Selisistat (SEN0014196; EX 527)

Alias: Selisistat; EX 527; SEN 0014196; EX527; SEN-0014196; SEN0014196; EX-527

Cat No.:V0429 Purity: ≥98%

COA Product Data Instructions for use SDS

Selisistat (SEN0014196; EX 527) Chemical Structure CAS No.: 49843-98-3
Product category: Sirtuin

This product is for research use only, not for human use. We do not sell to patients.

Size	Price	Stock	Qty
5mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

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Other Forms of Selisistat (SEN0014196; EX 527):

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Selisistat (formerly SEN-0014196; EX-527) is a novel, highly potent and selective inhibitor of SIRT1 (Sirtuin1, a NAD-dependent and class III histone deacetylase enzyme) with important biological activity. It inhibits SIRT1 with an IC50 of 38 nM in a cell-free assay, and exhibits >200-fold higher selectivity for SIRT1 over SIRT2, SIRT3 and other deacetylases as well as NAD-processing enzymes.

Biological Activity I Assay Protocols (From Reference)

ln Vitro

Selisistat (1-10 μM) decreases the deacetylation activity of both human SirT1 and Drosophila Sir2 in transfected cells[1].

ln Vivo

In the R6/2 mouse model of Huntington's disease (HD), selenisistat (5 and 20 mg/kg, PO, daily; transgenic R6/2 mice commencing at 4.5 weeks of age until death) is protective[1].

Animal Protocol

Dissolved in DMSO; ~5 μg/rat; Intracerebroventricular injection

Male Sprague-Dawley rats

References

[1]. Smith MR, et al. A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington's disease. Hum Mol Genet. 2014;23(11):2995-3007.
[2]. Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1 [published correction appears in J Med Chem. 2007 Mar 8;50(5):1086]. J Med Chem. 2005;48(25):8045-8054

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C13H13CLN2O
Molecular Weight	248.71
CAS #	49843-98-3
Related CAS #	(S)-Selisistat;848193-68-0;(R)-Selisistat;848193-69-1
SMILES	O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N
Chemical Name	6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
Synonyms	Selisistat; EX 527; SEN 0014196; EX527; SEN-0014196; SEN0014196; EX-527
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)

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (201.0 mM)

Water:<1 mg/mL

Ethanol: 18 mg/mL (72.4 mM)

Solubility (In Vivo)

1% DMSO+30% polyethylene glycol+1% Tween 80:14mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate Reset

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04184323	Withdrawn	Drug: EX-527 (Selisistat) Drug: Placebo	Endometriosis Uterine Diseases	Wake Forest University Health Sciences	January 2022	Phase 2

Biological Data

Pharmacologic blockade of SIRT1 blunts the orexigenic action of ghrelin.Diabetes.2011 Apr;60(4):1177-85.
Mice lacking p53 do not respond to ghrelin injection.Diabetes.2011 Apr;60(4):1177-85.
Pharmacologic blockade of SIRT1 does not modify the ghrelin-induced GH secretion.Diabetes.2011 Apr;60(4):1177-85.