2. Cell Cycle/DNA Damage Epigenetics
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  4. SIRT1 activator 4

SIRT1 activator 4 is an orally active, NAD+-independent SIRT1 activator. SIRT1 activator 4 is also an analog of (E)-2'-desmethyl Sulindac (HY-B0008), with weak or negligible inhibitory activity against COX-1 and no inhibitory activity against COX-2. SIRT1 activator 4 can be used for the research of metabolic diseases.

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SIRT1 activator 4

SIRT1 activator 4 Chemical Structure

CAS No. : 1049800-47-6

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Description

SIRT1 activator 4 is an orally active, NAD+-independent SIRT1 activator. SIRT1 activator 4 is also an analog of (E)-2'-desmethyl Sulindac (HY-B0008), with weak or negligible inhibitory activity against COX-1 and no inhibitory activity against COX-2. SIRT1 activator 4 can be used for the research of metabolic diseases[1].

IC50 & Target

SIRT1

 

In Vivo

SIRT1 activator 4 (compound B) (5-50 mg/kg, p.o.; once daily for 3 consecutive days) dose-dependently activates the SIRT1 signaling pathway in mouse liver, exerts anti-inflammatory effects, stimulates gluconeogenesis, inhibits adipogenesis, and regulates clock gene expression, with no acute toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 J Mice (male, 8 months of age)[1]
Dosage: 5 mg/kg/day; 50 mg/kg/day
Administration: p.o.; daily; 3 days
Result: Regulation of Gene Expression
1. Dose-dependently reduces levels of NF-κB target genes (e.g., Tnfα, Ccl2) and adipogenic genes (e.g., Acaca, Fasn); decreases expression of the glycolytic gene Gck.
2. Increases levels of gluconeogenic genes (e.g., Pgc1α, Pck1, G6pc), Fgf21, and Nampt; alters the expression of clock genes.

Metabolites: Decreases levels of gluconeogenic amino acids; increases levels of gluconeogenic intermediates, malate, and hepatic NAD+ (showing an upward trend).
Histology: Significantly reduces inflammatory cell infiltration in the liver.
Safety: With the exception of occasional mild hepatocyte hypertrophy observed in the high-dose group, no significant toxicity or changes in body weight were noted.
Molecular Weight

356.40

Formula

C24H17FO2
CAS No.
SMILES

C(=C\1/C=2C(C(CC(O)=O)=C1)=CC(F)=CC2)\C3=CC=C(C=C3)C4=CC=CC=C4
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Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SIRT1 activator 41049800-47-6SirtuinlipogenesisNAD+mouse livercircadian gene expressionCOX-1anti-inflammatory effectsCOX-2SIRT1metabolic diseasesgluconeogenesisInhibitorinhibitorinhibit

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