| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Free fatty acid receptor 4 (FFAR4/GPR120) as a selective partial agonist; also acts as a dual antagonist of voltage-gated sodium NaV1.7 and calcium CaV2.2 channels; natural carbonic anhydrase II (CAII) inhibitor.
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| ln Vitro |
The viability of RAW264.7 cells is reduced in a dose- and time-dependent manner by ggrifolic acid treatment (2.5–20 µM)[1].
Grifolic acid induces ERK activation and intracellular calcium ([Ca2+]i) responses in STC-1 cells that express GPR120 endogenously, but not those expressing GPR40. It is a selective partial agonist of GPR120. Grifolic acid (2.5-20 µM) treatment reduces RAW264.7 cell viability in a dose- and time-dependent manner. Grifolic acid shows inhibitory activity against carbonic anhydrase II with an IC50 of 6.37 μM. Grifolic acid has antibacterial activity, inhibiting the growth of Staphylococcus aureus and Staphylococcus epidermidis. Grifolic acid (30 μM) increases GLP-1 secretion in STC-1 cells via GPR120/Ca2+ signaling. The compound modulates the expression of cell surface receptors including Toll-like receptors and adhesion molecules. |
| ln Vivo |
In vivo, Grifolic acid has potent antinociceptive (pain-relieving) effects as a dual antagonist of voltage-gated sodium NaV1.7 and calcium CaV2.2 channels. It affects the expression of cell surface receptors including Toll-like receptors and adhesion molecules, suggesting immunomodulatory activity. As a GPR120 agonist, grifolic acid would be expected to show effects on metabolism, inflammation, and pain in animal models. Specific animal model data and detailed dosing regimens are available in the primary literature but not extensively detailed in public search results.
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| Enzyme Assay |
GPR120 agonist activity is assessed using in vitro cell-based assays measuring ERK phosphorylation and intracellular calcium mobilization. STC-1 cells (mouse enteroendocrine cells that express GPR120 endogenously) or cells transfected with GPR120 or GPR40 are treated with Grifolic acid at various concentrations (typically 0.1-100 μM). ERK phosphorylation is assessed by Western blot using phospho-specific antibodies (pERK1/2) and total ERK1/2 as loading control. Intracellular calcium levels are measured using fluorescent calcium indicators (e.g., Fluo-4 AM) in plate-reader-based or imaging assays. NaV1.7 and CaV2.2 channel inhibition is assessed using patch-clamp electrophysiology in cells expressing recombinant channels. Carbonic anhydrase II inhibition is assessed using in vitro enzyme assays measuring the esterase activity of CAII with p-nitrophenyl acetate as substrate. Antibacterial activity is assessed by measuring inhibition of bacterial growth in culture.
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| Cell Assay |
Cellular activity is evaluated in RAW264.7 macrophages, STC-1 enteroendocrine cells, and other relevant cell types. Cells are treated with Grifolic acid at various concentrations (typically 2.5-20 μM for RAW264.7, 30 μM for STC-1 cells) for appropriate time periods. Cell viability is measured by MTT or CellTiter-Glo assays. ERK phosphorylation is assessed by Western blot. Intracellular calcium is measured using fluorescent indicators. GLP-1 secretion is measured by ELISA from cell culture supernatants. Inflammatory mediator expression (cytokines, chemokines) is measured by ELISA or qRT-PCR. Toll-like receptor and adhesion molecule expression is assessed by flow cytometry or Western blot.
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| Animal Protocol |
In vivo efficacy is studied in animal models of pain and inflammation. Grifolic acid is administered via various routes (oral, intraperitoneal, subcutaneous) at doses determined from preliminary pharmacokinetic and tolerability studies. Antinociceptive effects are assessed using pain behavior tests including hot plate, tail flick, von Frey filaments, and formalin-induced paw licking. Inflammatory markers (cytokine levels, immune cell infiltration) are measured in serum or tissue by ELISA or multiplex assays. Metabolic parameters (glucose, insulin, lipids) may be measured in models of metabolic disease. Specific protocols are detailed in the primary literature.
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| ADME/Pharmacokinetics |
Grifolic acid has a molecular formula of C24H32O4 and a molecular weight of 384.51 g/mol. CAS Number: 80557-12-6. Purity: typically ≥98% by HPLC. It is a natural product from the Albatrellus confluens mushroom. The compound is soluble in DMSO and should be stored at -20°C for long-term stability, protected from light and moisture. Grifolic acid is a selective partial FFA4 (GPR120) agonist. Detailed pharmacokinetic parameters including half-life, oral bioavailability, volume of distribution, and plasma protein binding are not extensively characterized in publicly available literature.
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| Toxicity/Toxicokinetics |
Safety data for Grifolic Acid indicate it is a research compound for laboratory use only. As a natural product with multiple biological activities (GPR120 agonist, NaV1.7/CaV2.2 antagonist, CAII inhibitor, antibacterial), it should be handled with appropriate safety precautions. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval. Standard laboratory safety practices should be followed, including the use of personal protective equipment (gloves, lab coat, safety goggles) and adequate ventilation. Avoid inhalation, ingestion, and skin contact. Consult the material safety data sheet (MSDS) for detailed safety information, including potential hazards and disposal considerations.
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| References | |
| Additional Infomation |
It has been reported that gracilaria folic acid has been found in Albatrellus dispansus, Peperomia galioides, and other organisms with available data.
Grifolic Acid is a research tool compound for studying GPR120 biology, pain pathways, inflammation, and metabolism. It is not approved for clinical use. The compound is a natural product from the Albatrellus confluens mushroom with diverse pharmacological activities including GPR120 agonism, NaV1.7/CaV2.2 antagonism, CAII inhibition, and antibacterial activity. Grifolic acid has been investigated for its potential in metabolic diseases (via GLP-1 secretion), pain management (via NaV1.7/CaV2.2 antagonism), and inflammation (via modulation of inflammatory mediators). The compound's unique combination of activities makes it a valuable tool for understanding the complex interplay between metabolic, inflammatory, and pain signaling pathways. Grifolic acid methyl ether also increases GLP-1 secretion via GPR120/Ca2+ signaling. |
| Molecular Formula |
C23H32O4
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|---|---|
| Molecular Weight |
372.51
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| Exact Mass |
372.23
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| CAS # |
80557-12-6
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| Related CAS # |
80557-12-6 Ilicicolinic Acid B Grifolic acid
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| PubChem CID |
9976563
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
557.1±50.0 °C at 760 mmHg
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| Flash Point |
304.8±26.6 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.563
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| LogP |
8.22
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
27
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| Complexity |
569
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C(=C1C(=O)O)O)C/C=C(\C)/CC/C=C(\C)/CCC=C(C)C)O
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| InChi Key |
QPIZDZGIXDKCRC-JTCWOHKRSA-N
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| InChi Code |
InChI=1S/C23H32O4/c1-15(2)8-6-9-16(3)10-7-11-17(4)12-13-19-20(24)14-18(5)21(22(19)25)23(26)27/h8,10,12,14,24-25H,6-7,9,11,13H2,1-5H3,(H,26,27)/b16-10+,17-12+
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| Chemical Name |
2,4-dihydroxy-6-methyl-3-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]benzoic acid
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| Synonyms |
Related CAS# 80557-12-6; Ilicicolinic Acid B; Grifolic 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 2.6845 mL | 13.4225 mL | 26.8449 mL | |
| 5 mM | 0.5369 mL | 2.6845 mL | 5.3690 mL | |
| 10 mM | 0.2684 mL | 1.3422 mL | 2.6845 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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