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E1231

Alias: E1231; E 1231; E-1231
Cat No.:V20331 Purity: ≥98%
E1231 is an orally bioactive activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM) that regulates cholesterol and lipid metabolism.
E1231
E1231 Chemical Structure CAS No.: 1031195-19-3
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
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Product Description
E1231 is an orally bioactive activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM) that regulates cholesterol and lipid metabolism. E1231 interacts with SIRT1 and deacetylated liver X receptor-alpha (LXRα) and increases the expression of ATP-binding cassette transporter A1 (ABCA1). E1231 also reduces atherosclerotic plaque formation in the ApoE-/- mouse model. E1231 may be utilized to study diseases related to cholesterol and lipid disorders.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In RAW 264.7 cells, E1231 (0.1–10 μM; 18 hours) inhibits accumulation and encourages reflux [1]. In HepG2 cells, E1231 (10 μM; 6 hours) dramatically boosts Doxo-induced p53 dephospholipidation [1]. 1.].
ln Vivo
E1231 (40 mg/kg; once daily for 7 days) reduces the amount of food that golden hamsters on a high-fat diet consume on trays [1]. E1231 (once daily for 12 weeks at 25, 50, and 100 mg/kg in 0.5% CMC-Na; Manhattan) decreases the formation of atherosclerotic tumors in ApoE-/- mice without causing hepatotoxicity or nephrotoxicity.
Animal Protocol
Animal/Disease Models: HFD diet golden hamster (80-90 g) [1]
Doses: 40 mg/kg
Route of Administration: Oral; one time/day for 7 days
Experimental Results: SIRT1 protein expression increased, but not SIRT3, SIRT6 or SIRT7. and lowered liver and serum cholesterol in hamsters.

Animal/Disease Models: Atherosclerotic dietary ApoE-/- mice [1]
Doses: 25, 50 and 100 mg/kg
Route of Administration: Oral; one time/day for 12 weeks
Experimental Results: Modulation of plaque composition, immunofluorescence staining . And diminished the CD68-positive area in the aortic sinus while increasing ABCA1 expression.
References

[1]. SIRT1 activator E1231 protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression. Atherosclerosis. 2018 Jul;274:172-181.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H21N3O3
Molecular Weight
363.42
Exact Mass
363.158
CAS #
1031195-19-3
PubChem CID
24980435
Appearance
Off-white to light brown solid powder
Density
1.3±0.1 g/cm3
Boiling Point
605.8±55.0 °C at 760 mmHg
Flash Point
320.2±31.5 °C
Vapour Pressure
0.0±1.7 mmHg at 25°C
Index of Refraction
1.626
LogP
1.3
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
2
Heavy Atom Count
27
Complexity
561
Defined Atom Stereocenter Count
0
InChi Key
ZQJTYRXKAZFWPK-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H21N3O3/c1-14-7-8-20(27-14)19-13-17(16-5-3-4-6-18(16)22-19)21(26)24-11-9-23(10-12-24)15(2)25/h3-8,13H,9-12H2,1-2H3
Chemical Name
1-[4-[2-(5-methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl]ethanone
Synonyms
E1231; E 1231; E-1231
HS Tariff Code
2934.99.9001
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 : ~100 mg/mL (~275.17 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.88 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 (6.88 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.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7516 mL 13.7582 mL 27.5164 mL
5 mM 0.5503 mL 2.7516 mL 5.5033 mL
10 mM 0.2752 mL 1.3758 mL 2.7516 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

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

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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.

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)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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

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  • 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)
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.)
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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.

(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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