| Bioactivity | DC371739 is a potent and orally activity PCSK9 inhibitor. DC371739 decreases the mRNA expression of PCSK9 and ANGPTL3. DC371739 decreases the protein expression of PCSK9 and increases the protein expression of LDLR. DC371739 has the potential for the research of hyperlipidemia[1][2]. |
| Invitro | DC371739 (0-10 µM, 0-24 h) 以剂量和时间依赖的方式增加 HepG2 细胞中 DiI-LDL 摄取率[2]。DC371739 (0-5 µM; 4, 24, 48 h) 降低 HepG2 细胞中 PCSK9 和 ANGPTL3 的 mRNA 表达[2]。DC371739 (0-10 µM;24 h) 降低 PCSK9 的蛋白质表达并增加 LDLR 的蛋白质表达[2]。DC371739 (5µM; 24 h) 通过靶向 HNF-1α 抑制 ANGPTL3 转录和表达[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> DC371739 相关抗体: RT-PCR[2] Cell Line: |
| In Vivo | DC371739 (10, 30, 100 mg/kg; p.o.; daily for 21 days) 可降低仓鼠血浆中总胆固醇 (TC)、低密度脂蛋白胆固醇 (LDL-C) 和甘油三酯的水平[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 2135765-21-6 |
| Formula | C29H30N2O4 |
| Molar Mass | 470.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Bao X, et al. Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside. Signal Transduct Target Ther. 2024 Jan 8;9(1):13. [2]. Wang J, et al. Identification and evaluation of a lipid-lowering small compound in preclinical models and in a Phase I trial. Cell Metab. 2022 May 3;34(5):667-680.e6. |
DC371739
CAS: 2135765-21-6 F: C29H30N2O4 W: 470.56
DC371739 is a potent and orally activity PCSK9 inhibitor. DC371739 decreases the mRNA expression of PCSK9 and ANGPTL3. D
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