SML0486

Elacridar

Name: Elacridar
Brand: SIGMA

≥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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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):

C₃₄H₃₃N₃O₅

CAS 번호:

143664-11-3

Molecular Weight:

563.64

MDL number:

MFCD00912604

UNSPSC 코드:

12161501

PubChem Substance ID:

329825437

NACRES:

NA.77

주요 문서

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제품 이름

Elacridar, ≥98% (HPLC)

Quality Level

100

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

A comparative small-animal PET evaluation of [11C]tariquidar, [11C]elacridar and (R)-[11C]verapamil for detection of P-glycoprotein-expressing murine breast cancer.

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

Evaluation of the P-glycoprotein- and breast cancer resistance protein-mediated brain penetration of 11C-labeled topotecan using small-animal positron emission tomography.

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)

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

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문서

Discover Bioactive Small Molecules for ADME/Tox

Elacridar

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

크기 선택

제품정보 (DICE 배송 시 비용 별도)

주요 문서

속성

제품 이름

Quality Level

분석

양식

색상

solubility

배송 상태

저장 온도

SMILES string

InChI

InChI key

관련 카테고리

설명

애플리케이션

생화학적/생리학적 작용

특징 및 장점

안전성 정보

Storage Class Code

WGK

Flash Point (°F)

Flash Point (°C)

문서

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