2. Membrane Transporter/Ion Channel
  3. P-glycoprotein BCRP
  4. Elacridar

Elacridar  (Synonyms: GF120918; GW0918; GG918; GW120918)

Cat. No.: HY-50879 Purity: 99.94%
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Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer.

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

Elacridar Chemical Structure

Elacridar Chemical Structure

CAS No. : 143664-11-3

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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Elacridar:

Elacridar Related Antibodies

Top Publications Citing Use of Products

    Elacridar purchased from MedChemExpress. Usage Cited in: J Drug Target. 2016;24(5):441-9.  [Abstract]

    Cells are co-treated with 5 μM of free LY139481 or an equivalent dose of SMA-LY139481 and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer[1][2].

    IC50 & Target

    P-glycoprotein (Pgp), BCRP[1]
    In Vitro

    Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells[2].
    Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines[2].
    Elacridar (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells[2].

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

    Elacridar Related Antibodies

    Cell Viability Assay[2]

    Cell Line: 786-O cells
    Concentration: 2.5 and 5 μM
    Incubation Time: 2 hours
    Result: Dose-dependently inhibited cell viability of 786-O cells and showed better inhibitory effect with sunitnib adding

    Western Blot Analysis[2]

    Cell Line: MCF-7, Caki-1, and 786-O cell lines
    Concentration: 5 μM
    Incubation Time: 24 hours
    Result: Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells.

    Cell Viability Assay[2]

    Cell Line: MCF-7 and 786-O cell lines
    Concentration: 5 μM
    Incubation Time: 24 hours
    Result: Dose-dependently increased 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells.
    In Vivo

    Elacridar (100 mg/kg; i.p. once) shows different distribution in brain and plasma[1].
    1.19 Plasma Pharmacokinetic Parameters of Elacridar in mice[1].

    Mice
    PO 100 mg/kg    		 Mice
    IP 100 mg/kg    		 Mice
    IV 2.5 mg/kg
    CL/F (ml/min) 2.05 33.2 0.46
    Vd/F (liter) 3.5 12.3 0.17
    t1/2 (h) 20 4.3 4.4
    AUC0-inf (μg•min/ml) 1460 90.3 161.4
    F 0.22 0.013 1

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

    Animal Model: FVB wild-type mice[1].
    Dosage: 100 mg/kg
    Administration: Intraperitoneal injection; 100 mg/kg once
    Result: Showd a higher concertration in brain than plasma except at 4 h after the dose.
    Molecular Weight

    563.64

    Formula

    C34H33N3O5
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to brown

    SMILES

    O=C1C2=CC=CC(C(NC(C=C3)=CC=C3CCN4CC(C=C(C(OC)=C5)OC)=C5CC4)=O)=C2NC6=C1C=CC=C6OC
    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 : 5 mg/mL (8.87 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 1.7742 mL 8.8709 mL 17.7418 mL
    5 mM 0.3548 mL 1.7742 mL 3.5484 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.

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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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% (20% SBE-β-CD in Saline)

      Solubility: 1.67 mg/mL (2.96 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
    • Protocol 2

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

      Solubility: ≥ 0.5 mg/mL (0.89 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    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) LCMS (93 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 1.7742 mL 8.8709 mL 17.7418 mL 44.3546 mL
    5 mM 0.3548 mL 1.7742 mL 3.5484 mL 8.8709 mL
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    Elacridar 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:

    Elacridar143664-11-3GF120918 GW0918 GG918 GW120918GF 120918GF-120918GW0918GW 0918GW-0918GG918GG 918GG-918GW120918GW 120918GW-120918P-glycoproteinBCRPP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Breast cancer resistance proteinABCG2cancer786-OMCF-7sunitinibInhibitorinhibitorinhibit

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