2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs HMG-CoA Reductase (HMGCR)
  4. PROTAC HMGCR Degrader-1

PROTAC HMGCR Degrader-1 是一种口服活性的 HMGCR PROTAC 降解剂其 IC50 为 1.32 μM，也是一种由 PROTAC HMGCR Degrader-2 (HY-181134) 衍生而来的内酯前药。PROTAC HMGCR Degrader-1 在体内可实现活性成分的高血浆暴露，导致强效的 HMGCR 降解，并显示出良好的降胆固醇功效。PROTAC HMGCR Degrader-1 可用于高血脂症的相关研究。

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PROTAC HMGCR Degrader-1

PROTAC HMGCR Degrader-1 Chemical Structure

CAS No. : 2715104-45-1

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PROTAC HMGCR Degrader-1 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134). PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research[1].

体外研究
(In Vitro)

PROTAC HMGCR Degrader-1 (compound 21 b) 是一种口服活性前药，衍生自 PROTAC HMGCR Degrader-2 (HY-181134) (compound 21 c)。PROTAC HMGCR Degrader-2 是一种 HMGCR PROTAC 降解剂，在 Insig 基因沉默的 HepG2 细胞中通过 VHL 依赖性方式降解 HMGCR，其 DC50 为120 nM [1]。
PROTAC HMGCR Degrader-1 (0.01-3 μM，处理 16 小时) 在 HepG2 细胞中，高剂量下更倾向于发挥 HMGCR 抑制剂而非降解剂的作用，在 1 μM的高剂量下最大降解率 (Dmax) 为56%[1]。
PROTAC HMGCR Degrader-1 (1 μM，处理 16 小时) 在人工肝 HepG2 细胞中能阻止 HMGCR 的代偿性上调[1]。

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

PROTAC HMGCR Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.01. 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time: 16 h
Result: Attenuated the upregulation of HMGCR at low concentration.
Increase in HMGCR expression at high concentration.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1 μM
Incubation Time: 16 h
Result: Effectively attenuated the compensatory upregulation of HMGCR.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-24 AUC0-∞
Mice[1] 60 mg/kg p.o. 5.1 h 8.0 h 0.47 μM 5.0 μM 5.4 μM
体内研究
(In Vivo)

PROTAC HMGCR Degrader-1 (compound 21 b) (20 或 60 mg/kg，口服，每日一次，持续 5 周) 在中等脂肪饮食 (MFD) 诱导的小鼠模型中，低剂量下可通过降解 HMGCR 抑制胆固醇的从头合成，且在与协同lovastatin (HY-N0504) 联用时，对促进每日从 MFD27 饮食中吸收的多余脂质排泄具有更好的效果，并表现出良好的安全性[1]。

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

Animal Model: MFD (medium-fat containing 12% fat, 0.5% so dium cholate and 1.25% cholesterol) (8 weeks) induced-male C57BL/6 mice (20e24 g)[1]
Dosage: 20 or 60 mg/kg
Administration: p.o., once a day for 5 weeks
Result: Was well tolerated, with no significant change in body weight and food intake.
Demonstrated similar effects to lovastatin.
Decreased total cholesterol (TC), LDL-C and triglyceride (TG) in serum of mice fed on MFD.
Enhanced the reduction in serum lipid levels when combination with lovastatin.
Reduced serum TC and cholesteryl esters to lower levels at a higher dose of 60 mg/kg.
Reduced hepatic TC and TG in a dose-dependent manner.
Ameliorated MFD-induced steatosis and lipid deposition in liver sections.
Induced robust HMGCR degradation at 16 h after final gavage even at a low dose of 20 mg/kg.
Was more effective in lowering total lipids (TC, cholesteryl ester and TG) when cotreated with lovastatin.
分子量

960.27

Formula

C53H77N5O9S
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

PROTAC HMGCR Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

PROTAC HMGCR Degrader-12715104-45-1PROTAC HMGCR Degrader1PROTAC HMGCR Degrader 1PROTACsHMG-CoA Reductase (HMGCR)orally activeHMGCRPROTACVHL-dependent mannerhyperlipidemiaInhibitorinhibitorinhibit

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