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(R)-Selisistat

Cat. No. M30683
(R)-Selisistat Structure
Synonym:

(R)-EX-527

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Quality Control & Documentation
Biological Activity

(R)-Selisistat ((R)-EX-527) is a R-enantiomer of Selisistat. Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.

Chemical Information
Molecular Weight 248.71
Formula C13H13ClN2O
CAS Number 848193-69-1
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
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] Minsi Zheng, et al. Molecules. Resveratrol Reestablishes Mitochondrial Quality Control in Myocardial Ischemia/Reperfusion Injury through Sirt1/Sirt3-Mfn2-Parkin-PGC-1α Pathway

[2] Shidong Cao, et al. Front Pharmacol. Protocatechualdehyde Rescues Oxygen-Glucose Deprivation/Reoxygenation-Induced Endothelial Cells Injury by Inducing Autophagy and Inhibiting Apoptosis via Regulation of SIRT1

[3] Zheng-Nan Ren, et al. Acta Pharmacol Sin. A novel resveratrol analog upregulates sirtuin 1 and inhibits inflammatory cell infiltration in acute pancreatitis

[4] Nandini Ghosh, et al. Sci Rep. Urolithin A augments angiogenic pathways in skeletal muscle by bolstering NAD+ and SIRT1

[5] Guiping Luo, et al. Int J Mol Med. Sirt1 promotes autophagy and inhibits apoptosis to protect cardiomyocytes from hypoxic stress

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