2. Cell Cycle/DNA Damage Epigenetics
  3. Sirtuin
  4. E1231

E1231  (Synonyms: 1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one)

Cat. No.: HY-117006 Purity: 98.55%
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E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE-/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases.

For research use only. We do not sell to patients.

E1231 Chemical Structure

E1231 Chemical Structure

CAS No. : 1031195-19-3

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Based on 1 publication(s) in Google Scholar

E1231 Related Antibodies

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Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7

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Description

E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE-/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases[1].

IC50 & Target[1]

SIRT1

0.83 μM (EC50)

In Vitro

E1231 (0.1-10 μM; 18 h) promotes cholesterol efflux and inhibits lipid accumulation in RAW 264.7 cells[1].
E1231 (10 μM; 6 h) significantly increases deacetylation of Doxo-induced p53 in HepG2 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

E1231 Related Antibodies
In Vivo

E1231 (40 mg/kg; po; once daily for 7 days) regulates cholesterol and lipid metabolism in Golden hamsters fed with HFD diet[1].
E1231 (25, 50, and 100 mg/kg, in 0.5% CMC-Na; po; once daily for 12 weeks) reduces atherosclerosis development, without hepatotoxicity ornephrotoxicity in ApoE-/- mice fed with atherogenic diet[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HFD-diet Golden hamsters (80-90 g)[1]
Dosage: 40 mg/kg
Administration: PO; once daily for 7 days
Result: Increased SIRT1 protein expression but not SIRT3, SIRT6, or SIRT7. And reduced liver and serum cholesterol in hamsters.
Animal Model: Atherogenic diet ApoE-/- mice[1]
Dosage: 25, 50, and 100 mg/kg
Administration: PO; once daily for 12 weeks
Result: Modulated plaque composition, immunofluorescence staining. And reduced CD68 positive areas while increasing ABCA1 expression in the aortic sinus.
Molecular Weight

363.41

Formula

C21H21N3O3
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

CC(N1CCN(C(C2=CC(C3=CC=C(C)O3)=NC4=CC=CC=C24)=O)CC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (275.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7517 mL 13.7586 mL 27.5171 mL
5 mM 0.5503 mL 2.7517 mL 5.5034 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7517 mL 13.7586 mL 27.5171 mL 68.7928 mL
5 mM 0.5503 mL 2.7517 mL 5.5034 mL 13.7586 mL
10 mM 0.2752 mL 1.3759 mL 2.7517 mL 6.8793 mL
15 mM 0.1834 mL 0.9172 mL 1.8345 mL 4.5862 mL
20 mM 0.1376 mL 0.6879 mL 1.3759 mL 3.4396 mL
25 mM 0.1101 mL 0.5503 mL 1.1007 mL 2.7517 mL
30 mM 0.0917 mL 0.4586 mL 0.9172 mL 2.2931 mL
40 mM 0.0688 mL 0.3440 mL 0.6879 mL 1.7198 mL
50 mM 0.0550 mL 0.2752 mL 0.5503 mL 1.3759 mL
60 mM 0.0459 mL 0.2293 mL 0.4586 mL 1.1465 mL
80 mM 0.0344 mL 0.1720 mL 0.3440 mL 0.8599 mL
100 mM 0.0275 mL 0.1376 mL 0.2752 mL 0.6879 mL
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E1231 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

E12311031195-19-31-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-oneE 1231E-1231Sirtuincholesterollipid metabolismX receptor-alphaATP-binding cassette transporter A1atherosclerotic plaquelipid disorder-related diseasesInhibitorinhibitorinhibit

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