2. Metabolic Enzyme/Protease
  3. MMP
  4. F81-1144b

F81-1144b 是一种 MMP-1 和 MMP-3 抑制剂，其 IC50 分别为 5 nM 和 29 nM。F81-1144b 可降低血清和肝脏三酰甘油水平，减少极低密度脂蛋白-三酰甘油的分泌，抑制肝脏从头脂肪酸合成，降低血清胰岛素和葡萄糖水平。F81-1144b 可用于高甘油三酯血症的研究。

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F81-1144b

F81-1144b Chemical Structure

CAS No. : 306733-22-2

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F81-1144b 相关抗体

Top Publications Citing Use of Products

查看 MMP 亚型特异性产品:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

F81-1144b is a MMP-1 and MMP-3 inhibitor with IC50 values of 5 nM and 29 nM, respectively. F81-1144b reduces serum and hepatic triacylglycerol levels, decreases the secretion of very-low-density lipoprotein-triacylglycerol, inhibits de novo hepatic fatty acid synthesis, and lowers serum insulin and glucose levels. F81-1144b can be used for the research of hypertriglyceridemia[1].

IC50 & Target[1]

MMP-1

5 nM (IC50)

MMP-3

27 nM (IC50)

体内研究
(In Vivo)

F81-1144b (50-100 mg/kg；皮下注射；每日 1 次；连续 7 天) 可呈剂量依赖性降低 HSD 诱导的高甘油三酯血症大鼠的血清及肝脏甘油三酯水平，其中 100 mg/kg 剂量可使血清 TAG、胆固醇、葡萄糖及胰岛素水平恢复正常，并将 VLDL-TAG 分泌抑制 45%[1]。

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

Animal Model: Wistar rats (7-week-old male; high-sucrose diet-induced hypertriglyceridemia)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: s.c.; once daily; 7 days
Result: Reduced serum TAG levels in a dose-dependent manner, with 100 mg/kg restoring levels to normal diet-fed control values.
Reduced serum cholesterol levels in a dose-dependent manner, with 100 mg/kg restoring levels to normal diet-fed control values.
Returned slightly elevated serum glucose levels to normal values at both 50 mg/kg and 100 mg/kg.
Markedly reduced HSD-elevated serum insulin levels.
Significantly reduced hepatic TAG levels in a dose-dependent manner; did not significantly change hepatic phospholipid levels.
Significantly suppressed hepatic de novo fatty acid synthesis at 100 mg/kg.
Significantly decreased HSD-elevated microsomal glycerol-3-phosphate acyltransferase (GPAT) activity at 100 mg/kg.
Upregulated hepatic gene expression of Lpl, Cd36, Apoa1, Ucp2 in a dose-dependent manner.
分子量

483.60

Formula

C27H37N3O5
CAS 号
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

F81-1144b 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

F81-1144b306733-22-2MMPMatrix metalloproteinasesglucosevery low density lipoprotein-triacylglycerolinsulintriacylglycerolcarbohydrate response element-binding proteinMMP-3sterol regulatory element-binding protein-1cMMP-1uncoupling protein 2fatty acid synthesisInhibitorinhibitorinhibit

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产品名称：
F81-1144b
目录号：
HY-125507
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