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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
31 Results for "
human M1 receptors
" in MedChemExpress (MCE) Product Catalog:
Products (31)
31 Results for "human M1 receptors" in MCE Product Catalog:
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Tiotropium bromide monohydrate (BA-679 BR monohydrate) is a long-acting anticholinergic bronchodilator. Tiotropium bromide monohydrate blocks the action of acetylcholine at muscarinic M1, M2, and M3 receptors, prevents bronchoconstriction, and dilates bronchial airways. Tiotropium bromide monohydrate is applicable to research related to chronic obstructive pulmonary disease and asthma .
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2 Cited Publications
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PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
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1 Cited Publications
Synonyms: M1 receptor modulator
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MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (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) .
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1 Cited Publications
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VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells .
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1 Cited Publications
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PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease .
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3,5-Diiodothyropropionic acid is a thyroid hormone analog, induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (TR), with Ka of 2.40 and 4.06 M -1 for TRα1 and TRβ1, respectively. 3,5-Diiodothyropropionic acid promotes angiogenesis in 3-D human dermal microvascular endothelial cell sprouting assay. 3,5-Diiodothyropropionic acid prevents myocardial arteriolar loss in thyroidectomized rats and enhances cardiac energy-generating capacity in postinfarction heart failure rats. 3,5-Diiodothyropropionic can be used in studies related to angiogenesis and heart failure .
Cat. No.: HY-P99313
CAS No.: 1228538-47-3
Synonyms: Anti-human IGHE Recombinant Antibody; 47H4; MEMP1972A
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Quilizumab (Anti-Human IGHE Recombinant Antibody; 47H4; MEMP1972A) is a monoclonal antibody that targets FcγRIIIa and the M1 prime segment of human membrane-bound IgE. Quilizumab has enhanced FcγRIIIa binding affinity and activity against IgE class-switched B cells, and reduces serum IgE levels by inducing antibody-dependent cell-mediated cytotoxicity and apoptosis through cross-linking of membrane-bound IgE receptors. Quilizumab depletes IgE-producing cells; it also directly binds the membrane-bound M1 prime domain on IgE class-switched cells to inhibit IgE production. Quilizumab is used in research on allergic asthma and allergic diseases (asthma, allergic rhinitis) .
Cat. No.: HY-118363
CAS No.: 1186229-95-7
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Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS) .
Cat. No.: HY-173396
CAS No.: 1432438-14-6
Synonyms: VU319
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VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC50: 492 nM). VU0467319 is selective (EC50 > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research .
Synonyms: WAL 2014 FU free base
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Talsaclidine (WAL 2014 FU) is an orally active, blood-brain barrier-permeable muscarinic M1 receptor agonist. Talsaclidine activates the sympathetic nervous system and promotes adrenal catecholamine release in vivo. Talsaclidine exhibits extensive tissue distribution, kidney-dominant excretion and brain penetration properties, and it can be used in studies related to cholinergic signaling, cognitive function and Alzheimer's disease .
Cat. No.: HY-145491
CAS No.: 578008-43-2
Cat. No.: HY-118806A
CAS No.: 447407-36-5
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AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .
Cat. No.: HY-118356
CAS No.: 144177-32-2
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WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
Cat. No.: HY-U00302
CAS No.: 1004312-94-0
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CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .
Cat. No.: HY-148961
CAS No.: 1438242-59-1
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HTL-9936 is an orally active partial agonist of muscarinic M1 receptor. HTL-9936 has an EC50 of 32 nM for human M1 receptor and an EC50 of 224 nM for human M4 receptor. HTL-9936 activates Gq/11 coupling, promotes inositol phosphate accumulation, ERK1/2 phosphorylation, β-arrestin recruitment and receptor internalization. HTL-9936 can be used in the research of Alzheimer's disease and schizophrenia .
Cat. No.: HY-118806
CAS No.: 244291-63-2
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AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
Cat. No.: HY-184057
CAS No.: 34099-70-2
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M1 receptor modulator-1 is a low-efficacy positive allosteric modulator of the muscarinic M1 receptor (mAChR1), with an EC50 of 71 nM for the human M1 receptor. M1 receptor modulator-1 enables use-dependent attenuation of neurotransmitter signals and exhibits excellent in vivo properties without pseudo-agonist activity. M1 receptor modulator-1 can be used in research related to Alzheimer's disease and schizophrenia .
Cat. No.: HY-117953
CAS No.: 155180-53-3
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RU 59063 is a high-affinity, selective nonsteroidal androgen receptor (AR) ligand that acts as a partial AR agonist/antagonist in CV-1 cell transcription assays. RU 59063 has a Ka value of 6.2×10 9 M -1 for human AR. RU 59063 induces a conformation of AR that can bind to the androgen response element (ARE), triggers partial AR-dependent transcriptional activation, and antagonizes testosterone-induced AR transcriptional activity. RU 59063 inhibits testosterone propionate-induced ornithine decarboxylase activity in mouse kidneys and testosterone propionate-induced prostate weight gain in rats. RU 59063 can be used in studies related to prostate cancer .
Cat. No.: HY-P11298
CAS No.: 2120397-85-3
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Cat. No.: HY-119333
CAS No.: 250649-13-9
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NNC 11-1607 is a selective M1/M4 muscarinic acetylcholine receptor (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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
