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Selisistat (EX-527) S-enantiomer is a novel and potent SIRT1 inhibitor. As the S-enantiomer of Selisistat, it has an IC50 of 123 nM for SIRT1, much more potent than the R-enantiomer of Selisistat.
| ln Vitro |
(S)-Selisistat is a SIRT1 enzymatic activity inhibitor (IC50, 98 nM) that was found via a high-throughput screen employing human SIRT1 expressed in bacteria. With an IC50 of 38 nM, (S)-Selisistat inhibits SIRT1 in a concentration-dependent manner that is comparable with the activity of SIRT1 expressed in bacteria. (S)-Selisistat does not inhibit class I/II HDAC activity at concentrations up to 100 μM, but it is substantially less effective against SIRT2 (IC50, 19.6 μM) or SIRT3 (IC50, 48.7 μM) [1]. SIRT1 activity is inhibited by (S)-Selisistat, while SIRT1 mRNA and protein levels are unaffected [2].
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| ln Vivo |
In ob/ob septic mice, (S)-Selisistat eliminates the mitigating effect of resveratrol (RSV)-induced microvascular inflammation. Lastly, compared to the sepsis+vehicle group, the 7-day survival rate of ob/ob mice in the sepsis+RSV group was considerably higher [3].
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| References |
[1]. Solomon JM, et al. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol Cell Biol. 2006 Jan;26(1):28-38.
[2]. Jia Y, et al. SIRT1 is a regulator in high glucose-induced inflammatory response in RAW264.7 cells. PLoS One. 2015 Mar 20;10(3):e0120849. [3]. Wang X, et al. Resveratrol attenuates microvascular inflammation in sepsis via SIRT-1-Induced modulation of adhesion molecules in ob/ob mice. Obesity (Silver Spring). 2015 Jun;23(6):1209-17. [4]. Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J Med Chem. 2005 Dec 15;48(25):8045-54. |
| Molecular Formula |
C13H13CLN2O
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|---|---|
| Molecular Weight |
248.71
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| Exact Mass |
248.0716
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| CAS # |
848193-68-0
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| Related CAS # |
Selisistat;49843-98-3;(R)-Selisistat;848193-69-1
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| SMILES |
O=C([C@@H]1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N
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| Synonyms |
EX 527(S) (S)-Selisistat EX-527(S)
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~402.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.05 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 25.0 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: ≥ 2.5 mg/mL (10.05 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0207 mL | 20.1037 mL | 40.2075 mL | |
| 5 mM | 0.8041 mL | 4.0207 mL | 8.0415 mL | |
| 10 mM | 0.4021 mL | 2.0104 mL | 4.0207 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.
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.
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