| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Source | Plant — Compositae Artemisia capillaris Thunb. |
| Molecular weight | |
| Molecular formula | C19H24O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Artepillin C is an orally active inhibitor of CREB/CRTC2 and a covalent agonist of TRPA1 (EC50 = 1.8 μM). It inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism, and it can activate TRPA1 channels to induce spicy taste signals. It can also inhibit tumor cell proliferation, induce necroptosis, improve insulin resistance and inhibit liver lipid synthesis, and it can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation[1][2][3][4]. It is supplied as a light yellow to yellow solid (C19H24O3, MW 300.39) at 99.07% purity.
Physical & Chemical Properties
| CAS Number | 72944-19-5 |
|---|---|
| Molecular Formula | C19H24O3 |
| Molecular Weight | 300.39 g/mol |
| Purity | 99.07% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| Structure Classification | Ketones, Aldehydes, Acids |
| SMILES | C/C(C)=C\CC1=C(C(C/C=C(C)\C)=CC(/C=C/C(O)=O)=C1)O |
| Target | CREB/CRTC2, TRPA1 |
| Signaling Pathway | Epigenetics; Apoptosis; Neuronal Signaling; Membrane Transporter/Ion Channel |
| Initial Source | Plant — Compositae Artemisia capillaris Thunb. |
| Solubility | In Vitro: DMSO: 100 mg/mL (332.90 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[3]
|
TRPA1 1.8 μM () |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (332.90 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (8.32 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (8.32 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Artepillin C (1 μM-1 mM; 12-48 h) decreases HEp-2 tumor cell viability concentration- and time-dependently, giving CC50 values of 4.07 μM-0.9 μM[1]. Artepillin C (1-0.5 μM; 24 h) causes necrosis of HEp-2 cells and significantly raises cell membrane permeability[1]. Artepillin C (1 μM; 30 min; pH 3.2) increases the membrane permeability of DPPS-containing macropinosomes (GUVs) and significantly speeds up the efflux of fluorescent probes[1]. Artepillin C (3.13-50 μg/mL; 36 h) blocks HUVEC cell tube formation concentration-dependently, with complete inhibition at 50 μg/mL[2]. Artepillin C (3.13-50 μg/mL; 3 d) suppresses HUVEC cell proliferation, with an IC50 of approximately 37.2 μg/mL[2].
Apoptosis Analysis[1]
| Cell Line | HEp-2 cells |
|---|---|
| Concentration | 0.01 mM, 0.05 mM, 0.1 mM, 0.5 mM |
| Incubation Time | 24 h |
| Result | Increased propidium iodide (PI)-positive cells, indicating membrane permeabilization and necrosis. Morphological changes included cell swelling and granular nuclei, characteristic of necrotic cell death, without significant apoptosis induction. |
In Vivo
In the mouse dorsal air sac tumor model, Artepillin C (0.125%-0.5% diet; po; once a day; 6 days) suppresses tumor-induced angiogenesis and lowers the number of blood vessels in a dose-dependent manner[2]. In db/db obese mice, Artepillin C (20 mg/kg; intraperitoneal injection; once a day; 1-3 weeks) leads to significant improvement of glucose homeostasis, lowers fasting blood glucose and insulin resistance, suppresses hepatic BMAL1 expression and lipid synthesis-related genes, and decreases hepatic lipid accumulation[4]. In DIO mice fed a high-fat diet, Artepillin C (20 mg/kg; intraperitoneal injection; once a day; 3 weeks) enhances insulin sensitivity, lowers hepatic gluconeogenesis and lipid synthesis, and regulates expression of the circadian rhythm-related gene Bmal1[4].
| Animal Model | ICR mice (female, 30±5 g, 7-week-old), dorsal air sac (DAS) tumor angiogenesis model[2] |
|---|---|
| Dosage | 0.125%, 0.25%, 0.5% (w/w in diet) |
| Administration | Oral administration via diet, once daily, 6 days starting from chamber implantation |
| Result | Significantly reduced tumor-induced angiogenesis in a dose-dependent manner. No signs of toxicity were observed, with stable body weight throughout the treatment period. Histological analysis confirmed reduced vascular density in the treated groups, indicating anti-angiogenic activity without systemic toxicity. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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