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

Elacridar hydrochloride  (Synonyms: GF120918A)

Cat. No.: HY-50880 Purity: 99.73%
COA Handling Instructions

Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer.

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

Elacridar hydrochloride Chemical Structure

Elacridar hydrochloride Chemical Structure

CAS No. : 143851-98-3

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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Elacridar hydrochloride:

Top Publications Citing Use of Products

    Elacridar hydrochloride 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 hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer[1][2].

    In Vitro

    Elacridar hydrochloride (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells[2].
    Elacridar hydrochloride (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines[2].
    Elacridar hydrochloride (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 hydrochloride (100 mg/kg; i.p. once) shows different distribution in brain and plasma[1].
    1.19 Plasma Pharmacokinetic Parameters of Elacridar hydrochloride 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 administration.
    Molecular Weight

    600.10

    Appearance

    Solid

    Formula

    C34H34ClN3O5
    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.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (104.15 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6664 mL 8.3319 mL 16.6639 mL
    5 mM 0.3333 mL 1.6664 mL 3.3328 mL
    10 mM 0.1666 mL 0.8332 mL 1.6664 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: 2.08 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

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

    Purity: 99.73%

    COA (253 KB) HNMR (308 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    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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    Keywords:

    Elacridar143851-98-3GF120918AP-glycoproteinBCRPP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Breast cancer resistance proteinABCG2cancer786-OMCF-7sunitinibInhibitorinhibitorinhibit

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