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

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

Cat. No.: HY-50879 Purity: 99.80%
COA Handling Instructions

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 drug 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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Estimated Time of Arrival: December 31
50 mg USD 252 In-stock
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100 mg USD 372 In-stock
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200 mg USD 600 In-stock
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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Elacridar:

Top Publications Citing Use of Products

    Elacridar purchased from MCE. 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 drug 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].

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

    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

    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.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (8.87 mM; Need ultrasonic)

    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
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 0.25 mg/mL (0.44 mM); Clear solution

    • 4.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: 0.25 mg/mL (0.44 mM); Suspended solution; Need ultrasonic

    • 5.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: 0.05 mg/mL (0.09 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.80%

    References
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    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.

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    Product Name:
    Elacridar
    Cat. No.:
    HY-50879
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