RSVA405 是一种有效和具有口服活性的AMPK激活剂，EC50值为 1 μM。RSVA405 通过促进 CaMKKβ 依赖的 AMPK 活化，从而抑制mTOR，并促进自噬 (autophagy) 以增加 Aβ 的降解。RSVA405 通过抑制STAT3功能具有抗炎作用。RSVA405 也可用于肥胖症的研究。
| 生物活性 | RSVA405 is a potent, orally active activator ofAMPK, with anEC50of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation ofAMPK, inhibitsmTOR, and promotesautophagyto increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition ofSTAT3function. RSVA405 can also be used for the research of obesity[1][2][3][4]. |
| IC50& Target[2] | AMPK 1 μM (EC50, in cell-based assays) |
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体外研究
(In Vitro) | RSVA405 (0.2-2 μM; 24 h) inhibits adipocyte differentiation[2].
RSVA405 (0.2-2 μM; 24 h) significantly inhibits the expression of peroxisome proliferator-activated receptor (PPAR)-γ, fatty acid synthase (FAS) and fatty acid binding protein 4 (aP2) in 3T3-L1 cells[2].
RSVA405 (1-3 μM; 16 h) inhibits LPS-induced STAT3 activity, intracellular signaling, and cytokine response in activated RAW 264.7 macrophages[3].
RSVA405 (1-3 μM; 24 h) inhibits mTOR, induces autophagy, and facilitates the lysosomal degradation of Aβ, with an EC50of ~1 μM in APP-HEK293 cells[4].
Cell Viability Assay[2] | Cell Line: | 3T3-L1 preadipocytes | | Concentration: | 0.2, 0.5, 1, 2 μM | | Incubation Time: | 24 h | | Result: | Increased the phosphorylation of AMPK and its substrate acetyl-CoA carboxylase (ACC).
Inhibited the accumulation of lipid droplets in a dose-dependent manner, with an IC50of 0.5 μM. |
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体内研究
(In Vivo) | RSVA405 (3 mg/kg; i.p.) attenuates renal injury and protects renal function after ischemia-reperfusion (I/R) in rats[1].
RSVA405 (20-100 mg/kg/d; p.o. for 11 weeks) significantly reduces the body weight gain of mice fed a high-fat diet[2].
| Animal Model: | Male Sprague-Dawley rats (300-350 g) are induced I/R injury[1] | | Dosage: | 3 mg/kg | | Administration: | I.p. one hour before inducing I/R injury | | Result: | Decreased the levels of creatinine and blood urea nitrogen (BUN), by 35.8% and 44.3% in serum, respectively.
Decreased the levels of aspartate aminotransferase (AST) and lactate dehydrogenase (LDH) by 33.0% and 59.8% in serum, respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(400.17 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2013 mL | 16.0067 mL | 32.0133 mL | | 5 mM | 0.6403 mL | 3.2013 mL | 6.4027 mL | | 10 mM | 0.3201 mL | 1.6007 mL | 3.2013 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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