1. Epigenetics PI3K/Akt/mTOR
  2. AMPK
  3. AMPKα1 activator 1

AMPKα1 activator 1 是一种选择性且口服有效的 AMPKα1 激活剂,其 EC50 为 35.1 nM。AMPKα1 activator 1 对 AMPKα2 的选择性高达 176 倍。AMPKα1 activator 1 可用作细胞保护剂和肾脏保护剂。在肾缺血再灌注损伤模型中,AMPKα1 activator 1 能减轻血清肌酐和血尿素氮水平的升高,缓解肾脏损伤,并减少肾组织中的细胞浸润。AMPKα1 activator 1 可用于肾缺血再灌注损伤相关研究。

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AMPKα1 activator 1

AMPKα1 activator 1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMPKα1 activator 1 is a selective and orally active AMPKα1 activator with an EC50 of 35.1 nM. AMPKα1 activator 1 shows 176-fold selectivity over AMPKα2. AMPKα1 activator 1 can be used as a cell protectant and a kidney protectant. AMPKα1 activator 1 attenuates elevation of serum creatinine and blood urea nitrogen levels, alleviates kidney damage, and reduces cellular infiltration in renal ischemia-reperfusion injury contexts. AMPKα1 activator 1 can be associated with renal ischemia-reperfusion injury research[1].

IC50 & Target[1]

AMPK α1β1γ1

35.1 nM (IC50)

AMPK α2β1γ1

6200 nM (IC50)

体外研究
(In Vitro)

AMPKα1 activator 1 (22f) (0.25-0.5 μM;作用 10 h) 可通过激活 AMPKα1,以浓度依赖的方式调控 H/R 损伤的 NRK-52E 细胞中的氧化应激、细胞凋亡、自噬及脂代谢[1]
AMPKα1 activator 1 (22f) (0.25-0.5 μM;作用 10 h) 在 H/R 损伤的 NRK-52E 细胞中选择性激活 AMPKα1 (而非 AMPKα2)[1]

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

Cell Viability Assay[1]

Cell Line: NRK-52E cells (rat renal proximal tubular epithelial cells) subjected to hypoxia-reoxygenation (H/R) injury
Concentration: 0.25-0.5 μM (H/R injury period); 12 μM (Compound C co-treatment)
Incubation Time: 10 h (H/R injury period: 5 h hypoxia + 5 h reoxygenation)
Result: Concentration-dependently restored viability of H/R-injured NRK-52E cells; reduced viability restoration observed when co-treated with 12 μM Dorsomorphin (Compound C) (HY-13418A).

Western Blot Analysis[1]

Cell Line: H/R-injured NRK-52E cells
Concentration: 0.25-0.5 μM (H/R injury period); 12 μM (Compound C co-treatment)
Incubation Time: 10 h (H/R injury period: 5 h hypoxia + 5 h reoxygenation)
Result: Concentration-dependently increased p-AMPK/AMPK and p-ACC/ACC ratios; blunted p-AMPK/AMPK and p-ACC/ACC ratio increases observed when co-treated with 12 μM CDorsomorphin (Compound C) (HY-13418A)
体内研究
(In Vivo)

AMPKα1 activator 1 (compound 22f) (50-100 mg/kg;灌胃;每日给药;持续 4 天) 可通过选择性激活 AMPKα1,呈剂量依赖性地缓解雄性 C57BL/6 小鼠的肾缺血再灌注损伤[1]

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

Animal Model: C57BL/6 (male, 16-18 g) bearing renal ischemia-reperfusion injury[1]
Dosage: 50, 100 mg/kg
Administration: p.o.; daily; 4 days
Result: Dose-dependently attenuated IRI-induced increases in blood urea nitrogen and blood creatinine; significantly attenuated histological kidney damage and immune cell infiltration; dose-dependently up-regulated p-AMPKα1/AMPKα1 in renal tissue; up-regulated CPT1 and LC3B/LC3A protein levels; down-regulated BAX/BCl2 protein levels in renal tissue.
分子量

453.94

Formula

C22H20ClN5O2S

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
  • 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 *
= × ×

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.

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AMPKα1 activator 1
目录号:
HY-181077
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