Home DNA Damage/DNA Repair Sirtuin activator SRT3025 HCl For research use only.

SRT3025 HCl

SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.

SRT3025 HCl Chemical Structure

SRT3025 HCl Chemical Structure

CAS: 2070015-26-6

Selleck's SRT3025 HCl has been cited by 3 publications

Purity & Quality Control

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

SRT3025 HCl Related Products

Signaling Pathway

Sirtuin Signaling Pathways

Sirtuin Signaling Pathway

Choose Selective Sirtuin Inhibitors

Biological Activity

Description SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.
Targets
SIRT1 [1]
(Cell-free assay)
In vitro
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].
Cell Research Cell lines HPDE, Panc-1, SU86.86, Patu8988t cells
Concentrations 0-5 μM
Incubation Time 72 h
Method

Cells are treated with vehicle or different concentrations of SRT3025 for 72 hours and submitted to MTT analysis. 
In Vivo
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].
Animal Research Animal Models Female athymic nu/nu mice
Dosages 50-200 mg/kg
Administration oral administration
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

Chemical Information & Solubility

Molecular Weight 606.2 Formula

C31H31N5O2S2.HCl
CAS No. 2070015-26-6 SDF Download SRT3025 HCl SDF
Smiles COCCCC1=C(N=C(S1)C2=CC=CC=C2)C(=O)NC3=CC=CC=C3C4=NC5=C(S4)N=CC(=C5)CN6CCCC6.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (164.96 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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