2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. ESI-05

ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.

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

ESI-05 Chemical Structure

ESI-05 Chemical Structure

CAS No. : 5184-64-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 116 In-stock
50 mg USD 352 In-stock
100 mg USD 605 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

ESI-05 Related Antibodies

Top Publications Citing Use of Products

    ESI-05 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Nov 11;S1550-4131(22)00490-9.  [Abstract]

    CGRP-mediated enhanced interaction between Rap1 and Raptor is antagonized by blocking the activation of Rap1 into Rap1-GTP using ESI-05 (10 µM; 1 h), in Cal27 cells.

    View All Acyltransferase Isoform Specific Products:

    View All Isoforms
    ACAT1 ACAT2 MGAT2 ACAT

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders[1][2].

    IC50 & Target

    IC50: 0.43 μM (EPAC2)[1]
    In Vitro

    ESI-05 (0.01 μM -1 nM) inhibits cAMP-mediated EPAC2 GEF activity with IC50 of 0.43 μM, but completely ineffective in suppressing EPAC1 GEF activity[1].
    ESI-05 (1, 5, 10, and 25 μM; 5 min) selectively modulates EPAC2 activation in living cells[1].

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

    ESI-05 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: HEK293 cells
    Concentration: 1, 5, 10, and 25 μM
    Incubation Time: 5 min
    Result: Led to a dose-dependent reduction of the EPAC-selective cAMP analog (007-AM) induced Rap1 activation.
    In Vivo

    ESI-05 (2, 4, and 8 mg/kg) decreases neuronal apoptosis by inhibiting the p38/BIM pathway in vivo[2].

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

    Animal Model: Intracranial hemorrhage (ICH) model[2]
    Dosage: 2, 4, and 8 mg/kg
    Administration:
    Result: Decreased the apoptosis rate of nerve cells in the cortex accompanied by a corresponding decrease in the protein expression of phosphorylated p38, Bcl-2like protein 11 (BIM), and caspase-3.
    Molecular Weight

    274.38

    Formula

    C16H18O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(C1=C(C)C=C(C)C=C1C)(C2=CC=C(C)C=C2)=O
    Shipping

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

    DMSO : 50 mg/mL (182.23 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 3.6446 mL 18.2229 mL 36.4458 mL
    5 mM 0.7289 mL 3.6446 mL 7.2892 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (9.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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

    Purity: 99.94%

    COA (251 KB) HNMR (243 KB) LCMS (99 KB)

    Handling Instructions (2659 KB)
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.6446 mL 18.2229 mL 36.4458 mL 91.1145 mL
    5 mM 0.7289 mL 3.6446 mL 7.2892 mL 18.2229 mL
    10 mM 0.3645 mL 1.8223 mL 3.6446 mL 9.1115 mL
    15 mM 0.2430 mL 1.2149 mL 2.4297 mL 6.0743 mL
    20 mM 0.1822 mL 0.9111 mL 1.8223 mL 4.5557 mL
    25 mM 0.1458 mL 0.7289 mL 1.4578 mL 3.6446 mL
    30 mM 0.1215 mL 0.6074 mL 1.2149 mL 3.0372 mL
    40 mM 0.0911 mL 0.4556 mL 0.9111 mL 2.2779 mL
    50 mM 0.0729 mL 0.3645 mL 0.7289 mL 1.8223 mL
    60 mM 0.0607 mL 0.3037 mL 0.6074 mL 1.5186 mL
    80 mM 0.0456 mL 0.2278 mL 0.4556 mL 1.1389 mL
    100 mM 0.0364 mL 0.1822 mL 0.3645 mL 0.9111 mL
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    ESI-05 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:

    ESI-055184-64-5NSC 116966ESI05ESI 05NSC116966NSC-116966AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseexchange proteins directly activated by cAMP 2 (EPAC2)cAMPGEFdiabetesinsulin secretionneurological disordersIntracranial hemorrhage (ICH)Inhibitorinhibitorinhibit

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