ChemicalBook CAS DataBase List 1031195-19-3

1031195-19-3

Name	E1231
CAS	1031195-19-3
Molecular Formula	C21H21N3O3
Molecular Weight	363.41
MOL File	1031195-19-3.mol

Chemical Properties

Boiling point	605.8±55.0 °C(Predicted)
density	1.259±0.06 g/cm3(Predicted)
form	Solid
pka	2.90±0.61(Predicted)
color	Off-white to light brown

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H319-H335-H315
Precautionary statements	P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P

Hazard Information

Description

E1231 is a SIRT1 activator which protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression.

Uses

E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE-/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases[1].

in vivo

E1231 (40 mg/kg; po; once daily for 7 days) regulates cholesterol and lipid metabolism in Golden hamsters fed with HFD diet^[1].
E1231 (25, 50, and 100 mg/kg, in 0.5% CMC-Na; po; once daily for 12 weeks) reduces atherosclerosis development, without hepatotoxicity ornephrotoxicity in ApoE^-/- mice fed with atherogenic diet^[1].

Animal Model:	HFD-diet Golden hamsters (80-90 g)^[1]
Dosage:	40 mg/kg
Administration:	PO; once daily for 7 days
Result:	Increased SIRT1 protein expression but not SIRT3, SIRT6, or SIRT7. And reduced liver and serum cholesterol in hamsters.

Animal Model:	Atherogenic diet ApoE^-/- mice^[1]
Dosage:	25, 50, and 100 mg/kg
Administration:	PO; once daily for 12 weeks
Result:	Modulated plaque composition, immunofluorescence staining. And reduced CD68 positive areas while increasing ABCA1 expression in the aortic sinus.

IC 50

SIRT1: 0.83 μM (EC₅₀)

References

[1] Feng T, et al. SIRT1 activator E1231 protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression. Atherosclerosis. 2018 Jul;274:172-181. DOI:10.1016/j.atherosclerosis.2018.04.039

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