| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
Artepillin C targets CREB/CRTC2-mediated gene transcription and TRPA1 channels. It downregulates BMALL expression to regulate glucose and lipid metabolism. It also activates TRPA1 channels to induce spicy taste signals. Additionally, it may have activities related to necroptosis and epigenetic reader domains.
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| ln Vitro |
Artepillin C inhibits tumor cell proliferation and induces apoptosis. It improves insulin resistance and inhibits liver lipid synthesis. It has been used in studies of metabolic syndrome, tumor prevention and treatment, and inflammation. It also demonstrates activity against Candida albicans, Epidermophyton floccosum, and Trichophyton rubrum.
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| ln Vivo |
In db/db obese mice, Artepillin C (20 mg/kg; intraperitoneal injection; once daily for 1-3 weeks) significantly improves glucose homeostasis, reduces fasting blood glucose and insulin resistance, inhibits hepatic BMALL expression and lipid synthesis-related genes, and reduces hepatic lipid accumulation.
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| Enzyme Assay |
TRPA1 agonism is typically assessed using calcium imaging assays in TRPA1-expressing cells. CREB/CRTC2 inhibition is evaluated using luciferase reporter gene assays to measure transcriptional activity. Binding affinity can be determined using surface plasmon resonance or isothermal titration calorimetry.
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| Cell Assay |
Cytotoxicity assays against tumor cell lines (e.g., HEP-2 cells) are performed using MTT or SRB assays. Cells are treated with Artepillin C at various concentrations for defined periods to determine IC50 values. Endothelial cell proliferation assays evaluate anti-angiogenic effects.
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| Animal Protocol |
In vivo studies in db/db obese mice involve intraperitoneal injection of Artepillin C at 20 mg/kg once daily for 1-3 weeks. Blood glucose, insulin resistance, and lipid synthesis markers are measured. Hepatic BMALL expression is assessed by Western blot or qPCR.
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| ADME/Pharmacokinetics |
Artepillin C is orally active. In vivo administration at 20 mg/kg (i.p.) shows significant metabolic effects. Solubility and bioavailability data are not extensively reported. Storage conditions follow standard recommendations.
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| Toxicity/Toxicokinetics |
Toxicological data are limited to in vitro cytotoxicity assessments. As a natural product from propolis, it is generally considered safe at research doses, but comprehensive toxicology studies are lacking. It inhibits tumor cell proliferation, suggesting potential therapeutic applications.
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| References |
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| Additional Infomation |
Atepspirin C has been reported to have been found in Artemisia scoparia, Sophora flavescens, and other organisms with available data.
Artepillin C is a research-use-only compound. It has been extensively studied for its metabolic syndrome-ameliorating effects. It is one of the primary constituents of Brazilian green propolis responsible for neuroprotective effects against oxytosis/ferroptosis. |
| Molecular Formula |
C19H24O3
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|---|---|
| Molecular Weight |
300.39206
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| Exact Mass |
300.173
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| CAS # |
72944-19-5
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| PubChem CID |
5472440
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.092g/cm3
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| Boiling Point |
447.672ºC at 760 mmHg
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| Flash Point |
238.674ºC
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| Index of Refraction |
1.586
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| LogP |
4.507
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
421
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=CCC1=CC(=CC(=C1O)CC=C(C)C)C=CC(=O)O)C
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| InChi Key |
KABCFARPAMSXCC-JXMROGBWSA-N
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| InChi Code |
InChI=1S/C19H24O3/c1-13(2)5-8-16-11-15(7-10-18(20)21)12-17(19(16)22)9-6-14(3)4/h5-7,10-12,22H,8-9H2,1-4H3,(H,20,21)/b10-7+
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| Chemical Name |
(E)-3-[4-hydroxy-3,5-bis(3-methylbut-2-enyl)phenyl]prop-2-enoic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.3290 mL | 16.6450 mL | 33.2901 mL | |
| 5 mM | 0.6658 mL | 3.3290 mL | 6.6580 mL | |
| 10 mM | 0.3329 mL | 1.6645 mL | 3.3290 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.
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