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(S)-Selisistat

Cat. No. M30682
(S)-Selisistat Structure
Synonym:

(S)-EX-527

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Biological Activity

(S)-Selisistat ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC50 of 98 nM.

Chemical Information
Molecular Weight 248.71
Formula C13H13ClN2O
CAS Number 848193-68-0
Form Solid
Solubility (25°C) DMSO ≥ 100 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] Iram Khan Iqbal, et al. Autophagy. Hydrogen sulfide-induced GAPDH sulfhydration disrupts the CCAR2-SIRT1 interaction to initiate autophagy

[2] Xinfa Bai, et al. Mini Rev Med Chem. Small Molecules as SIRT Modulators

[3] J D Rollnik. Nervenarzt. [Huntington's disease]

[4] Sigurd D Süssmuth, et al. Br J Clin Pharmacol. An exploratory double-blind, randomized clinical trial with selisistat, a SirT1 inhibitor, in patients with Huntington's disease

[5] Pushkar Kulkarni, et al. Expert Opin Investig Drugs. Investigational drugs for the management of Huntington's disease: are we there yet?

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