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Merck
모든 사진(1)

주요 문서

SML0486

Sigma-Aldrich

Elacridar

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

동의어(들):

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

실험식(Hill 표기법):
C34H33N3O5
CAS Number:
Molecular Weight:
563.64
MDL number:
UNSPSC 코드:
12161501
PubChem Substance ID:
NACRES:
NA.77

제품명

Elacridar, ≥98% (HPLC)

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

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

배송 상태

wet ice

저장 온도

−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

애플리케이션

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)

생화학적/생리학적 작용

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).

특징 및 장점

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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문서 라이브러리 방문

Thomas Wanek et al.
European journal of nuclear medicine and molecular imaging, 39(1), 149-159 (2011-10-11)
One important mechanism for chemoresistance of tumours is overexpression of the adenosine triphosphate-binding cassette transporter P-glycoprotein (Pgp). Pgp reduces intracellular concentrations of chemotherapeutic drugs. The aim of this study was to compare the suitability of the radiolabelled Pgp inhibitors [(11)C]tariquidar
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
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

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