Selisistat
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MedKoo CAT#: 319734

CAS#: 49843-98-3

Description: Selisistat, also known as EX-527, is a SirT1 inhibitor for treatment of Huntington's disease. Selisistat is widely used as a major inhibitor of Sirtuin enzymes, which are a family of highly conserved protein deacetylases and have been linked with caloric restriction and aging by modulating energy metabolism, genomic stability, and stress resistance.


Chemical Structure

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Selisistat
CAS# 49843-98-3

Theoretical Analysis

MedKoo Cat#: 319734
Name: Selisistat
CAS#: 49843-98-3
Chemical Formula: C13H13ClN2O
Exact Mass: 248.07
Molecular Weight: 248.710
Elemental Analysis: C, 62.78; H, 5.27; Cl, 14.25; N, 11.26; O, 6.43

Price and Availability

Size Price Availability Quantity
5g USD -1
10mg USD 150
25mg USD 250
50mg USD 450
100mg USD 850
200mg USD 1250
500mg USD 1950
1g USD 3250
2g USD 4650
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Synonym: EX-527; EX-527; EX-527; Selisistat.

IUPAC/Chemical Name: 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

InChi Key: FUZYTVDVLBBXDL-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)

SMILES Code: O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: Selisistat is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1. Selisistat inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism. Galectin-9 in combination with Selisistat prolongs the survival of cardiac allografts in mice after cardiac transplantation. Selisistat alleviates pathology in multiple animal and cell models of Huntington's disease.
In vitro activity: Selisitat suppressed hepatitis B replication by silencing the expression of SIRT1, therefore inhibiting its activity. Reference: Acta Virol. 2023;67(1):51-58. https://pubmed.ncbi.nlm.nih.gov/36950885/
In vivo activity: Selisistat prevented the progression of high-fat diet-induced hepatic steatosis and fibrosis in Zucker rats, making it a promising candidate HFD-induced liver fibrosis inhibition. Selisistat reduced the serum levels of triglyceride, total cholesterol, alanine aminotransferase, and aspartate aminotransferase, and attenuated hepatic fibrosis. Selisistat upregulated SIRT2, SIRT3, and SIRT4 expression in the liver of HFD fed rats but downregulated TGF-β1 and α-SMA expression. It decreased proinflammatory cytokine production and hydroxyproline levels in the serum and SMAD4 expression and restored apoptotic protein expression. Reference: Cells. 2020 Apr 29;9(5):1101. https://pubmed.ncbi.nlm.nih.gov/32365537/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.7 75.00
Ethanol 12.4 50.00

Preparing Stock Solutions

The following data is based on the product molecular weight 248.71 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Zhang W, Cui J, Li L, Chai L, Hou Q, Yu H. Notoginsenoside R1 inhibits hepatitis B virus replication by modulating SIRT1 activity. Acta Virol. 2023;67(1):51-58. doi: 10.4149/av_2023_105. PMID: 36950885. 2. Kundu A, Dey P, Park JH, Kim IS, Kwack SJ, Kim HS. EX-527 Prevents the Progression of High-Fat Diet-Induced Hepatic Steatosis and Fibrosis by Upregulating SIRT4 in Zucker Rats. Cells. 2020 Apr 29;9(5):1101. doi: 10.3390/cells9051101. PMID: 32365537; PMCID: PMC7290750. 3. Nikseresht S, Khodagholi F, Ahmadiani A. Protective effects of ex-527 on cerebral ischemia-reperfusion injury through necroptosis signaling pathway attenuation. J Cell Physiol. 2019 Feb;234(2):1816-1826. doi: 10.1002/jcp.27055. Epub 2018 Aug 1. PMID: 30067864.
In vitro protocol: 1. Zhang W, Cui J, Li L, Chai L, Hou Q, Yu H. Notoginsenoside R1 inhibits hepatitis B virus replication by modulating SIRT1 activity. Acta Virol. 2023;67(1):51-58. doi: 10.4149/av_2023_105. PMID: 36950885.
In vivo protocol: 1. Kundu A, Dey P, Park JH, Kim IS, Kwack SJ, Kim HS. EX-527 Prevents the Progression of High-Fat Diet-Induced Hepatic Steatosis and Fibrosis by Upregulating SIRT4 in Zucker Rats. Cells. 2020 Apr 29;9(5):1101. doi: 10.3390/cells9051101. PMID: 32365537; PMCID: PMC7290750. 2. Nikseresht S, Khodagholi F, Ahmadiani A. Protective effects of ex-527 on cerebral ischemia-reperfusion injury through necroptosis signaling pathway attenuation. J Cell Physiol. 2019 Feb;234(2):1816-1826. doi: 10.1002/jcp.27055. Epub 2018 Aug 1. PMID: 30067864.

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1: Tao YF, Lin F, Yan XY, Gao XG, Teng F, Fu ZR, Wang ZX. Galectin-9 in
Combination With EX-527 Prolongs the Survival of Cardiac Allografts in Mice After
Cardiac Transplantation. Transplant Proc. 2015 Jul-Aug;47(6):2003-9. doi:
10.1016/j.transproceed.2015.04.091. PubMed PMID: 26293089.


2: Ohata Y, Matsukawa S, Moriyama Y, Michiue T, Morimoto K, Sato Y, Kuroda H.
Sirtuin inhibitor Ex-527 causes neural tube defects, ventral edema formations,
and gastrointestinal malformations in Xenopus laevis embryos. Dev Growth Differ.
2014 Aug;56(6):460-8. doi: 10.1111/dgd.12145. Epub 2014 Aug 5. PubMed PMID:
25131500.


3: Gertz M, Fischer F, Nguyen GT, Lakshminarasimhan M, Schutkowski M, Weyand M,
Steegborn C. Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent
deacetylation mechanism. Proc Natl Acad Sci U S A. 2013 Jul 23;110(30):E2772-81.
doi: 10.1073/pnas.1303628110. Epub 2013 Jul 9. PubMed PMID: 23840057; PubMed
Central PMCID: PMC3725051.