RSVA405
目录号 : KM4914 CAS No. : 140405-36-3 纯度 : 98%

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。

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5mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

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 also can be used for the research of obesity.

体外研究

RSVA405 (0.2-2 μM; 24 h) inhibits adipocyte differentiation.
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.
RSVA405 (1-3 μM; 16 h) inhibits LPS-induced STAT3 activity, intracellular signaling, and cytokine response in activated RAW 264.7 macrophages.
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.

Cell Viability Assay

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 IC50 of 0.5 μM.
体内研究

RSVA405 (3 mg/kg; i.p.) attenuates renal injury and protects renal function after ischemia-reperfusion (I/R) in rats.
RSVA405 (20-100 mg/kg/d; p.o. for 11 weeks) significantly reduces the body weight gain of mice fed a high-fat diet.

Animal Model: Male Sprague-Dawley rats (300-350 g) are induced I/R injury
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.
分子式
C17H20N4O2
分子量
312.37
CAS号
140405-36-3
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
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (400.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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