden (Standard) is the analytical standard of Biperiden. This product is intended for research and analytical applications. Biperiden (KL 373) is a non-selective muscarinicreceptor antagonist that competitively binds to M1muscarinicreceptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Thiochrome (Standard) is the analytical standard of Thiochrome. This product is intended for research and analytical applications. Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinicreceptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors .
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinicreceptor antagonist that competitively binds to M1muscarinicreceptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Pirenzepine (dihydrochloride) (Standard) is the analytical standard of Pirenzepine (dihydrochloride). This product is intended for research and analytical applications. Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinicacetylcholinereceptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
Pirenzepine (Standard) is the analytical standard of Pirenzepine. This product is intended for research and analytical applications. Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinicacetylcholinereceptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
NNC 11-1607 is a selective M1/M4muscarinicacetylcholinereceptor (mAChR) agonist. NNC 11-1607 inhibits Forskolin (HY-15371)-stimulated cAMP accumulation in Chinese hamster ovary cells expressing the human M2 or M4 mAChR. NNC 11-1607 is promising for research of central nervous system disorders, such as Alzheimer’s disease and schizophrenia .
Cevimeline (hydrochloride) (Standard) is the analytical standard of Cevimeline (hydrochloride). This product is intended for research and analytical applications. Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinicM1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .
Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinicM1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinicM1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR(muscarinicacetylcholinereceptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
Tiotropium (Bromide) (Standard) is the analytical standard of Tiotropium (Bromide). This product is intended for research and analytical applications.
Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinicM1, M2, and M3receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinicacetylcholinereceptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinicM1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .
Clemastine (HS-592; Meclastine)-d5 fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinicacetylcholinereceptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinicacetylcholinereceptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinicacetylcholinereceptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinicM1 and 5-HT2receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
MIPS1455 is a light-activated M1muscarinicacetylcholinereceptor ligand with irreversible binding activity to the allosteric site of the receptor. MIPS1455 is a drug target under investigation for the suppression of cognitive deficits and may become a valuable molecular tool for further investigation of allosteric interactions of the receptor .
Vedaclidine is an orally active muscarinicacetylcholinereceptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinicM1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinicreceptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states .
(R)-PAD-PF2 is an isomer of PAD-PF2 (HY-176710). PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1muscarinicacetylcholinereceptor antagonist (IC50 = 12.3 μM).
Cevimeline (hydrochloride hemihydrate) (Standard) is the analytical standard of Cevimeline (hydrochloride hemihydrate). This product is intended for research and analytical applications. Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinicM1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .
VU6052254, a derivative of VU0467319 (HY-173396), is a selective, potent, orally active and brain-penetrant muscarinicM1acetylcholinereceptor (mAChR1) positive allosteric modulator with an EC50 of 59 nM. VU6052254 has no activity on the M2-5 receptor (EC50 > 30 μM). VU6052254 can improve memory recognition ability and reverse the cognitive impairment induced by Scopolamine (HY-N0296) with minimum effective dose both of 1 mg/kg. VU6052254 can be used for the research of neurological disease, such as Alzheimer's disease .
M3 mAChR agonist 1 is an M3-preferring M3/M5 mAChR dual positive allosteric modulators (PAM). M3 mAChR agonist 1 shows excellent subtype selectivity over other subtypes of mAChRs including M1, M2, and M4 mAChRs. M3 mAChR agonist 1 increases the contraction of isolated rat bladder strips by modulating the M3muscarinicacetylcholinereceptor, leading to enhanced signaling pathways. M3 mAChR agonist 1 can be used for the research of endocrinology .
4-Bromo-2-hydroxypyridine is an intermediate. 4-Bromo-2-hydroxypyridine can be used to synthesize M1muscarinicacetylcholinereceptor(M1 mAChR) positive allosteric modulators. 4-Bromo-2-hydroxypyridine can be used in the research of Alzheimer's disease and schizophrenia .
Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) is a potent amyloid β (Aβ) inhibitor. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases the expression of acetylcholine (ACh) levels, choline acetyltransferase (ChAT) activity, and ChAT gene induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) decreases in acetyl cholinesterase (AChE) activity and AChE gene expression induced by Aβ (1-42). Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) increases muscarinicM1receptor gene expression and muscarinicM1receptor binding activity. Fustinis ((±)-Fustin; 3,7,3',4'-Tetrahydroxyflavanone) can be used for Alzheimer's disease research .
Scotanamine D (N1-Dihydrocaffeoyl, N10-caffeoyl spermidine) is a spermidine alkaloid. It can be isolated from S. tangutica. Scotanamine D potently and selectively inhibits the activity of the M1muscarinicacetylcholinereceptor, with an IC50 of 32 nM. It can be used in studies related to Parkinson's disease .
Isopteropodine is a positive modulator that selectively acts on muscarinicM1 and 5-HT2receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinicM1 and 5-HT2receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .
CHRM1, the muscarinic acetylcholine receptor, mediates cellular responses, including adenylate cyclase inhibition, phosphoinositide breakdown, and potassium channel modulation through G protein actions.It engages with GPRASP2 and TMEM147, contributing to a complex network of signaling pathways and cellular processes regulated by the receptor.CHRM1 Protein, Rat (His) is the recombinant rat-derived CHRM1 protein, expressed by E.coli , with N-6*His labeled tag.
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinicM1, M2, and M3receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium bromide (BA-679 BR) is a long-acting anticholinergic bronchodilator. Tiotropium bromide blocks the action of acetylcholine at muscarinicM1, M2, and M3receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide is applicable to research related to chronic obstructive pulmonary disease and asthma .
Trihexyphenidyl-d5 is deuterium labeled Trihexyphenidyl (HY-B1277A). Trihexyphenidyl is a selective and orally active M1muscarinicreceptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1muscarinicreceptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease. .
Trihexyphenidyl-d5 hydrochloride is deuterium labeled Trihexyphenidyl hydrochloride (HY-B1277). Trihexyphenidyl hydrochloride is a selective and orally active M1muscarinicreceptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1muscarinicreceptors. Trihexyphenidyl hydrochloride modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl hydrochloride improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl hydrochloride can be used for the research of Parkinson's disease. .
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinicreceptor antagonist that competitively binds to M1muscarinicreceptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR(muscarinicacetylcholinereceptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
Pirenzepine-d11 (LS 519 (free base)-d11; Pirenzepin-d11; Gastrozepin-d11) is the deuterium labeled Pirenzepine (HY-17037A). Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinicacetylcholinereceptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
Clemastine (HS-592; Meclastine)-d5 fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinicacetylcholinereceptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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