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Ko143 hydrate  ≥98%

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包装规格：5mg 25mg 50mg in glass bottle
溶解性：溶于DMSO(≥50mg/ml）
产品描述：基本信息 产品编号： K10127  产品名称： Ko143 hydrate CAS: 461054-93-3   储存条件 粉末 -20℃ 四年     分子式： C26H35N3O5 溶于液体 -80℃ 6个月 分子量： 469.57 -20℃ 1个月 化学名：  Ko-143 hydrate,(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1′,2′:1,6]pyrido[3,4- b]indole-3-propanoic acid 1,1-dimethylethyl ester hydrate Solubility (25°C)：   体外:   DMSO 94mg/mL (200.18mM) Ethanol 94mg/mL (200.18mM) Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.1296mL 10.6480 mL 21.2961mL 5mM 0.4259mL 2.1296 mL 4.2592mL 10mM 0.2130mL 1.0648 mL 2.1296mL   生物活性 产品描述 一种有效且选择性的ATP结合盒亚家族G成员2(ABCG2/BCRP)抑制剂。 靶点 EC90:26nM (BCRP)   体外研究 Ko143 (10nM) significantly decreases (2.5-fold) the IC50 of MTX for HEK G2 cells and mouse G2 cells.Ko143 (1-100μM) metabolite does not inhibit the function of ABC Transporters.Reversal of drug resistance in SKF 104864A-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells by FTC analogue Ko143.Ko143 is applied at zero,one,or eight times the EC90 concentration of 25nM.Ko143 inhibits BCRP-mediated transport of ZD 4522 in Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC (wild type) cells and MDCK2-BCRP421AA (mutant type) cells. 体内研究 Ko143 (10mg/kg,p.o.) increases the oral availability of SKF 104864A in mice.Ko143 significantly affects the pharmacokinetics of ZD 4522 in rats.   推荐实验方法(仅供参考) 细胞实验:   cells are plated at 400 or 1000/well in 96-well plates the night before addition of drugs.A concentration series of 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 0.1μm PSC833 to inhibit confounding P-gp activity.   动物实验:   Oral toxicity of FTC analogues in mice is tested by mixing 50mg/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 10μL/g of body weight.Pairs of mice are administered oral doses of 50mg/kg Ko132,Ko134,Ko143,or vehicle under light methoxyflurane anesthesia.Final tests of 50mg/kg Ko134 or Ko143 are performed on additional pairs of unanesthetized animals to observe any behavioral effects.Further,another pair of mice receive the higher dose of 100mg/kg Ko134.For i.p.toxicity tests,the FTC analogue stocks in DMSO are dispersed in at least 10 volumes of sterile corn oil such that the injected volume is 5μL/g of body weight.After pilot tests at lower doses show no adverse effects,mice (4 per group) are administered vehicle or 10mg/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 including brain,salivary glands,heart,lungs,liver,adrenal glands,kidneys,urinary tract,spleen,thymus,bone marrow,pancreas,stomach,intestines,cecum,colon,testes,epididymus,skin,head,trunk,and limbs.
保存条件：-20℃

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