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Ko 143 {[allProObj[0].p_purity_real_show]}

货号:A414772 Ambeed 开学季,买赠积分,赢豪礼

Ko 143是一种高效且选择性的 ATP 结合盒亚家族 G 成员 2 (ABCG2/BCRP) 抑制剂,显示出对 P-gp 和 MRP-1 转运蛋白超过 200 倍的选择性。

Ko 143 化学结构 CAS号:461054-93-3
Ko 143 化学结构
CAS号:461054-93-3
Ko 143 3D分子结构
CAS号:461054-93-3
Ko 143 化学结构 CAS号:461054-93-3
Ko 143 3D分子结构 CAS号:461054-93-3
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Ko 143 纯度/质量文件 产品仅供科研

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Ko 143 生物活性

描述 Ko 143, a potent inhibitor specific to ATP-binding cassette subfamily G member 2 (ABCG2/BCRP), exhibits over 200-fold selectivity against P-gp and MRP-1 transporters[1][2]. At a concentration of 10 nM, Ko 143 notably reduces the IC50 of MTX for HEK G2 cells and mouse G2 cells by 2.5 times. However, Ko143 metabolites, ranging from 1-100 μM, do not affect the function of ABC Transporters[1]. The drug resistance reversal in Topotecan-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells is achieved by the FTC analogue Ko 143, applied at 0, 1, or 8 times the EC90 concentration of 25 nM[2]. Ko 143 also blocks the BCRP-mediated transport of ZD 4522 in both wild type Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC cells and mutant MDCK2-BCRP421AA cells[3].

Ko 143 动物研究

Animal study When administered orally at 10 mg/kg, Ko 143 enhances the bioavailability of SKF 104864A in mice and significantly alters the pharmacokinetics of ZD 4522 in rats[2][3].

Ko 143 参考文献

[1]Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93.

[2]JD Allen et al. Potent and Specific Inhibition of the Breast Cancer Resistance Protein Multidrug Transporter in Vitro and in Mouse Intestine by a Novel Analogue of Fumitremorgin C. Mol. Cancer Ther. 2002, 1, 417-425.

[3]Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25.

Ko 143 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.30mL

4.26mL

2.13mL

Ko 143 技术信息

CAS号461054-93-3
分子式C26H35N3O5
分子量 469.573
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(223.61 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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