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SRT2183

Cat. No. M10109
SRT2183 Structure
Synonym:

SRT-2183

Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 220  USD220 In stock
25mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

SRT2183 is a selective activator of Sirtuin-1 (SIRT1) with EC1.5 value of 0.36 μM. SRT2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels. SRT2183 leads to increased mRNA levels of pro-apoptosis and DNA-damage-response genes, accompanied by accumulation of phospho-H2A.X levels. SRT2183 reduces the DNA-binding activity of both NF-κB and STAT3 to the promoter of GADD45G, which is one of the most upregulated genes following SRT2183 treatment.

Chemical Information
Molecular Weight 468.57
Formula C27H24N4O2S
CAS Number 1001908-89-9
Solubility (25°C) DMSO ≥ 150 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] A Scuto, et al. Cell Death Dis. SIRT1 activation enhances HDAC inhibition-mediated upregulation of GADD45G by repressing the binding of NF-κB/STAT3 complex to its promoter in malignant lymphoid cells

[2] Jill C Milne, et al. Nature. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes

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