Elacridar - CAS 143664-11-3
Catalog number: B0084-311800
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Elacridar hydrochloride (GF120918A) is a  P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.  In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.
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B0084-311800 100 mg $198 In stock
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Yellow solid powder
GF120918; GF-120918; GF 120918; GF-120918A; GF120918A; GF 120918A; GG 918; D03968. Elacridar hydrochloride.
1.Liposomes Coloaded with Elacridar and Tariquidar To Modulate the P-Glycoprotein at the Blood-Brain Barrier.
Nieto Montesinos R1, Béduneau A1, Lamprecht A1,2, Pellequer Y1. Mol Pharm. 2015 Nov 2;12(11):3829-38. doi: 10.1021/acs.molpharmaceut.5b00002. Epub 2015 Sep 29.
This study prepared three liposomal formulations coloaded with elacridar and tariquidar to overcome the P-glycoprotein-mediated efflux at the blood-brain barrier. Their pharmacokinetics, brain distribution, and impact on the model P-glycoprotein substrate, loperamide, were compared to those for the coadministration of free elacridar plus free tariquidar. After intravenous administration in rats, elacridar and tariquidar in conventional liposomes were rapidly cleared from the bloodstream. Their low levels in the brain did not improve the loperamide brain distribution. Although elacridar and tariquidar in PEGylated liposomes exhibited 2.6 and 1.9 longer half-lives than free elacridar and free tariquidar, respectively, neither their Kp for the brain nor the loperamide brain distribution was improved. However, the conjugation of OX26 F(ab')2 fragments to PEGylated liposomes increased the Kps for the brain of elacridar and tariquidar by 1.4- and 2.
2.Whole-body Distribution and Radiation Dosimetry of 11C-Elacridar and 11C-Tariquidar in Humans.
Bauer M1, Blaickner M2, Philippe C1, Wadsak W1, Hacker M1, Zeitlinger M1, Langer O1. J Nucl Med. 2016 Apr 14. pii: jnumed.116.175182. [Epub ahead of print]
11C-elacridar and11C-tariquidar are two new PET tracers to assess the transport activities of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2). This study investigates the whole-body distribution and radiation dosimetry of both radiotracers in humans.
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