Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
Cyclic Adenosine monophosphate (cAMP)[5]
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ln Vitro |
Human lung epithelial cells A549 are not affected by spilanthol (50~150 μM, 24h) in terms of viability [3]. Applied at 50~150 μM for 24 hours, spilanthol possesses anti-inflammatory properties on the human lung epithelial cell line A549 [3]. The ICAM-1 gene can be expressed less in the A549 human lung epithelial cell line when spilanthol (50–150 μM) is applied for 24 hours [3].
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ln Vivo |
In the male ICR mouse model, where acetic acid promotes belly twisting and capsaicin causes paw licking, spilanthol (1-1.875 mg/kg, Ip, Once) exerts an analgesic effect[2]. The 5-fluorouracil-induced intestinal mucositis model in Swiss mice shows a protective effect against intestinal damage when Spilanthol (30 mg/kg, orally, once day for 4 days) is administered[4]. Adult male C57BL/6J mice are susceptible to the diuretic effects of spilanthol (800 mg/kg, oral, once)[5].
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Cell Assay |
Cell Viability Assay[3]
Cell Types: A549 human lung epithelial cell line Tested Concentrations: 50μM, 75μM, 100μM, 150 μM Incubation Duration: 24h Experimental Results: There was no significant change in cell viability. Cell Cytotoxicity Assay[3] Cell Types: A549 human lung epithelial cell line Tested Concentrations: 50μM, 75μM, 100μM, 150 μM Incubation Duration: 24h Experimental Results: Dramatically inhibited the release of the inflammatory cytokine TNF-α and the chemokine MCP-1. Western Blot Analysis[3] Cell Types: A549 human lung epithelial cell line Tested Concentrations: 50μM, 75μM, 100μM, 150 μM Incubation Duration: 24h Experimental Results: Inhibited COX-2 expression and increased the expression of HO-1. Cell Viability Assay[3] Cell Types: A549 human lung epithelial cell line Tested Concentrations: 50μM, 75μM, 100μM, 150 μM Incubation Duration: 24h Experimental Results: Dramatically diminished THP-1 cells adhered. |
Animal Protocol |
Animal/Disease Models: Acetic acid-induced abdominal writhes Male ICR mice model[2]
Doses: 1-1.875 mg/kg Route of Administration: intraperitoneal (ip) administration(ip), Once Experimental Results: As the dose increased, the number of abdominal contractions and licking behavior diminished, and a maximum antinociceptive effect of 46.67%. Animal/Disease Models: Swiss mice model of intestinal mucositis induced by 5-fluorouracil[4]. Doses: 30 mg/kg Route of Administration: Oral adminstraion(po), one time/day for four days Experimental Results: demonstrated the Intestinal wall recovery, villi are higher and less irregularity and high number and greater length of intestinal crypts. Animal/Disease Models: Adult C57BL/6J male mice[5]. Doses: 800 mg/Kg Route of Administration: Oral adminstraion (po), Once Experimental Results: Increased in urine output, sodium, and increased excretion of sodium, potassium and chloride. |
References |
[1]. Alan F, et al. Spilanthol: occurrence, extraction, chemistry and biological activities. Elsevier. 2016:128-133
[2]. Déciga-Campos M, et al. Antinociceptive effect of Heliopsis longipes extract and affinin in mice. Planta Med. 2010 May;76(7):665-70. [3]. Huang WC, et al. Spilanthol Inhibits COX-2 and ICAM-1 Expression via Suppression of NF-κB and MAPK Signaling in Interleukin-1β-Stimulated Human Lung Epithelial Cells. Inflammation. 2018 Oct;41(5):1934-1944. [4]. de Freitas-Blanco VS, et al. Spilanthol, the Principal Alkylamide from Acmella oleracea, Attenuates 5-Fluorouracil-Induced Intestinal Mucositis in Mice. Planta Med. 2019 Feb;85(3):203-209. [5]. [5]Gerbino A, et al.. Spilanthol from Acmella Oleracea Lowers the Intracellular Levels of cAMP Impairing NKCC2 Phosphorylation and Water Channel AQP2 Membrane Expression in Mouse Kidney. PLoS One. 2016 May 23;11(5):e0156021. |
Molecular Formula |
C14H23NO
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Molecular Weight |
221.34
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CAS # |
25394-57-4
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SMILES |
C/C=C/C=C/CC/C=C/C(NCC(C)C)=O
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.5179 mL | 22.5897 mL | 45.1794 mL | |
5 mM | 0.9036 mL | 4.5179 mL | 9.0359 mL | |
10 mM | 0.4518 mL | 2.2590 mL | 4.5179 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.