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SML3960

Sigma-Aldrich

JNJ-42226314

≥98% (HPLC)

Synonym(s):

[1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, [4-[1-[[1-(4-Fluorophenyl)-1H-indol-5-yl]carbonyl]-3-azetidinyl]-1-piperazinyl]-2-thiazolylmethanone

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About This Item

Empirical Formula (Hill Notation):
C26H24FN5O2S
CAS Number:
1252765-13-1
Molecular Weight:
489.56
MDL number:
MFCD32671350
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

Brain penetrant, highly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL).


JNJ-42226314 is a brain penetrant, highly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL)(IC50 = 1.1) that exhibits antinociceptive efficacy in the rat models neuropathic and inflammatory pain. JNJ-42226314 elevates hippocampal 2-arachidonoylglycerol (2-AG) levels and prolongs wakefulness in rats.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors
Bioorganic & Medicinal Chemistry Letters, 30(14), 127243-127243 (2020)
Ryan M Wyatt et al.
The Journal of pharmacology and experimental therapeutics, 372(3), 339-353 (2019-12-11)
The serine hydrolase monoacylglycerol lipase (MAGL) is the rate-limiting enzyme responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) into arachidonic acid and glycerol. Inhibition of 2-AG degradation leads to elevation of 2-AG, the most abundant endogenous agonist of the

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