An inhibitor of MRP-1 and BCRP
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Elacridar

Item No. 18128

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide
CAS Number
143664-11-3
Synonyms
  • GF120918
  • GG918
  • GW0918
Molecular Formula
C34H33N3O5
Formula Weight
563.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 1 mg/ml
λmax
258, 406 nm
SMILES
COC1=C(OC)C=C(CCN(CCC2=CC=C(NC(C3=CC=CC4=C3NC5=C(C=CC=C5OC)C4=O)=O)C=C2)C6)C6=C1
InChi Code
InChI=1S/C34H33N3O5/c1-40-28-9-5-7-26-32(28)36-31-25(33(26)38)6-4-8-27(31)34(39)35-24-12-10-21(11-13-24)14-16-37-17-15-22-18-29(41-2)30(42-3)19-23(22)20-37/h4-13,18-19H,14-17,20H2,1-3H3,(H,35,39)(H,36,38)
InChi Key
OSFCMRGOZNQUSW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $77

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    10 mg

    $120

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    50 mg

    $387

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    Cayman Chemical
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    Product Description

    Elacridar is a dual inhibitor of P-glycoprotein (MRP-1, ABCB1) and breast cancer resistance protein (BCRP, ABCG2). It maximally inhibits P-glycoprotein in isolated human peripheral blood leukocytes at 200 nM.1 Elacridar blocks the activity of P-glycoprotein at the blood-brain barrier, altering the pharmacokinetics of certain drugs in the brain.2 This compound is effective against both human BCRP and the mouse homolog, Bcrp1.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Witherspoon, S.M., Emerson, D.L., Kerr, B.M., et al. Flow cytometric assay of modulation of P-glycoprotein function in whole blood by the multidrug resistance inhibitor GG918. Clin. Cancer Res. 2(1), 7-12 (1996).

    2. Letrent, S.P., Pollack, G.M., Brouwer, K.R., et al. Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphine in the rat. Drug Metab. Dispos. 27(7), 827-834 (1999).

    3. de Bruin, M., Miyake, K., Litman, T., et al. Reversal of resistance by GF120918 in cell lines expressing the ABC halftransporter, MXR. Cancer Lett. 146(2), 117-126 (1999).

    4. Jonker, J.W., Smit, J.W., Brinkhuis, R.F., et al. Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. J. Natl. Cancer Inst. 92(20), 1651-1656 (2000).

    Product Citations

    Rana, P.S., Gibbons, B.A., Vereninov, A.A., et al. Calibration and characterization of intracellular Asante Potassium Green probes, APG-2 and APG-4. Anal. Biochem. 567, 8-13 (2019).