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网站主页 (3S,6S,12aS)-1,2,3,4,6,7,12,12a-八氢-9-甲氧基-6-(2-甲基丙基)-1,4-二氧代吡嗪并[1',2':1,6]吡啶并[3,4-b]吲哚-3-丙酸叔丁酯 化合物 Ko 143
  • 化合物 Ko 143|TQ0186|TargetMol

化合物 Ko 143|TQ0186|TargetMol

Ko 143
461054-93-3
￥348 1mg 起订
￥493 2mg 起订
￥771 5mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐
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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 Ko 143
英文名称：
Ko 143
CAS号：
461054-93-3
品牌：
TargetMol
产地：
美国
保存条件：
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.89%
产品类别：
抑制剂
货号：
TQ0186

Product Introduction

Bioactivity

NameKo 143
DescriptionKo 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).
Cell ResearchCells 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].
Animal ResearchOral 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].
In vitro在HEK G2细胞和鼠标G2细胞中，Ko143 (10 nM) 显著降低了MTX的IC50值。Ko143 (1-100 μM) 的代谢物并不抑制ABC转运蛋白的功能[1]。在经SKF 104864A选育的鼠标MEF3.8/T6400细胞和人IGROV1/T8细胞中，Ko143能够逆转药物抗性[2]。Ko143抑制了在Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC（野生型）细胞和MDCK2-BCRP421AA（突变型）细胞中BCRP介导的ZD 4522运输[3]。
In vivoKo143（10 mg/kg，p.o.）在小鼠中提高了SKF 104864A的口服可用性[2]。
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : Insoluble
DMSO : 90 mg/mL (191.66 mM), Sonication is recommended.
KeywordsBCRP | Breast cancer resistance protein | ABCG2 | Ko-143 | Inhibitor | Ko143 | inhibit | Ko 143
Inhibitors RelatedChlorpropamide | Acridone | Elacridar | Vigabatrin | Probucol | Thiethylperazine dimaleate | DIDS sodium salt | Prazosin hydrochloride | Novobiocin Sodium | Vismodegib | Glipizide | GS-9191 PM
Related Compound LibrariesInhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Membrane Protein-targeted Compound Library
BCRP|||Breast cancer resistance protein|||ABCG2|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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