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SML0486

Elacridar

≥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:
Molecular Weight:
563.64
UNSPSC Code:
12161501
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Pricing and availability is not currently available.
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Product Name

Elacridar, ≥98% (HPLC)

Quality Level

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

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

Application

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

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.

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1 of 1

This Item
SML1297SML1790SML1184
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)

color

white to beige

color

white to beige

color

white to light brown

color

white to beige


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Christopher Rowbottom et al.
Pharmacology research & perspectives, 9(2), e00740-e00740 (2021-03-05)
Transporters can play a key role in the absorption, distribution, metabolism, and excretion of drugs. Understanding these contributions early in drug discovery allows for more accurate projection of the clinical pharmacokinetics. One method to assess the impact of transporters in
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)
Tomoteru Yamasaki et al.
Nuclear medicine and biology, 38(5), 707-714 (2011-07-02)
Topotecan (TPT) is a camptothecin derivative and is an anticancer drug working as a topoisomerase-I-specific inhibitor. But TPT cannot penetrate through the blood-brain barrier. In this study, we synthesized a new positron emission tomography (PET) probe, [(11)C]TPT, to evaluate the



Global Trade Item Number

SKUGTIN
SML0486-10MG04061837084652
SML0486-50MG04061837084669

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