质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
颜色
white to beige
溶解性
H2O: 2 mg/mL, clear (Warmed)
储存温度
-10 to -25°C
SMILES字符串
Cl.[n]2(ncc(c2)c3c4c(ccc3)C(=O)c5c(cccc5)C4=O)C1CCNCC1
InChI key
ZIMLKZKPNALXKK-UHFFFAOYSA-N
生化/生理作用
Potent, orally active PDK4 inhibitor with antidiabetic and anticancer efficacy.
PDK4-IN-1 (PDK4i-8c) is a cell-penetrating anthraquinone derivative that has been identified as an allosteric inhibitor of pyruvate dehydrogenase kinase 4 (PDK4), whis is binding to its lipoamide binding site with a high affinity (IC50 = 84 nM). PDK4-IN-1 is orally available, demonstrates excellent metabolic stability, and exhibits a promising pharmacokinetic profile in rat studies. Moreover, PDK4-IN-1 substantially enhances glucose tolerance in mice with diet-induced obesity and mitigates allergic reactions in a passive cutaneous anaphylaxis mouse model. The in vivo data support its effectiveness as a potential treatment for diabetes. Additionally, PDK4-IN shows notable anticancer properties by regulating cell proliferation, transformation, and apoptosis.
PDK4-IN-1 (PDK4i-8c) is a cell-penetrating anthraquinone derivative that has been identified as an allosteric inhibitor of pyruvate dehydrogenase kinase 4 (PDK4), whis is binding to its lipoamide binding site with a high affinity (IC50 = 84 nM). PDK4-IN-1 is orally available, demonstrates excellent metabolic stability, and exhibits a promising pharmacokinetic profile in rat studies. Moreover, PDK4-IN-1 substantially enhances glucose tolerance in mice with diet-induced obesity and mitigates allergic reactions in a passive cutaneous anaphylaxis mouse model. The in vivo data support its effectiveness as a potential treatment for diabetes. Additionally, PDK4-IN shows notable anticancer properties by regulating cell proliferation, transformation, and apoptosis.
免责声明
Hygroscopic
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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