KPLH1130是一种特异性的丙酮酸脱氢酶激酶(PDK)抑制剂,能够有效阻断巨噬细胞的极化并减轻促炎反应。该化合物在高脂饮食小鼠模型中显示出改善葡萄糖耐受性的潜力,适用于研究代谢疾病和炎症相关疾病。


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| 描述 | KPLH1130 is a selective inhibitor of pyruvate dehydrogenase kinase (PDK), which inhibits macrophage polarization and reduces proinflammatory reactions. Furthermore, KPLH1130 enhances glucose tolerance in mice fed with a high-fat diet (HFD)[1]. |
| Concentration | Treated Time | Description | References | |
| PMs | 10 µM | 12 h | To evaluate the effect of KPLH1130 on M1 polarization of macrophages. | Front Immunol. 2019 May 7;10:944. |
| BMDMs | 10 µM | 12 h | To evaluate the effect of KPLH1130 on M1 polarization of macrophages. | Front Immunol. 2019 May 7;10:944. |
| HD11 cells | 7 μM | 24 h | Inhibited DEHP-induced M1 polarization and promoted M2 polarization in HD11 cells | Poult Sci. 2025 Jan;104(1):104558. |
| hUC-MSCs | 10 μM | 1 h | Inhibits pyruvate dehydrogenase kinase activity, affecting the immunosuppressive function of hUC-MSCs | Life Sci Alliance. 2022 Sep 9;5(12):e202201493. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | High-fat diet-induced obesity model | 70 mg/kg | 4 weeks | Evaluate the effect of KPLH1130 on high-fat diet-induced insulin resistance, results showed that KPLH1130 significantly improved glucose tolerance and insulin sensitivity | Front Immunol. 2019 May 7;10:944. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.53mL 0.71mL 0.35mL |
17.65mL 3.53mL 1.77mL |
35.30mL 7.06mL 3.53mL |
|
| CAS号 | 906669-07-6 |
| 分子式 | C15H13N3O3 |
| 分子量 | 283.28 |
| SMILES Code | O=C1NN=C(N1C2=CC=C(C)C=C2)C3=C(O)C=C(O)C=C3 |
| MDL No. | MFCD32067959 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 130 mg/mL(458.91 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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