Ko143 hydrate - CAS:461054-93-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Ko143 hydrate
英文名称:	Ko143 hydrate
别名:	(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 tert-Butyl 3-((3S,6S,12aS)-6-isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydropyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl)propanoate
CAS No:	461054-93-3	分子式:	C₂₆H₃₅N₃O₅	分子量:	469.57
CAS No:	461054-93-3
分子式:	C₂₆H₃₅N₃O₅
分子量:	469.57

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

K10127 Ko143 hydrate ≥98% (psaitong)

相关产品

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℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果