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Merck
CN

SML4188

E17241

≥98% (HPLC), powder, pan-PPAR agonist

Synonym(s):

4-(1,3-Dithiolan-2-yl)-N-(3-hydroxy-2-pyridinyl)benzamide, 4-(1,3-Dithiolan-2-yl)-N-(3-hydroxypyridin-2-yl)benzamide, E 17241, E-17241

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About This Item

Empirical Formula (Hill Notation):
C15H14N2O2S2
CAS Number:
Molecular Weight:
318.41
MDL number:
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Technical Service
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Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Application

E17241 may be used to explore its impact on liver steatosis and adipose tissue inflammation in high-fat/high-glucose-fed mice by analyzing histological changes and gene expression profiling; to assess its cardiorenal protective effects in diabetic nephropathy and cardiomyopathy models through tissue morphology and biochemical markers.

Biochem/physiol Actions

E17241 is an orally active pan-PPAR agonist (EC50 in µM = 0.29/γ, 0.88/δ(β), 3.9/α in HepG2 reporter cells) that upregulates PPAR target genes expression (ABCA1 EC50 = 626.9 nM in HepG2 reporter cells). E17241 boosts ABCA1-dependent cholesterol efflux and insulin secretion in INS-1 rat insulinoma cultures (20 nM to 10 µM) and exhibits therapeutic efficacy in diabetic mice in vivo (50 mg/kg via daily p.o.).


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Warning

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - Skin Sens. 1B

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Yanni Xu (许艳妮) et al.
Arteriosclerosis, thrombosis, and vascular biology, 41(6), e284-e298 (2021-01-15)
[Figure: see text].
Ren Sheng et al.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 172, 116220-116220 (2024-02-04)
Type 2 diabetes mellitus (T2DM) is a common chronic metabolic disease. Peroxisome proliferator-activated receptors (PPARs) play crucial roles in regulating glucolipid metabolism. Previous studies showed that E17241 could ameliorate atherosclerosis and lower fasting blood glucose levels in ApoE-/- mice. In



Global Trade Item Number

SKUGTIN
SML4188-50MG04065272725545
SML4188-10MG04065272725538