SML0486

Elacridar

Name: Elacridar
Brand: SIGMA

≥98% (HPLC), powder, ABC transporters MDR-1 (P-gp) inhibitor

Synonym(s):

GF120918, GG918, GW0918, N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide

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About This Item

Empirical Formula (Hill Notation):

C₃₄H₃₃N₃O₅

CAS Number:

143664-11-3

Molecular Weight:

563.64

UNSPSC Code:

12161501

PubChem Substance ID:

329825437

NACRES:

NA.77

MDL number:

MFCD00912604

Key Documents

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Product Name

Elacridar, ≥98% (HPLC)

SMILES string

COc1cccc2C(=O)c3cccc(C(=O)Nc4ccc(CCN5CCc6cc(OC)c(OC)cc6C5)cc4)c3Nc12

InChI

1S/C34H33N3O5/c1-40-28-9-5-7-26-32(28)36-31-25(33(26)38)6-4-8-27(31)34(39)35-24-12-10-21(11-13-24)14-16-37-17-15-22-18-29(41-2)30(42-3)19-23(22)20-37/h4-13,18-19H,14-17,20H2,1-3H3,(H,35,39)(H,36,38)

InChI key

OSFCMRGOZNQUSW-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL (clear solution, warmed)

shipped in

wet ice

storage temp.

−20°C

Quality Level

100

Related Categories

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

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Show Differences

1 of 4

This Item	SML1297	SML1790	SML1184
Sigma-Aldrich SML0486 Elacridar	Sigma-Aldrich SML1297 SB269652	Sigma-Aldrich SML1790 Tariquidar	Sigma-Aldrich SML1184 OF-1
form powder	form powder	form powder	form powder
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. −20°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 2 mg/mL (clear solution, warmed)	solubility DMSO: 2 mg/mL	solubility DMSO: 10 mg/mL, clear	solubility DMSO: 5 mg/mL, clear (warmed)
shipped in wet ice	shipped in -	shipped in -	shipped in -

Application

Elacridar has been used:

as a chemical to decipher the link between autophagy and the mechanism of resistance to sunitinib[1]
as an ATP-binding cassette sub-family B member 1 inhibitor to study its effects on the NSC23766 cytotoxicity[2]
to treat rhodamine 123 (Rh123) labeled cells to set sorting gates in fluorescence-activated cell sorting (FACS)[3]

Biochem/physiol Actions

GF120918 (Elacridar) is a very potent inhibitor of the ABC transporters MDR-1 (P-gp) and BCRP. GF120918 increases the bioavailability of cytotoxic anti-tumor drugs, and also leads to increased levels of anti-HIV drugs in the brain and CNS.

GF120918 (Elacridar) is an inhibitor of MDR-1 (P-gp).

Features and Benefits

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number

0000516659

0000464197

0000424769

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The xenobiotic transporter Mdr1 enforces T cell homeostasis in the presence of intestinal bile acids

Cao W, et al.

Immunity, 47(6), 1182-1196 (2017)

Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability.

Ramola Sane et al.

Journal of pharmaceutical sciences, 102(4), 1343-1354 (2013-01-22)

The study objective was to develop a formulation of elacridar to overcome its dissolution-rate-limited bioavailability. Elacridar is a P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor that has been used to improve the brain distribution of drugs that are

PXR/CYP3A4-humanized mice for studying drug-drug interactions involving intestinal P-glycoprotein.

Nico Holmstock et al.

Molecular pharmaceutics, 10(3), 1056-1062 (2013-01-31)

Rodent models are less suitable for predicting drug-drug interactions at the level of the human intestinal mucosa, especially when nuclear receptors such as pregnane X receptor (PXR) are involved. Recently, a transgenic mouse model, expressing both human PXR and CYP3A4

Exploiting transport activity of p-glycoprotein at the blood-brain barrier for the development of peripheral cannabinoid type 1 receptor antagonists.

Hanneke G M Wittgen et al.

Molecular pharmaceutics, 9(5), 1351-1360 (2012-03-21)

Although the CB1 receptor antagonist/inverse agonist rimonabant has positive effects on weight loss and cardiometabolic risk factors, neuropsychiatric side effects have prompted researchers to develop peripherally acting derivatives. Here, we investigated for a series of 3,4-diarylpyrazoline CB1 receptor antagonists if

Resistance to sunitinib in renal clear cell carcinoma results from sequestration in lysosomes and inhibition of the autophagic flux

Giuliano S, et al.

Autophagy, 11(10), 1891-1904 (2015)

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