mAChR Modulator
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Desalkylquazepam
0 ImagesCat. No.: HY-W664824CAS No.: 1645-32-5Synonyms: N-DesmethylquazepamDesalkylquazepam (Compound 23; N-Desmethylquazepam) is a precursor in the synthesis of triazolobenzodiazepines. Desalkylquazepam is a mAChR modulator (EC 50 = 0.317 µM).
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VU6002703
0 ImagesCat. No.: HY-171981CAS No.: 1934241-32-3VU6002703 (Compound 17) is a BBB-penetrable M4 mAChR positive allosteric modulator (PAM) with an EC50 of 0.6 μM for hM4. VU6002703 can be used for neuropsychiatric and rare genetic CNS disorders research.
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Vedaclidine
0 ImagesCat. No.: HY-183144CAS No.: 141575-50-0Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states.
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VU6052254
0 ImagesCat. No.: HY-180143CAS No.: 3035701-02-8VU6052254, a derivative of VU0467319 (HY-173396), is a selective, potent, orally active and brain-penetrant muscarinic M1 acetylcholine receptor (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.
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M1 mAChR modulator-1
0 ImagesCat. No.: HY-177498CAS No.: 2247999-07-9
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(E/Z)-VU0029767
0 ImagesCat. No.: HY-119082CAS No.: 326001-01-8(E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
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DC-98-LC74
0 ImagesCat. No.: HY-188044DC-98-LC74 is a selective modulator of adult skeletal muscle-type nicotinic acetylcholine receptor (α1β1δε), with an EC50 value of 6.5 µM for the human receptor and an IC50 of 13.45 µM for the human α3β4 nicotinic acetylcholine receptor. DC-98-LC74 increases the ligand-free opening probability of the receptor via the ε subunit M2-M3 loop, and prolongs the burst duration and opening probability of wild-type and fast-channel mutant AChR. DC-98-LC74 exerts weak effects on neuronal AChR subtypes and has no agonist activity. DC-98-LC74 prolongs the mouse diaphragm endplate current and improves muscle contractility in isolated neuromuscular preparations from sarcopenic mice. DC-98-LC74 can be used for studies on neuromuscular junction function and myasthenia-related diseases.
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PTAC oxalate
0 ImagesCat. No.: HY-107656CAS No.: 201939-40-4PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects.
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Muscarinic M4 modulator-1
0 ImagesCat. No.: HY-174259CAS No.: 3082186-91-9Muscarinic M4 modulator-1 is a Muscarinic M4 receptor positive allosteric modulator. Muscarinic M4 modulator-1 activates the muscarinic M4 receptor with allosteric potency EC50 s of 14 and 3 Nm in CHO-K1 cells and HEK293 cells. Muscarinic M4 modulator-1 has an antipsychotic-like activity, promising for psychiatric and/or neurological disorders research.
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ML169
0 ImagesCat. No.: HY-120576CAS No.: 1222878-02-5Synonyms: VU0405652ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease.
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M1R modulator-1
0 ImagesCat. No.: HY-183487CAS No.: 2257498-40-9M1R modulator-1 is an orally effective positive allosteric modulator of muscarinic M1R, with an IP value of 0.88 nM. M1R modulator-1 can be used in constipation-related research.
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M4 mAChR Modulator-1
0 ImagesCat. No.: HY-159177M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment.
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Lu 26-046
0 ImagesCat. No.: HY-120329CAS No.: 143756-51-8Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats.
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VU6009048
0 ImagesCat. No.: HY-180421CAS No.: 2226116-93-2VU6009048 is a CNS-penetrant human M4 muscarinic acetylcholine receptor (mAChR4) positive allosteric modulator. VU6009048 can be used for the research of parkinson’s disease, huntington’s disease, schizophrenia.
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VU0029767
0 ImagesCat. No.: HY-119082ACAS No.: 1134973-88-8VU0029767 is an allosteric enhancer of the M1 muscarinic receptor with the activity to modulate M1 receptor activity. VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
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MK-97
0 ImagesCat. No.: HY-184172CAS No.: 2102194-98-7Synonyms: Merck-97MK-97 (Merck-97) is an M4 mAChR positive allosteric modulator. MK-97 can be used for the research of neurological disorders.
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Clozapine dihydrochloride
0 ImagesCat. No.: HY-14539BCAS No.: 2711603-38-0Synonyms: HF 1854 dihydrochlorideClozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
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VU0090157
0 ImagesCat. No.: HY-128783CAS No.: 312622-77-8VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (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.
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PF-06764427
0 ImagesCat. No.: HY-123852CAS No.: 1842371-08-7PF-06764427 is a selective M1 muscarinic acetylcholine receptor positive allosteric modulator. PF-06764427 exhibits robust M1 agonist activity. PF-06764427 can be used in the research of Alzheimer's disease and schizophrenia.
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Clozapine-d3
0 ImagesCat. No.: HY-14539S3CAS No.: 1215691-72-7Synonyms: HF 1854-d3Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
