SRT3025 HCL

Alias: SRT3025;SRT-3025;SRT 3025;SRT3025 HCl
Cat No.:V2699 Purity: ≥98%
SRT3025 is an orally bioactive small molecule activator of the SIRT1 enzyme.
SRT3025 HCL Chemical Structure CAS No.: 2070015-26-6
Product category: Sirtuin
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: 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. 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. 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).


Kinase Assay:


Cell Assay: Cells (HPDE, Panc-1, SU86.86, Patu8988t cells) are treated with vehicle or different concentrations of SRT3025 for 72 hours and submitted to MTT analysis.

ln 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. SRT3025 administration expands HSPCs and boosts blood counts while long term SRT3025 administration does not permanently increase or decrease HSC repopulating potential. SRT3025 reduces plasma cholesterol, inflammation, and atherosclerosis in Apoe−/− mice, and it increases hepatic Ldlr expression and Pcsk9 accumulation.
Animal Protocol
Dissolved in PBS containing 1% Hydroxypropyl)-β-cyclodextrine and 12% propylene glycol; 50-200 mg/kg; p.o. administration.
Female athymic nu/nu mice
References
Clin Cancer Res.2016;22(10):2496-507;PLoS One.2015;10(7):e0134391;Stem Cell Res.2015;15(1):130-40.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C31H31N5O2S2.HCL
Molecular Weight
606.2
CAS #
2070015-26-6
Related CAS #
1231952-55-8;2070015-26-6 (HCl);
SMILES
Cl.S1C(C2=CC=CC=C2NC(C2=C(CCCOC)SC(C3C=CC=CC=3)=N2)=O)=NC2C1=NC=C(C=2)CN1CCCC1
Synonyms
SRT3025;SRT-3025;SRT 3025;SRT3025 HCl
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (165 mM)
Water:<1 mg/mL
Ethanol: 5 mg/mL (8.2 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.25 mg/mL (2.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6496 mL 8.2481 mL 16.4962 mL
5 mM 0.3299 mL 1.6496 mL 3.2992 mL
10 mM 0.1650 mL 0.8248 mL 1.6496 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • SRT3025 HCL

    Effects of SRT3025 on hematopoiesis.Stem Cell Res.2015 Jul;15(1):130-40.
  • SRT3025 HCL

    Effects of SRT3025 on HSPC proliferation.Stem Cell Res.2015 Jul;15(1):130-40.

  • SRT3025 HCL

    Frequency and repopulating capacity of long-term HSCs after SRT3025 administration.Stem Cell Res.2015 Jul;15(1):130-40.

  • SRT3025 HCL

    Serial transplantation experiment.Stem Cell Res.2015 Jul;15(1):130-40.

  • SRT3025 HCL

    Effects of SRT3025 on hematopoiesis after conditional deletion of Sirt1 in blood cells or transgenic overexpression.Stem Cell Res.2015 Jul;15(1):130-40.

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