V4515
VU0238429
solubility: ≥20 mg/mL in DMSO
Synonym(s):
1-[(4-Methoxyphenyl)methyl]-5-(trifluoromethoxy)-1H-indole-2,3-dione
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About This Item
Empirical Formula (Hill Notation):
C17H12F3NO4
CAS Number:
Molecular Weight:
351.28
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
assay
≥98% (HPLC)
Quality Level
form
powder
color
orange
solubility
DMSO: ≥20 mg/mL
storage temp.
2-8°C
SMILES string
COc1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc23)cc1
InChI
1S/C17H12F3NO4/c1-24-11-4-2-10(3-5-11)9-21-14-7-6-12(25-17(18,19)20)8-13(14)15(22)16(21)23/h2-8H,9H2,1H3
InChI key
CKLGZXFOLMHCMC-UHFFFAOYSA-N
Biochem/physiol Actions
VU0238429 is a selective muscarinic acetylcholine receptor 5 (M5) positive allosteric modulator; causes leftward shift in acetylcholine potency.
VU0238429 is a selective muscarinic acetylcholine receptor 5 (M5) positive allosteric modulator; causes leftward shift in acetylcholine potency. M5 is thought to regulate cerebral blood flow, and activation of M5 may be therapeutic for Alzheimer′s disease. VU0238429 is the first reported M5-selective small molecule of any kind. It is >30-fold more selective for M5 over M1, M2, M3, and M4.
Features and Benefits
This compound is featured on the Acetylcholine Receptors (Muscarinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
signalword
Warning
hcodes
Hazard Classifications
Aquatic Acute 1 - Eye Irrit. 2
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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Muscarinic receptors 2 and 5 regulate bitter response of urethral brush cells via negative feedback.
Klaus Deckmann et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 32(6), 2903-2910 (2018-02-07)
We have recently identified a cholinergic chemosensory cell in the urethral epithelium, urethral brush cell (UBC), that, upon stimulation with bitter or bacterial substances, initiates a reflex detrusor activation. Here, we elucidated cholinergic mechanisms that modulate UBC responsiveness. We analyzed