ChemicalBook CAS数据库列表 (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

(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

CAS号:461054-93-3
英文名:Ko 143
中文名:(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
CBNumber:CB81562442
分子式:C26H35N3O5
分子量:469.57
MOL File:461054-93-3.mol

(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-丙酸叔丁酯化学性质

熔点 :147 ºC
沸点 :689.8±55.0 °C(Predicted)
密度 :1.24
储存条件 :Desiccate at -20°C
溶解度 :DMSO: >10mg/mL
形态 :powder
酸度系数(pKa) :13.31±0.60(Predicted)
颜色 :white to off-white
稳定性 :Stable for 2 years from date of purchase as supplied. Protect from exposure to moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

安全信息

(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-丙酸叔丁酯性质、用途与生产工艺

生物活性 KO143 是一种有效的、相对选择性的 ATP-binding cassette sub-family G member 2 (ABCG2/BCRP) 抑制剂。KO143 可降低ABCG2的ATPase活性，对应IC50值为9.7 nM。
靶点
Target Value
BCRP
(Cell-free assay) 9.7 nM
体外研究

Ko143 (10 nM) significantly decreases (2.5-fold) the IC ₅₀ of MTX for HEK G2 cells and mouse G2 cells. Ko143 (1-100 μM) 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 EC ₉₀ concentration of 25 nM. 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 (10 mg/kg, p.o.) increases the oral availability of SKF 104864A in mice. Ko143 significantly affects the pharmacokinetics of ZD 4522 in rats.

(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-丙酸叔丁酯上下游产品信息

上游原料

下游产品

更新日期：2024/04/30
产品编号：HY-10010
产品名称：(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 Ko 143
CAS编号：461054-93-3
包装：5mg
价格：949元

(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-丙酸叔丁酯生产厂家

461054-93-3, (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-丙酸叔丁酯相关搜索:

Target	Value
BCRP (Cell-free assay)	9.7 nM