SML0777
Oltipraz metabolite M2
≥98% (HPLC)
别名:
7-Methyl-6,8-bis(methylthio)-pyrrolo[1,2-a]pyrazine
SMILES string
S(C)c1[n]2c(c(c1C)SC)C=NC=C2
InChI
1S/C10H12N2S2/c1-7-9(13-2)8-6-11-4-5-12(8)10(7)14-3/h4-6H,1-3H3
InChI key
MYLBTCQBKAKUTJ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
protect from light
color
white to light brown
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
M2 is a metabolite of the chemopreventive agent oltipraz. Oltipraz metabolite M2 has been shown to inhibit liver steatosis by inhibiting lipogenesis and enhancing mitochondrial function, including fuel oxidation. Oltipraz metabolite M2 acts as a potent inhibitor of LXRa transcriptional activity, and also AMPK activator inducing the phosphorylation of AMPK.
M2 is a metabolite of the chemopreventive agent oltipraz; LXRa inhibitor; AMPK activator.
Features and Benefits
This compound is featured on the AMPKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Other Notes
Light sensitive and air sensitive.
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
H J Prochaska et al.
Molecular pharmacology, 48(1), 15-20 (1995-07-01)
Oltipraz, an inhibitor of human immunodeficiency virus type 1 replication in vitro (ED50 approximately 10 microM), undergoes extensive metabolism in vivo. Most of the orally administered drug undergoes opening of the dithiolethione ring, reduction, recyclization, and methylation to form 7-methyl-6,8-bis(methylthio)pyrrolo[1,2-a]pyrazine
S G Kim et al.
Clinical pharmacology and therapeutics, 88(3), 360-368 (2010-07-29)
Oltipraz is a potential candidate drug for the treatment of liver fibrosis (LF) and liver cirrhosis (LC). The pharmacokinetics of oltipraz and its major rearranged metabolite (7-methyl-6,8-bis(methylthio)H-pyrrolo[1,2-a]pyrazine (RM)) were evaluated after single-dose (30-90 mg) and multiple-dose (60 mg b.i.d. or
商品
The AMP-activated protein kinase (AMPK) acts as a sensor of cellular energy status. AMPK exists as heterotrimeric complexes comprising a catalytic α subunit and regulatory β and γ subunits.
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