PeptideDB

SIRT3 activator 2

SIRT3 activator 2

CAS No.:

SIRT3 activator 2 (compound 2a) is a SIRT3 activator. SIRT3 activator 2 can directly bind to SIRT3 in SH-SY5Y cells base
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SIRT3 activator 2 (compound 2a) is a SIRT3 activator. SIRT3 activator 2 can directly bind to SIRT3 in SH-SY5Y cells based on its thermal stability and clear α-Syn in a SIRT3-dependent manner. SIRT3 activator 2 improves the motor function of Parkinson's mice and dose-dependently prevents the loss of DA neurons in the substantia nigra.

Physicochemical Properties


Molecular Formula C22H24N2O9S
Molecular Weight 492.50
Appearance Typically exists as solids at room temperature
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets SIRT3
ln Vitro SIRT3 activator 2 (compound 2) (10 μM, 100 μM) is a SIRT3 activator [1]. SIRT3 activator 2 (10 μM; 24h) increases the thermal stability of SIRT3 in SH-SY5Y cells (CETSA) and is shown to bind directly to SIRT3 (wb) [1]. SIRT3 activator2 (10 μM; 24h) protects neurons through SIRT3-dependent elimination of α-Syn (wb) in SH-SY5Y cells [1].
ln Vivo SIRT3 activator 2 (10, 20, 40 mg/kg; intravenous injection (iv); once each time; 24 days) improves motor function in Parkinson's mice induced by overexpression of α-synuclein[1]. SIRT3 activator 2 (10, 20, 40 mg/kg; microinjection into the brain) dose-dependently prevents the loss of DA neurons in the substantia nigra induced by overexpression of α-synuclein (immunohistochemistry)[1].
Cell Assay Western Blot Analysis[1]
Cell Types: SH-SY5Y Concentration: 10 μM
Incubation Duration: 24 h
Experimental Results: Improved the thermal stability (CETSA) of SIRT3 in SH-SY5Y cells and could bind directly to SIRT3.

Apoptosis Analysis[1]
Cell Types: Ttransfected with SIRT3 siRNAs in SH-SY5Y cells. Concentration: 10 μM
Incubation Duration: 24 h
Experimental Results: Showed that the protective effect of SIRT3 activator 2 on MPP+ (600 μM) or 6-OHDA(100μM)-induced neuronal injury disappeared and the expression level of α-Syn did not change significantly after SIRT3 silences.
Animal Protocol Animal/Disease Models: Parkinson mouse model injected with overexpression of A53T α-synuclein[1]
Doses: 10, 20, 40 mg/kg
Route of Administration: Intravenous injection (i.v.);Once daily; 24 days;The viruses (2.5 x 1012 genomic particles/ml) were infused to the right substantia nigra of mouse
Experimental Results: Showed that the movement function of mice was improved by increasing the walking distance, decreasing the descending time on the rod and increasing the descending time on the rotating rod.
References

[1]. Tongyu Bi, et al. Ligand-Enabled Pd-Catalyzed sp3 C‒H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease. Angewandte Chemie. 2024 Jul 30:e202412296.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0305 mL 10.1523 mL 20.3046 mL
5 mM 0.4061 mL 2.0305 mL 4.0609 mL
10 mM 0.2030 mL 1.0152 mL 2.0305 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.