2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. LXR
  4. TLC-2716

TLC-2716 是一种口服有效、局限于肠道和肝脏的 LXRα 和 LXRβ 抑制剂，EC50 分别为 7 nM 和 15 nM。TLC-2716 可抑制 LXRα/β 的转录活性，下调参与脂肪生成、脂质吸收和脂蛋白代谢的基因，并保留外周胆固醇逆向转运功能。TLC-2716 能够减少脂质蓄积，抑制炎症和纤维化基因的表达，增强富含甘油三酯的脂蛋白清除能力，同时改善葡萄糖稳态与胰岛素敏感性。TLC-2716 可在动物模型和人源化肝脏小鼠中降低血清和肝脏甘油三酯水平、血浆胆固醇水平及其他致动脉粥样硬化的血脂指标。TLC-2716 可用于血脂异常及相关心脏代谢疾病的研究。

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TLC-2716

TLC-2716 Chemical Structure

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Other Forms of TLC-2716:

TLC-2716 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TLC-2716 is an orally available, gut- and liver-restricted inhibitor against LXRα and LXRβ, with EC50 values of 7 nM and 15 nM, respectively. TLC-2716 represses LXRα/β transcriptional activity, downregulates genes involved in lipogenesis, lipid absorption and lipoprotein metabolism, and preserves peripheral reverse cholesterol transport. TLC-2716 reduces lipid accumulation, suppresses inflammation and fibrotic gene expression, enhances triglyceride-rich lipoprotein clearance, and improves glucose homeostasis and insulin sensitivity. TLC-2716 lowers serum and hepatic triglycerides, plasma cholesterol and other atherogenic lipid profiles in experimental models and humanized liver mice. TLC-2716 can be used for the research of dyslipidemia and related cardiometabolic disorders[1].

IC50 & Target[1]

LXRα

7 nM (EC50)

LXRβ

15 nM (EC50)

体外研究
(In Vitro)

TLC-2716 (4 °C 下处理 1 h) 在生化结合实验中可结合重组人源 LXRα (EC50 = 7 nM) 和 LXRβ (EC50 = 15 nM)[1]。
TLC-2716 (16 h) 可在 HEK293 哺乳动物双杂交实验中诱导 NCOR 招募至 LXRα 和 LXRβ，对应的 EC50 值分别为 8 nM 和 11 nM；并可分别在 HT‑29 和 HepG2 细胞中抑制 ABCA1 和 SREBP1c 报告基因活性，对应的 IC50 值分别为 15 nM 和 7 nM[1]。
TLC-2716 (连续 5 天) 可呈剂量依赖性降低原代人 Upcyte 肝细胞内的甘油三酯蓄积，其 EC50 为 289 nM[1]。
TLC-2716 (500 nM-5 μM; 3 days) 可在脂肪变性人肝脏类器官中剂量依赖性地降低细胞内脂质含量，并抑制 LXR 相关基因、脂质代谢相关基因、炎症相关基因及纤维化相关基因的表达，且在 GCKRTT 类器官中的作用效果更强[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TLC-2716 相关抗体:
体内研究
(In Vivo)

TLC-2716 (0.3-1 mg/kg；灌胃；每日 1 次；持续 3 周) 可通过抑制肝脏从头脂生成、降低肝脏 TG 含量及血浆 TG 和 TC 水平，且不损伤外周胆固醇逆向转运，呈剂量依赖性改善高脂饮食诱导肥胖小鼠的血脂异常[1]。
TLC-2716 (0.1-15 mg/kg；口服；每日) 可降低 ZDF 大鼠的血脂异常相关终点指标并改善糖稳态，且不会损伤肝功能[1]。
TLC-2716 (0.1-1 mg/kg；口服；每日；21 天) 可降低高脂饮食喂养的 SD 大鼠肝脏 DNL 基因的表达水平、肝脏 TG、血浆 TG 及 TC 含量，且不会损伤肝功能[1]。
TLC-2716 (1 mg/kg；口服；每日一次；连续 8 天) 可降低人源化肝脏嵌合小鼠中脂代谢基因的肝脏表达水平，并呈现出降低肝脏 TG 的趋势[1]。
TLC-2716 (15-120 mg/kg；灌胃；每日 1 次；持续 26 周) 可降低瘦型 CD-1 小鼠的血浆 TG 和 TC 水平，且未产生可见的不良反应[1]。
TLC-2716 (1-15 mg/kg；灌胃；每日 1 次；连续 28 天) 可降低食蟹猴血浆 TG 和 TC 水平，且未产生可观察到的不良反应[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male, 18 weeks old, diet-induced obese via 14 weeks high-fat diet)[1]
Dosage: 0.3 mg/kg; 1 mg/kg
Administration: p.o.; daily; 21 days
Result: Dose-dependently reduced hepatic expression of de novo lipogenesis (DNL) genes including Scd1, Fasn, Srebp1c and Acaca.
Decreased liver triglyceride (TG) content as well as area under the curve (AUC) values for plasma TG and total cholesterol (TC) at 1 mg/kg, with milder reductions observed at 0.3 mg/kg.
Maintained comparable plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels versus vehicle treatment.
Dose-dependently downregulated ileal Srebp1c expression.
Animal Model: Zucker diabetic fatty (ZDF) (male, 6-7 weeks old, obese fa/fa)[1]
Dosage: 0.1 mg/kg; 1 mg/kg; 15 mg/kg
Administration: p.o.; daily; 14 days (0.1, 1 mg/kg); p.o.; daily; 28 days (15 mg/kg)
Result: Reduced hepatic DNL gene expression, liver TG content, and AUC for plasma TG and TC at 0.1 and 1 mg/kg.
Reduced fasting plasma glucose by approximately 56% and lowered hepatic Angptl3 expression and plasma ANGPTL3 levels at 15 mg/kg.
Remained unchanged plasma ALT and AST levels relative to vehicle.
Animal Model: Sprague-Dawley (SD) (male, 6-7 weeks old, high-fat diet-induced obese)[1]
Dosage: 0.1 mg/kg; 1 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced hepatic DNL gene expression, liver TG content, and AUC for plasma TG and TC at both doses.
Remained unchanged plasma ALT and AST levels relative to vehicle.
Animal Model: PXB (male, humanized liver chimeric)[1]
Dosage: 1 mg/kg
Administration: oral gavage; once daily; 8 days
Result: Trended to reduce liver TG content.
Reduced hepatic expression of cholesterol synthesis gene HMGCR, lipid clearance gene ANGPTL3, and de novo lipogenesis genes SREBP1C, FASN, ACACA, SCD1.
Animal Model: CD-1 (male and female, lean)[1]
Dosage: 15 mg/kg; 60 mg/kg; 120 mg/kg
Administration: p.o.; daily; 182 days
Result: Reduced plasma TG and TC in both male and female mice at all doses.
Observed no adverse clinical observations, liver biochemistry changes, or histopathological signs of liver injury at any dose.
分子量

739.12

Formula

C38H22ClF3N4O5S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TLC-2716 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TLC-2716TLC2716TLC 2716LXRLiver X receptorLXRαhuman liver organoidsHEK293 cellsLXRβcynomolgus monkeysHT-29 cellsprimary human Upcyte hepatocytesDIO miceHepG2 cellsZDF ratsInhibitorinhibitorinhibit

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