Elacridar HCl Inhibitor CAS No. 143851-98-3

Cat. No.	Name	Size	Price
KI1482	Elacridar HCl	20 mg	$670
	Elacridar HCl	50 mg	$1204
	Elacridar HCl	100 mg	$1990

Chemical Characteristic

Product Name	Elacridar HCl
CAS No.	143851-98-3
Molecular Weight	600.1
Formula	C₃₄H₃₃N₃O₅.HCl
Chemical Name	N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide;hydrochloride
Smiles	c1ccc(c2[nH]c3c(cccc3c(=O)c12)OC)C(=O)Nc1ccc(cc1)CCN1Cc2c(CC1)cc(c(c2)OC)OC Cl
Chemical Structure
Documents	HNMR HPLC-220nm HPLC-254nm MS

Biological activities

Elacridar HCl is a specific P-glycoprotein (P-gp) inhibitor. Elacridar HCl fully reverses multidrug resistance (MDR) at 50 to 100 nM and is half maximally active at 20 nM. In CHRC5 cells, Elacridar HCl (10-100 nM) enhances the uptake of [3H]daunorubicin and blocks the efflux from preloaded cells. Elacridar HCl is still active several hours after being taken away from the culture medium showing that Elacridar HCl is not effluxed rapidly by P-glycoprotein.^[1] In vitro, elacridar HCl is able to sensitize both S1-B1-20, a subline expressing Pgp, and S1-M1-80, a subline expressing a newly identified mitoxantrone transporter, MXR.^[2] Elacridar HCl increases the absorption and decreases the secretion of fexofenadine across Caco-2 monolayers in vitro.^[3]After i.v. administration to mice in vivo, elacridar HCl penetrates thoroughly various organs that have a tissue level/blood level ratio above 10. Elacridar HCl is also well absorbed after p.o. administration. In mice implanted i.p. with the MDR P388/Dox tumor, a single i.v. or p.o. dose of elacridar HCl restores sensitivity of the tumor to a single i.p. dose (5 mg/kg) of doxorubicin administered 1 hour later, showing a statistically significant effect at 1 mg/kg elacridar HCl i.v. and maximal effect at 5 mg/kg elacridar HCl .^[1]

References

[1] Hyafil F, et al. In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 1993, 53(19): 4595-4602. [2] de Bruin M, et al. Reversal of resistance by GF120918 in cell lines expressing the ABC half-transporter, MXR. Cancer Lett. 1999, 146(2): 117-126. [3] Petri N, et al. Transport characteristics of fexofenadine in the Caco-2 cell model. Pharm Res. 2004, 21(8): 1398-1404.

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