SML3913
VU0486846
≥98% (HPLC)
Synonym(s):
VU-0486846, (2R)-3,4-Dihydro-N-[(1S,2S)-2-hydroxycyclohexyl]-4-[[4-(1H-pyrazol-1-yl)phenyl]methyl]-2H-1,4-benzoxazine-2-carboxamide, (2R)-N-[(1S,2S)-2-Hydroxycyclohexyl]-4-[(4-pyrazol-1-ylphenyl)-methyl]-2,3-dihydro-1,4-benzoxazine-2-carboxamide, VU 0486846
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About This Item
Empirical Formula (Hill Notation):
C25H28N4O3
CAS Number:
Molecular Weight:
432.51
NACRES:
NA.77
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally active, CNS-penetrant, muscarinic acetylcholine receptor M1-selective positive allosteric modulator (PAM) without agonist activity or adverse cholinergic toxicity.
VU0486846 is an orally active, CNS-penetrant and highly selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) with little agonist activity (rat M1 EC50 = 230 nM, 93% ACh max; agonist EC50 > 10 μM) or adverse cholinergic toxicity. VU0486846 improves pathology and cognitive deficits in female APPswe/PSEN1ΔE9 mice (10 mg/day via drinking water), as well as enhances recognition memory and reverses 3 mg/kg risperidone-induced deficits in acquisition of contextual fear conditioning in rats in vivo (3-10 mg/kg i.p.).
VU0486846 is an orally active, CNS-penetrant and highly selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) with little agonist activity (rat M1 EC50 = 230 nM, 93% ACh max; agonist EC50 > 10 μM) or adverse cholinergic toxicity. VU0486846 improves pathology and cognitive deficits in female APPswe/PSEN1ΔE9 mice (10 mg/day via drinking water), as well as enhances recognition memory and reverses 3 mg/kg risperidone-induced deficits in acquisition of contextual fear conditioning in rats in vivo (3-10 mg/kg i.p.).
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity
ACS Chemical Neuroscience, 9(9), 2274-2285 (2018)
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core
Bioorganic & Medicinal Chemistry Letters, 28(12), 2175-2179 (2018)
M1 muscarinic receptor activation reduces the molecular pathology and slows the progression of prion-mediated neurodegenerative disease
Science Signaling, 15(760) (2022)
Khaled S Abd-Elrahman et al.
British journal of pharmacology, 179(8), 1769-1783 (2021-11-26)
Alzheimer's disease (AD) is a neurodegenerative disease characterized by progressive cognitive decline, and women account for 60% of diagnosed cases. β-Amyloid (Aβ) oligomers are considered the principal neurotoxic species in AD brains. The M1 muscarinic ACh receptor (M1 mAChR) plays
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