SML2728
ML375
≥98% (HPLC)
Synonym(s):
(S)-9b-(4-Chlorophenyl)-1-(3,4-difluorobenzoyl)-1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-one, (S)-9b-(4-Chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one, ML 375, VU0483253
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About This Item
Empirical Formula (Hill Notation):
C23H15ClF2N2O2
CAS Number:
Molecular Weight:
424.83
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -150 to -175, c = 0.5 in chloroform-d
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
Fc1c(ccc(c1)C(=O)N2[C@]4(N(CC2)C(=O)c5c4cccc5)c3ccc(cc3)Cl)F
InChI key
GXBAKXRLQAPKEE-QHCPKHFHSA-N
Biochem/physiol Actions
ML375 is an orally active, brain-penetrant, potent and M5 subtype-selective muscarinic acetylcholine receptor (mAChR) negative allosteric modulator (NAM) (IC50 = 300/790 nM against 10 μM NMS-induced Ca2+ mobilization in h/r M5-transfected CHO cells; h/r M1-M4 IC50 >30 μM) that reduces N-methylscopolamine (NMS) ML5 dissociation rate without competing against NMS for receptor binding. M375 shows in vivo efficacy in rat models of substances addiction (cocaine, ethanol, oxycodone) with excellent multispecies pharmacokinetic properties.
Orally active, brain-penetrant, potent & M5-selective muscarinic acetylcholine receptor (mAChR) NAM with in vivo efficacy in rat models of substances addiction.
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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