Elacridar

• CAT Number: I001687
• CAS Number: 143664-11-3
• Molecular Formula: C34H33N3O5
• Molecular Weight: 563.6
• Purity: ≥95%
• Target: P-glycoprotein
• Solubility: 10 mM in DMSO
• Storage: -20°C
• InChIKey: OSFCMRGOZNQUSW-UHFFFAOYSA-N

Elacridar (CAT: I001687), also known as GF120918 or GW0918, acts as a potent inhibitor of P-glycoprotein (Pgp), a transporter pivotal in drug efflux. Its versatile utility spans in vitro and in vivo applications, serving as a tool inhibitor to explore transporters’ role in the distribution of diverse test molecules. By suppressing Pgp activity, Elacridar unveils insights into drug interactions, bioavailability, and distribution, contributing to safer pharmaceutical development. 

Reference

[1]. Sane R, Mittapalli RK, Elmquist WF. Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci. 2013 Jan 18.

[2]. Bankstahl JP, Bankstahl M, Romermann K, et al. Tariquidar and Elacridar Are Dose-Dependently Transported by P-Glycoprotein and Bcrp at the Blood-Brain Barrier: A Small-Animal PET and In-Vitro Study. Drug Metab Dispos. 2013 Jan 10.

[3]. Sane R, Agarwal S, Elmquist WF. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.

[4]. Tang SC, Lagas JS, Lankheet NA, et al. Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. Int J Cancer. 2012 Jan 1;130(1):223-33. doi: 10.1002/ijc.26000.

[5]. Kuppens IE, Witteveen EO, Jewell RC, et al. A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res. 2007 Jun 1;13(11):3276-85.