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Chemical Structure| 49843-98-3 Chemical Structure| 49843-98-3

Structure of Selisistat
CAS No.: 49843-98-3

Chemical Structure| 49843-98-3

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EX-527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits > 200-fold selectivity against SIRT2 and SIRT3.

Synonyms: EX-527; SEN0014196; (±)-EX-527

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Product Details of Selisistat

CAS No. :49843-98-3
Formula : C13H13ClN2O
M.W : 248.71
SMILES Code : O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N
Synonyms :
EX-527; SEN0014196; (±)-EX-527
MDL No. :MFCD03009471
InChI Key :FUZYTVDVLBBXDL-UHFFFAOYSA-N
Pubchem ID :5113032

Safety of Selisistat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Selisistat

epigenetics

Isoform Comparison

Biological Activity

Description
Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1, which alleviates pathology in multiple animal and cell models of Huntington's disease[1].[2].
Target
  • SIRT1

    SIRT1, IC50:38 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse astrocytes 10 μM 30 min To investigate the inhibitory effect of Selisistat on IL-1β-induced astrocyte activation. Results showed that Selisistat significantly inhibited IL-1β-induced astrocyte activation. Neural Regen Res. 2021 Apr;16(4):721-726.
HepG2 cells 40 µM 8 h To validate the effect of Selisistat as a SIRT1 inhibitor Hepatol Commun. 2020 Jan 16;4(3):434-449.
HT22 cells 1 μM 2 h To evaluate the effect of Selisistat on the Sirt1/FoxO1/Rab7 axis, it was found that Selisistat significantly reduced the expression of Sirt1, Rab7, and FoxO1 and inhibited autophagosome formation. Cells. 2022 Nov 21;11(22):3701.
human skeletal stem cells (hSSCs) 1 µM 14 days To investigate the inhibitory effect of Selisistat on osteogenic differentiation of hSSCs, results showed that Selisistat significantly reduced the osteogenic differentiation capacity of hSSCs. Aging Cell. 2020 Jul;19(7):e13164.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Early social isolation (ESI) model Oral gavage 20 mg/kg Once daily for 12 days To investigate the effect of Selisistat on depression-like behavior in adult mice when administered during early development. Results showed that Selisistat administration during juvenility increased immobility and decreased activity in the FST in control mice, while no significant changes were observed in ESI mice. Transl Psychiatry. 2015 Sep 1;5(9):e629
Mice Nigrostriatal pathway injury model Intraperitoneal injection 5 mg/kg Single dose, 30 minutes before injury To investigate the neuroprotective effect of Selisistat after nigrostriatal pathway injury. Results showed that Selisistat significantly reversed the neuroprotective effects of Batroxobin. Neural Regen Res. 2021 Apr;16(4):721-726.
Mice Diabetic and obese model Oral 10 mg/kg Once daily for 4 weeks TMS alleviated endothelial dysfunction in diet-induced obese mice by enhancing the AMPK/SIRT1/eNOS pathway and attenuating oxidative stress and ER stress in aortas. Antioxidants (Basel). 2022 Jun 28;11(7):1286
Mice Sepsis model Intraperitoneal injection 5 mg/kg Selisistat (EX-527) inhibited the expression of Sirt1 and partially reversed the upregulation of Sirt1 by NMN. Cell Death Dis. 2024 Jun 28;15(6):462

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01485965 Huntington's Disease PHASE1 COMPLETED 2025-12-12 University of California San D... More >>iego, La Jolla, California, 92037-0706, United States|University of California Davis Medical Center, Sacramento, California, 95655, United States|Washington University, St. Louis, Missouri, 63110, United States|University of Rochester, Rocherster, New York, 14627, United States|Wake Forest School of Medicine, Winston-Salem, North Carolina, 27157-1078, United States|University of Texas Southwestern Medical Center, Dallas, Texas, 75390-8527, United States|Baylor College of Medicine, Houston, Texas, 77030, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.02mL

0.80mL

0.40mL

20.10mL

4.02mL

2.01mL

40.21mL

8.04mL

4.02mL

References

 

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