| Bioactivity | RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity[1][2][3][4]. | |||||||||
| Invitro | 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 EC50 of ∼1 μM in APP-HEK293 cells[4]. Cell Viability Assay[2] Cell Line: | |||||||||
| 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: | |||||||||
| Name | RSVA405 | |||||||||
| CAS | 140405-36-3 | |||||||||
| Formula | C17H20N4O2 | |||||||||
| Molar Mass | 312.37 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Khader A, et, al. Novel resveratrol analogues attenuate renal ischemic injury in rats. J Surg Res. 2015 Feb;193(2):807-15. [2]. Vingtdeux V, et, al. Small-molecule activators of AMP-activated protein kinase (AMPK), RSVA314 and RSVA405, inhibit adipogenesis. Mol Med. Sep-Oct 2011;17(9-10):1022-30. [3]. Capiralla H, et, al. Identification of potent small-molecule inhibitors of STAT3 with anti-inflammatory properties in RAW 264.7 macrophages. FEBS J. 2012 Oct;279(20):3791-9. [4]. Vingtdeux V, et, al. Novel synthetic small-molecule activators of AMPK as enhancers of autophagy and amyloid-β peptide degradation. FASEB J. 2011 Jan;25(1):219-31. |