化合物 Ko 143|TQ0186|TargetMol

價(jià)格	￥348	￥493	￥771
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2026-04-02

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產(chǎn)品詳情

中文名稱:化合物 Ko 143	英文名稱:Ko 143
CAS:461054-93-3	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Store at low temperature Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 99.46%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): TQ0186

Product Introduction

Bioactivity

名稱	Ko 143
描述	Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).
細(xì)胞實(shí)驗(yàn)	Cells are plated at 400 or 1000/well in 96-well plates the night before the addition of drugs. A concentration series of the drug is applied along one plate axis and left for the duration of the assay. Plates are harvested after 4-5 days while untreated wells are still subconfluent. Relative cell proliferation is quantified with CyQuant or Sybr Green I fluorescent nucleic acid stains. Assays with human cell lines are performed in the presence of 0.1 μm PSC833 to inhibit confounding P-gp activity [2].
動(dòng)物實(shí)驗(yàn)	Oral toxicity of FTC analogs in mice is tested by mixing 50 mg/mL stocks in DMSO 1:1 with Tween 80 (polyoxyethylene sorbitan mono-oleate) and diluting with 5% w/v glucose such that the final volume administered by oral gavage is 10 μL/g of body weight. Pairs of mice are administered oral doses of 50 mg/kg Ko132, Ko134, Ko143, or vehicle under light methoxyflurane anesthesia. Final tests of 50 mg/kg Ko134 or Ko143 are performed on additional pairs of unanesthetized animals to observe any behavioral effects. Further, another pair of mice receive a higher dose of 100 mg/kg Ko134. For i.p. toxicity tests, the FTC analog stocks in DMSO are dispersed in at least 10 volumes of sterile corn oil such that the injected volume is 5 μL/g of body weight. After pilot tests at lower doses show no adverse effects, mice (4 per group) are administered vehicle or 10 mg/kg i.p. of Ko132, Ko134, or Ko143. The mice are observed continuously during the first hour after administration and then at increasing intervals for 2 weeks, after which they are sacrificed for histological examination of major organs and structures [2].
體外活性	在HEK G2細(xì)胞和鼠標(biāo)G2細(xì)胞中，Ko143 (10 nM) 顯著降低了MTX的IC50值。Ko143 (1-100 μM) 的代謝物并不抑制ABC轉(zhuǎn)運(yùn)蛋白的功能[1]。在經(jīng)SKF 104864A選育的鼠標(biāo)MEF3.8/T6400細(xì)胞和人IGROV1/T8細(xì)胞中，Ko143能夠逆轉(zhuǎn)藥物抗性[2]。Ko143抑制了在Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC（野生型）細(xì)胞和MDCK2-BCRP421AA（突變型）細(xì)胞中BCRP介導(dǎo)的ZD 4522運(yùn)輸[3]。
體內(nèi)活性	Ko143（10 mg/kg，p.o.）在小鼠中提高了SKF 104864A的口服可用性[2]。
存儲(chǔ)條件	Store at low temperature Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	H2O : Insoluble DMSO : 90 mg/mL (191.66 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.03 mM), Sonication is recommended.
關(guān)鍵字	Ko-143 \| Ko143 \| Ko 143 \| Inhibitor \| inhibit \| Breast cancer resistance protein \| BCRP \| ABCG2
相關(guān)產(chǎn)品	Chlorpropamide \| Acridone \| Elacridar \| Vigabatrin \| Probucol \| Isoxazole \| Thiethylperazine dimaleate \| Moxidectin \| DIDS sodium salt \| Prazosin hydrochloride \| Vismodegib \| Glipizide
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌化合物庫(kù) \| 已知活性化合物庫(kù) \| 多靶點(diǎn)化合物庫(kù) \| 膜蛋白靶向化合物庫(kù)

關(guān)鍵字： BCRP|||Breast cancer resistance protein|||ABCG2|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類(lèi)型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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