Chemical Name: N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide hydrochloride
Biological ActivityElacridar hydrochloride is a P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) inhibitor. Elacridar hydrochloride blocks P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs doxorubicin (Cat. No. 2252) and vincristine (Cat. No. 1257) in CHRC5 cells. Orally active.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative.
Hyafil et al.
Cancer Res., 1993;53:4595
The chemosensitizing potential of GF120918 is independent of the magnitude of P-glycoprotein-mediated resistance to conventional chemotherapeutic agents in a small cell lung cancer line.
Myer et al.
Oncol Rep., 1999;6:217
Citations for Elacridar hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:
3 Citations: Showing 1 - 3
Systemic Administration of Glibenclamide Fails to Achieve Therapeutic Levels in the Brain and Cerebrospinal Fluid of Rodents.
Authors: Lahmann Et al.
PLoS One 2015;10:e0134476
Pro-inflammatory human Th17 cells selectively express P-glycoprotein and are refractory to glucocorticoids.
Authors: Ramesh Et al.
J Exp Med 2014;211:89
Inhibiting drug efflux transporters improves efficacy of ALS therapeutics.
Authors: Jablonski Et al.
Ann Clin Transl Neurol 2014;1:996
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Elacridar is used as P glycoprotein transporter blocker to enhance drug penetration in iPsc derived endothelial cell co cultured with ALS astrocytes.