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リコンビナント
expressed in human cells (expressed in proprietary human “M” cells)
フォーム
liquid
濃度
5.0 mg/mL
色
off-white
UniProtアクセッション番号
輸送温度
dry ice
保管温度
−70°C
遺伝子情報
human ... ABCG2(9429)
詳細
Membrane Preparations for Vesicular Transport Assays (VT) are suitable for general drug-efflux transporter interaction studies. Both substrate and inhibitor interactions can be assessed using vesicles. The success of substrate interaction studies strongly depends on the passive permeability of the compound. High permeability substrates might not be detected. Control Membranes with no-, or significantly lower transporter activity are also available.
アプリケーション
In the vesicular transport assay so-called "inside-out" membrane vesicles containing ABC transporters are applied. Incubating substrates of the respective efflux transporter in the presence of the inverted membrane vesicles and ATP will allow measuring accumulation of the substrates into the vesicles. In many cases radiolabeled reporter substrates are used but recently SOLVO developed the new PREDIVEZ Vesicular Transport Kits that use fluorescent reporter substrates.
The standard vesicular transport assay is an inhibitory assay performed with cold test articles. This assay provides information on any interaction between the ABC transporter and the test article. The transport of the reporter substrate is measured in the presence of the test article (typically in 7 concentrations) and IC50 is defined as the concentration inhibiting the transport of the reporter substrate by 50%.
Should radiolabeled form of the investigated compound or adequate analytical methods (LC/MS, HPLC) be available, the vesicular transport assay may be performed in a direct format without the reporter substrate and may identify substrate nature of the test article. The vesicular transport substrate assay is a low throughput assay. It is suitable for low permeability test compounds as high permeability compounds may escape from the vesicles through the lipid bilayer.
PREDIVEZ vesicular transport kit is sold separately. This transporter membrane vesicle assay requires the PREDIVEZ vesicular transport kit and corresponding control membrane below:
SB PREDIVEZ Reagent Kit for BCRP part number SBPVR4-9RXN and corresponding control membrane SB-M-CTRL part number SBCT02-1EA
The standard vesicular transport assay is an inhibitory assay performed with cold test articles. This assay provides information on any interaction between the ABC transporter and the test article. The transport of the reporter substrate is measured in the presence of the test article (typically in 7 concentrations) and IC50 is defined as the concentration inhibiting the transport of the reporter substrate by 50%.
Should radiolabeled form of the investigated compound or adequate analytical methods (LC/MS, HPLC) be available, the vesicular transport assay may be performed in a direct format without the reporter substrate and may identify substrate nature of the test article. The vesicular transport substrate assay is a low throughput assay. It is suitable for low permeability test compounds as high permeability compounds may escape from the vesicles through the lipid bilayer.
PREDIVEZ vesicular transport kit is sold separately. This transporter membrane vesicle assay requires the PREDIVEZ vesicular transport kit and corresponding control membrane below:
SB PREDIVEZ Reagent Kit for BCRP part number SBPVR4-9RXN and corresponding control membrane SB-M-CTRL part number SBCT02-1EA
物理的形状
Supplied as frozen membrane vesicles, containing 5 mg/ml membrane protein, labeled with volume, catalog number (transporter) and date of production.
法的情報
SOLVO Biotechnology, Inc.より提供。
関連製品
製品番号
詳細
価格
保管分類コード
12 - Non Combustible Liquids
WGK
WGK 2
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
SBVT09-1EA:
最新バージョンのいずれかを選択してください：
Albert Mennone et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(10), 1673-1678 (2010-07-06)
Breast cancer resistance protein (Bcrp) is a member of the ATP-binding cassette membrane transporter family, which is expressed apically in liver, kidney, and intestine epithelium. Recent reports suggest that in addition to xenobiotics, porphyrins, and food toxins, Bcrp can also
Márton Jani et al.
Journal of pharmaceutical sciences, 100(1), 94-97 (2010-06-25)
Ivermectin is an antiparasitic drug frequently administered to humans. It has a limited brain exposure that is attributed to the efflux activity of ABCB1/Abcb1. ABCG2/Abcg2 is also a major transporter present in most pharmacologically important barriers. However, interaction of ivermectin
M Maliepaard et al.
Cancer research, 61(8), 3458-3464 (2001-04-20)
High expression of the Breast Cancer Resistance Protein (BCRP) gene has been shown to be involved in resistance to chemotherapeutic drugs. Knowledge of the localization of BCRP protein in normal tissues may help unravel the normal function of this protein.
Márton Jani et al.
Biological & pharmaceutical bulletin, 32(3), 497-499 (2009-03-03)
The pharmacokinetics of sulfasalazine, an anti-inflammatory drug is influenced by ATP-binding cassette G2 (ABCG2) (breast cancer resistance protein (BCRP), mitoxantrone resistance protein (MXR)) both in vitro and clinically. Due to its low passive permeability, the intracellular concentration of sulfasalazine is
Hiroshi Kodaira et al.
The Journal of pharmacology and experimental therapeutics, 333(3), 788-796 (2010-03-23)
A synergistic effect of P-glycoprotein (P-gp)/Abcb1a and breast cancer resistance protein (Bcrp)/Abcg2 was reported to limit the brain penetration of their common substrates. This study investigated this based on pharmacokinetics using Mdr1a/1b(-/-), Bcrp(-/-), and Mdr1a/1b(-/-)/Bcrp(-/-) mice. Comparison of the brain-
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