Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
AMPK 1 μM (EC50, in cell-based assays)
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ln Vitro |
RSVA405 (0.2-2 μM; 24 h) suppresses the development of adipocytes[2]. In 3T3-L1 cells, the production of fatty acid synthase (FAS), PPAR-γ, and fatty acid binding protein 4 (aP2) is strongly inhibited by RSVA405 (0.2-2 μM; 24 h)[2]. In activated RAW 264.7 macrophages, RSVA405 (1-3 μM; 16 h) suppresses LPS-induced STAT3 activity, intracellular signaling, and cytokine response[3]. With an EC50 of approximately 1 μM in APP-HEK293 cells, RSVA405 (1-3 μM; 24 h) suppresses mTOR, induces autophagy, and promotes the lysosomal breakdown of Aβ[4].
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ln Vivo |
In rats undergoing ischemia-reperfusion (I/R), RSVA405 (3 mg/kg; ip) reduces kidney damage and preserves renal function[1]. Mice on a high-fat diet have significantly less body weight gain when given RSVA405 (20–100 mg/kg/d; po for 11 weeks)[2].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: 3T3-L1 preadipocytes Tested Concentrations: 0.2, 0.5, 1, 2 μM Incubation Duration: 24 h Experimental Results: 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. |
Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (300-350 g) are induced I/ R injury[1]
Doses: 3 mg/kg Route of Administration: Ip one hour before inducing I/R injury Experimental Results: diminished the levels of creatinine and blood urea nitrogen (BUN), by 35.8% and 44.3% in serum, respectively. diminished the levels of aspartate aminotransferase (AST) and lactate dehydrogenase (LDH) by 33.0% and 59.8% in serum, respectively. |
References |
[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. |
Molecular Formula |
C17H20N4O2
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Molecular Weight |
312.37
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CAS # |
140405-36-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CCN(C1C=C/C(=C\NNC(C2=CC=NC=C2)=O)/C(=O)C=1)CC
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 125 mg/mL (400.17 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.