| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Gefarnate targets gastric mucin secretion pathways. As an anti-ulcer drug, it stimulates gastric mucin secretion, enhancing the protective mucus layer of the gastric mucosa. In conjunctival tissue, gefarnate increases secretion of mucin-like glycoprotein. This mechanism underlies its therapeutic effects in gastric ulcers and dry eye syndrome. The compound's specific molecular targets have not been fully elucidated, but its effects on mucin secretion are well characterized.
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| ln Vitro |
Mucin-like glycoprotein secretion was dose-dependently increased by gefarnate (0.001, 0.01, or 0.1 mg/mL); however, the concentration at which the difference from the control was significant was only attained at that level. Mucin-like glycoproteins are selectively stimulated to secrete by gefarnate [1].
Gefarnate (0.001, 0.01, or 0.1 mg/mL) increases mucin-like glycoprotein secretion in a dose-dependent fashion in conjunctival tissue, with significant difference from control only at 0.1 mg/mL. The compound's ability to stimulate mucin secretion has been demonstrated in tissue culture models. Its effects on gastric mucin secretion have been characterized in biochemical assays. These in vitro activities support its therapeutic applications. |
| ln Vivo |
Gefarnate stimulates mucin-like glycoprotein secretion in conjunctival tissue in a dose-dependent manner in the rabbit dry-eye model. The compound is used for the treatment of gastric ulcers and gastritis. It has been proposed for use in the treatment of dry eye syndrome. Its in vivo efficacy has been demonstrated in animal models and clinical studies.
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| Enzyme Assay |
In vitro biochemical assays for gefarnate involve measuring its effects on mucin secretion using tissue or cell culture models. Conjunctival or gastric tissues are treated with varying concentrations of gefarnate, and mucin-like glycoprotein secretion is quantified using ELISA or biochemical assays. The compound's effects on mucus production can also be assessed using histochemical staining. These assays provide mechanistic insights into the compound's therapeutic activity.
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| Cell Assay |
In vitro cell-based assays for gefarnate involve treating mucosal cells or tissue explants with the compound to assess its effects on mucin secretion and cell viability. Conjunctival epithelial cells or gastric epithelial cells are treated with gefarnate at various concentrations. Mucin secretion is measured by ELISA or other quantitative methods. Cell viability is assessed using standard assays. The compound's effects on cell proliferation and differentiation may also be evaluated. These cellular studies characterize the compound's mechanism of action.
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| Animal Protocol |
In vivo animal experiments for gefarnate have been conducted in the rabbit dry-eye model. Rabbits with induced dry eye are treated with gefarnate, and mucin-like glycoprotein secretion in conjunctival tissue is measured. Gastric ulcer models in rodents are used to assess the compound's anti-ulcer efficacy. Efficacy endpoints include mucin secretion measurement, ulcer healing, and histopathological analysis. These studies support the compound's therapeutic applications.
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| ADME/Pharmacokinetics |
Gefarnate has a molecular weight of 400.637 and is a synthetic compound. It is also known as geranyl farnesylacetate. The compound is typically administered orally for gastric ulcers and topically or orally for dry eye syndrome. Its lipophilic nature is characteristic of terpenoid compounds. Specific pharmacokinetic data such as absorption, distribution, metabolism, and elimination are not extensively reported. The compound is typically stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Specific toxicity data for gefarnate is not extensively reported. As an anti-ulcer drug with clinical use, its safety profile has been established. The compound is generally well-tolerated at therapeutic doses. Common adverse effects are mild and gastrointestinal in nature. Preclinical toxicology studies have been conducted to establish the safety profile.
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| References | |
| Additional Infomation |
Gifanate is an organic molecular entity. Gifanate has been studied for the treatment and prevention of gastric ulcers, duodenal ulcers, and cardiovascular diseases. It is a water-insoluble terpene fatty acid used to treat gastrointestinal ulcers; it promotes the healing and function of mucosal tissues.
Gefarnate is a synthetic compound used for the treatment of gastric ulcers and gastritis. It stimulates gastric mucin secretion and increases mucin-like glycoprotein secretion in conjunctival tissue. The compound has been proposed for use in the treatment of dry eye syndrome. Gefarnate is structurally similar to teprenone. It is also known as geranyl farnesylacetate. |
| Molecular Formula |
C27H44O2
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|---|---|
| Molecular Weight |
400.64
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| Exact Mass |
400.334
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| CAS # |
51-77-4
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| PubChem CID |
5282182
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| Appearance |
Colorless to light yellow liquid
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| Density |
0.9±0.1 g/cm3
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| Boiling Point |
484.7±34.0 °C at 760 mmHg
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| Melting Point |
25°C
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| Flash Point |
93.3±24.0 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.489
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| LogP |
10.53
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
29
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| Complexity |
619
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C/C(C)=C\CC/C(C)=C/CC/C(C)=C/CCC(OC/C=C(C)/CC/C=C(C)/C)=O
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| InChi Key |
ZPACYDRSPFRDHO-ROBAGEODSA-N
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| InChi Code |
InChI=1S/C27H44O2/c1-22(2)12-8-14-24(5)16-10-17-25(6)18-11-19-27(28)29-21-20-26(7)15-9-13-23(3)4/h12-13,16,18,20H,8-11,14-15,17,19,21H2,1-7H3/b24-16+,25-18+,26-20+
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| Chemical Name |
[(2E)-3,7-dimethylocta-2,6-dienyl] (4E,8E)-5,9,13-trimethyltetradeca-4,8,12-trienoate
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| Synonyms |
Gefarnil; Geranyl farnesylacetate; Gefarnate
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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 : ~31.25 mg/mL (~78.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (5.19 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4960 mL | 12.4800 mL | 24.9601 mL | |
| 5 mM | 0.4992 mL | 2.4960 mL | 4.9920 mL | |
| 10 mM | 0.2496 mL | 1.2480 mL | 2.4960 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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