Elacridar hydrochloride

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Cat.No. 4646 - Elacridar hydrochloride | C34H33N3O5.HCl | CAS No. 143851-98-3
Description: P-gp inhibitor
Alternative Names: GF 120918
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
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews (1)
Literature (2)

Biological Activity

P-glycoprotein (P-gp/ABCG1) inhibitor. Blocks P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs doxorubicin (Cat. No. 2252) and vincristine (Cat. No. 1257) in CHRC5 cells. Also inhibits breast cancer resistance protein (BCRP/ABCG2). Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data

M. Wt 600.1
Formula C34H33N3O5.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 143851-98-3
PubChem ID 170320
InChI Key IQOJZZHRYSSFJM-UHFFFAOYSA-N
Smiles O=C1C3=C(C(C(NC4=CC=C(CCN5CC(C=C(OC)C(OC)=C6)=C6CC5)C=C4)=O)=CC=C3)NC2=C1C=CC=C2OC.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 12 20

Preparing Stock Solutions

The following data is based on the product molecular weight 600.1. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 8.33 mL 41.66 mL 83.32 mL
1 mM 1.67 mL 8.33 mL 16.66 mL
2 mM 0.83 mL 4.17 mL 8.33 mL
10 mM 0.17 mL 0.83 mL 1.67 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Hyafil et al (1993) In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 53 4595 PMID: 8402633

Myer et al (1999) 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. Oncol Rep. 6 217 PMID: 9864431


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Keywords: Elacridar hydrochloride, Elacridar hydrochloride supplier, GF120918, P-glycoprotein, P-gp, inhibitors, inhibits, multidrug, resistance, MDR, BCRP, ABCG1, ABCG2, ABCB1, GF, 120918, Multidrug, Transporters, 4646, Tocris Bioscience

3 Citations for Elacridar hydrochloride

Citations are publications that use Tocris products. Selected citations for Elacridar hydrochloride include:

Lahmann et al (2015) Systemic Administration of Glibenclamide Fails to Achieve Therapeutic Levels in the Brain and Cerebrospinal Fluid of Rodents. PLoS One 10 e0134476 PMID: 26225433

Jablonski et al (2014) Inhibiting drug efflux transporters improves efficacy of ALS therapeutics. Ann Clin Transl Neurol 1 996 PMID: 25574474

Ramesh et al (2014) Pro-inflammatory human Th17 cells selectively express P-glycoprotein and are refractory to glucocorticoids. J Exp Med 211 89 PMID: 24395888


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1uM of elacridar is used to block the p glycoprotein.
By Shashirekha Shamamandri Markandaiah on 10/29/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Endothelial cell, Astrocytes

Elacridar is used as P glycoprotein transporter blocker to enhance drug penetration in iPsc derived endothelial cell co cultured with ALS astrocytes.


Literature in this Area

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