Elacridar - CAS 143664-11-3
Catalog number: B0084-311800
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
P-glycoprotein
Description:
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.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-311800 100 mg $198 In stock
Bulk Inquiry
Publictions citing BOC Sciences Products
  • >> More
Appearance:
Yellow solid powder
Synonyms:
GF120918; GF-120918; GF 120918; GF-120918A; GF120918A; GF 120918A; GG 918; D03968. Elacridar hydrochloride.
MSDS:
Inquire
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related P-glycoprotein Products


Tariquidar methanesulfonate hydrate
(CAS: 625375-83-9)

Tariquidar methanesulfonate is a potent and selective noncompetitive inhibitor of P-glycoprotein(Kd =5.1 nM)

MC70
(CAS: 1031367-64-2)

MC70 is a potent and selective modulator of P-glycoprotein(P-gp) with EC50 value of 0.69 μM. It is also an inhibitor of the ABC transporter ABCB1 (aka MDR1). It...

Dofequidar fumarate
(CAS: 153653-30-6)

Dofequidar fumarate, a quinoline derivative, is a multidrug resistance (MDR)-reversing quinoline derivative by inhibiting ABCB1/P-gp, ABCC1/MDR-associated prote...

CAS 143664-11-3 Elacridar

Elacridar
(CAS: 143664-11-3)

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 i...

CAS 142716-85-6 CP 100356

CP 100356
(CAS: 142716-85-6)

CP 100356 is a high affinity P-glycoprotein inhibitor.Ki value is 58 nM for mouse Pgp1a and 94nMfor Pgp1b isoforms. It can Inhibit calcein-AM uptake in MDR1-tra...

CAS 129716-58-1 Dofequidar

Dofequidar
(CAS: 129716-58-1)

Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein...

CAS 121584-18-7 Valspodar

Valspodar
(CAS: 121584-18-7)

Valspodar, P-glycoprotein (P-gp) modulator; inhibits P-gp-mediated multidrug-resistance (MDR). Reverses resistance to several cytotoxic drugs including mitoxant...

CAS 143851-98-3 Elacridar hydrochloride

Elacridar hydrochloride
(CAS: 143851-98-3)

Elacridar hydrochloride, the hydrochloride salt form of Elacridar, is an oral P-glycoprotein (P-gp) inhibitor both in vitro and in vivo. Elacridar is a dual inh...

CAS 159997-94-1 Biricodar

Biricodar
(CAS: 159997-94-1)

Biricodar, also known as VX-710 or INCEL, is a novel compound that binds directly to P-gp. VX-710 concentrations of 0.5 to 2.5 M are sufficient to fully restore...

HM-30181 mesylate
(CAS: 849675-87-2)

HM30181 is a P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. HM30181 showed the highest potency among sev...

CAS 167465-36-3 Zosuquidar trihydrochloride

Zosuquidar trihydrochloride
(CAS: 167465-36-3)

Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with a Ki value of 60 nM.

CAS 140646-80-6 MCI826

MCI826
(CAS: 140646-80-6)

MCI-826 potently antagonized LTD4- and LTE4-induced contractions at extremely low concentrations in the isolated guinea pig trachea with pA2 values of 8.3 and 8...

CAS 206873-63-4 Tariquidar

Tariquidar
(CAS: 206873-63-4)

Tariquidar, also known as XR9576, is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-compe...

CAS 167354-41-8 Zosuquidar

Zosuquidar
(CAS: 167354-41-8)

Zosuquidar, also called as LY335979, a cyclopropyldibenzosuberane, was developed as an inhibitor of P-glycoprotein (P-gp). It is undergoing testing in a phase I...

HM-30181 hydrochloride
(CAS: 849675-88-3)

HM30181 is a P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. HM30181 showed the highest potency among sev...

MC70 hydrochloride

MC70 hydrochloride is the hydrochloride salt form of MC70, which is a potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μ...

HM-30181 mesylate
(CAS: 49675-66-7)

HM30181 is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. HM30181 showed the highest potency (IC...

Chemical Structure

CAS 143664-11-3 Elacridar

Quick Inquiry

Verification code

Featured Items