Home DNA Damage/DNA Repair Sirtuin activator SRT3025 HCl

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SRT3025 HCl Sirtuin activator

Cat.No.S8481

SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.
SRT3025 HCl Sirtuin activator Chemical Structure

Chemical Structure

Molecular Weight: 606.2

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Quality Control

Batch: S848101 DMSO]100 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.72%
99.72

Chemical Information, Storage & Stability

Molecular Weight 606.2 Formula

C31H31N5O2S2.HCl

 Storage (From the date of receipt)
CAS No. 2070015-26-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COCCCC1=C(N=C(S1)C2=CC=CC=C2)C(=O)NC3=CC=CC=C3C4=NC5=C(S4)N=CC(=C5)CN6CCCC6.Cl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (164.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
SIRT1 [1]
(Cell-free assay)
In vitro
SRT3025 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival. SRT3025 inhibits RANKL-induced osteoclastogenesis in bone marrow-derived macrophages (BMMs) by activating AMPK and deacetylating RelA/p65 lysine 310, critical for activation of the NF-κB signaling pathway[2]. SRT3025 acts faster than oxymetholone to improve hematopoiesis. It does not work by direct activation of Sirt1 in hematopoietic cells. SRT3025 might suppress p21 transcription through the down-regulation of Egr1[3]. SRT3025 is found to activate wild-type Sirt1 protein but failed to activate the E230K mutant, an activation-resistant Sirt1 protein (due to a mutation at position 230)[4].
In vivo
SRT3025 treatment also inhibits tumor growth in Panc-1 xenografts, even though it is not as effective in inhibiting the viability of Panc-1 cells in culture. SRT3025 is well tolerated in mice and has the potential to be used in several diseases[1]. SRT3025 administration expands HSPCs and boosts blood counts while long term SRT3025 administration does not permanently increase or decrease HSC repopulating potential[3]. SRT3025 reduces plasma cholesterol, inflammation, and atherosclerosis in Apoe−/− mice, and it increases hepatic Ldlr expression and Pcsk9 accumulation[4].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01340911 Completed
Diabetes Mellitus Type 2
Sirtris a GSK Company|GlaxoSmithKline
 June 3 2011 Phase 1

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