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Merck

SML0486

Elacridar

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

Sinônimo(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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10 MG

R$ 877,00

50 MG

R$ 3.522,00

R$ 877,00


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Sobre este item

Fórmula empírica (Notação de Hill):
C34H33N3O5
Número CAS:
Peso molecular:
563.64
UNSPSC Code:
12161501
PubChem Substance ID:
NACRES:
NA.77
MDL number:

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Nome do produto

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

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Este Item
SML1297SML1790SML1184
Elacridar ≥98% (HPLC)

Sigma-Aldrich

SML0486

Elacridar

SB269652 ≥98% (HPLC)

Sigma-Aldrich

SML1297

SB269652

Tariquidar ≥98% (HPLC)

Sigma-Aldrich

SML1790

Tariquidar

OF-1 ≥98% (HPLC)

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.

Classe de armazenamento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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)
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
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
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)
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

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