SRT3025 HCl

Catalog No.S8481

SRT3025 HCl Chemical Structure

Molecular Weight(MW): 606.2

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

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Biological Activity

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

Protocol

Cell Research:

[1]
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  • 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. 


    (Only for Reference)
Animal Research:

[1]
+ Expand
  • Animal Models: Female athymic nu/nu mice
  • Formulation: PBS containing 1% Hydroxypropyl)-β-cyclodextrine and 12% propylene glycol
  • Dosages: 50-200 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (164.96 mM)
Ethanol 5 mg/mL warmed (8.24 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 606.2
Formula

C31H31N5O2S2.HCl
CAS No. 2070015-26-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

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

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

Tel: +1-832-582-8158 Ext:3

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Sirtuin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID