Ko143

製品コードS7043 バッチS704301

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₆H₃₅N₃O₅

分子量

469.57

CAS No.

461054-93-3

Solubility (25°C)*

体外

DMSO

94 mg/mL (200.18 mM)

Ethanol

94 mg/mL (200.18 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.35mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 47 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.78mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 15.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	KO143 is a potent and relatively selective ATP-binding cassette sub-family G member 2 (ABCG2/BCRP) inhibitor. KO143 decreases the ATPase activity of ABCG2 with IC50 of 9.7 nM.
in vitro	Ko143, a nontoxic analog of fungal toxin fumitremorgin C, is a potent inhibitor of ABCG2. Ko143 has an effect on the transport activity of both ABCB1 and ABCC1. Furthermore, Ko143 is found to be unstable in rat plasma. These findings indicate that Ko143 lacks specificity for ABCG2.^[1]
in vivo	[¹¹C]Ko143 is extensively metabolized in vivo and unidentified radiolabeled metabolites are found in all investigated tissues. [¹¹C]Ko143 and possibly its radiolabeled metabolites are transported by Abcb1a and not by Abcg2 at the mouse blood-brain barrier. [¹¹C]Ko143-derived radioactivity undergoes both hepatobiliary and urinary excretion, with Abcg2 playing a possible role in mediating the transport of radiolabeled metabolites of [¹¹C]Ko143 from the kidney into urine.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK-293 cells, HEK PC cells, MCF-7 cells
	濃度	1 μM
	反応時間	0 - 45 min
	実験の流れ	Cells are seeded at a density of 2.5×10⁵ cells/ml media per well in a 24-well plate. A time-course assay is performed to determine the time at which a stable level of [³H]Ko143 is reached, as follows: media containing [³H]Ko143 is added to each well and subsequently aspirated at specific time points between 0 and 45 minutes. Three wells receive nonradioactive media to account for background signal, whereas another three are reserved for cell counts to standardize.
動物実験	動物モデル	female wild-type, Abcg2(-/-), Abcb1a/b(-/-) and Abcb1a/b(-/-)Abcg2(-/-) mice with a FVB genetic background
	投薬量	10 mg/kg
	投与方法	IV

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Modern Day Heracles: Patient-derived Liver Organoids to Model Rare Pediatric Liver Diseases [ DSpace, 2023, 10.33540/2012]	PubMed: none
Heat Shock Protein 90 Triggers Multi-Drug Resistance of Ovarian Cancer via AKT/GSK3β/β-Catenin Signaling [ Front Oncol, 2021, 11:620907]	PubMed: 33738259

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。