| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Amiloxate has no direct biological target in the context of pharmacology. Its function is physical and chemical: absorbing incident ultraviolet (UV) radiation. It acts as a sun-screening agent by absorbing high-energy UVB photons and dissipating the energy as lower-energy, harmless heat, preventing it from reaching and damaging DNA in the skin. It is not intended to modulate any specific enzyme or receptor.
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| ln Vitro |
Amiloxate (isoamyl p-methoxycinnamate, 10% w/w) inhibits edema (83%) to have anti-inflammatory effects [1].
In vitro, Amiloxate is evaluated for its ability to absorb UV radiation. UV absorption spectroscopy is used to measure its absorbance spectrum. An aqueous or ethanol solution of the compound is scanned in a UV-Vis spectrophotometer from 250 to 400 nm. Its peak absorbance at 310 nm confirms its effectiveness as a UVB filter. Additionally, in vitro photostability tests are performed by irradiating the solution with a solar simulator and measuring the decrease in absorbance over time. |
| ln Vivo |
Amiloxate is not typically studied for systemic in vivo activity as a drug. However, its in vivo efficacy as a sunscreen is determined by the Sun Protection Factor (SPF) measured on human volunteers. A standard protocol involves applying 2 mg/cm2 of the sunscreen formulation to a small area of a volunteer's back. The skin is then exposed to a solar simulator with increasing UV doses. The SPF is calculated as the ratio of the UV dose required to induce minimal erythema (sunburn) on protected skin to the dose required on unprotected skin.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Amiloxate is not used as a ligand. Instead, its efficacy is measured via UV absorption spectroscopy. A standard protocol involves preparing a 10 microg/mL solution of Amiloxate in ethanol or isopropanol. A background scan is taken with the solvent alone. The solution is then scanned in a UV-Vis spectrophotometer from 250 nm to 400 nm. The absorbance maximum is recorded (typically near 310 nm). The area under the absorption curve (280-320 nm) is integrated to calculate UVB protection potential.
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| Cell Assay |
Amiloxate is not typically used in in vitro cell culture assays as a drug. However, its safety is assessed using standard in vitro toxicology assays. For example, a 3D reconstructed human epidermis model (e.g., EpiDerm) can be used. The test compound is applied topically to the tissue. After exposure, cell viability is measured using an MTT assay. Additionally, its potential to cause phototoxicity is assessed by exposing the treated tissue to UVA/UVB light and comparing viability to non-irradiated controls.
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| Animal Protocol |
Amiloxate is not used in animal experiments as a therapeutic drug. Historically, SPF testing was performed on animals (e.g., guinea pigs), but ethical regulations have largely replaced this with human volunteer testing. Standard safety testing of the final sunscreen product would involve a repeat-dose dermal toxicity study in rats. The test material (sunscreen containing Amiloxate) is applied dermally to shaved rat skin daily for 28 or 90 days. Animals are observed for clinical signs of toxicity, and clinical chemistry, hematology, and histopathology are performed.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Based on in vitro studies of amiloride-containing tape on pig ears, no transdermal penetration of amiloride was detected. No pharmacokinetic data. No pharmacokinetic data. No pharmacokinetic data. No pharmacokinetic data. No pharmacokinetic data. No pharmacokinetic data. No pharmacokinetic data. No pharmacokinetic data. As a topically applied chemical, the pharmacokinetics of Amiloxate are primarily dermal, not systemic. The compound is oil-soluble and has a molecular weight of approximately 248.32 g/mol (C15H20O3). It is designed to remain on the skin surface and within the stratum corneum. While some systemic absorption can occur, it is minimal (<0.5% of applied dose in animal studies). Absorbed material is metabolized by esterases in the skin and liver to its constituent parts (isoamyl alcohol and methoxycinnamic acid) and excreted in urine. |
| Toxicity/Toxicokinetics |
Protein Binding
No pharmacokinetic data available. Amiloxate is recognized as a safe and effective UV filter in cosmetic products. It has been approved by the European Medicines Agency (EMA) for use in over-the-counter sunscreens at concentrations up to 10%. It has low acute and subchronic toxicity following dermal exposure. It is not a significant skin irritant or sensitizer in standard tests. However, like many UV filters, it has been reported to cause photoallergic contact dermatitis in rare cases. It is not classified as a carcinogen or reproductive toxicant. |
| References |
[1]. Céline Couteau, et al. UV Filters, Ingredients with a Recognized Anti-Inflammatory Effect. PLoS One. 2012; 7(12): e46187.
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| Additional Infomation |
Amiloxate is a cinnamic acid ester. Amiloxate is an EMA-approved chemical UV filter commonly found in over-the-counter sunscreens at concentrations up to 10% (molar concentration). It is often referred to as isoamyl 4-methoxycinnamate or isoamyl p-methoxycinnamate. Amiloxate is a cinnamic acid derivative with anti-inflammatory activity. Pharmacological Indications: Used as an active sunscreen agent. Mechanism of Action: Amiloxate is a UVB filter that selectively absorbs UVB rays. It is presumed that Amiloxate exerts its antioxidant effect by scavenging free radicals. Pharmacodynamics: In mouse studies, Amiloxate exhibited dose-dependent anti-inflammatory effects, inhibiting approximately 70% of edema even at low doses. Due to structural similarity, tranexamic acid may also possess the antioxidant and antibacterial properties of cinnamic acid.
Amiloxate is a commonly used cosmetic ingredient and is not a pharmaceutical drug. Its primary application is as a UVB filter in sunscreens and other personal care products (lip balms, moisturizers) to prevent sunburn and reduce the risk of skin cancer and photoaging. It is often combined with UVA filters (e.g., avobenzone, zinc oxide) to provide broad-spectrum protection. The compound is EMA-approved, but its use varies globally; for example, it is not currently approved by the US FDA for use in sunscreens in the United States. |
| Molecular Formula |
C15H20O3
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|---|---|
| Molecular Weight |
248.3175
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| Exact Mass |
248.141
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| CAS # |
71617-10-2
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| PubChem CID |
1549789
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
362.8±17.0 °C at 760 mmHg
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| Melting Point |
< -30
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| Flash Point |
151.6±15.5 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.524
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| LogP |
4.06
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
18
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| Complexity |
263
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(C([H])=C([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H])=O)C([H])([H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H]
|
| InChi Key |
UBNYRXMKIIGMKK-RMKNXTFCSA-N
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| InChi Code |
InChI=1S/C15H20O3/c1-12(2)10-11-18-15(16)9-6-13-4-7-14(17-3)8-5-13/h4-9,12H,10-11H2,1-3H3/b9-6+
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| Chemical Name |
3-methylbutyl (E)-3-(4-methoxyphenyl)prop-2-enoate
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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 | 4.0271 mL | 20.1353 mL | 40.2706 mL | |
| 5 mM | 0.8054 mL | 4.0271 mL | 8.0541 mL | |
| 10 mM | 0.4027 mL | 2.0135 mL | 4.0271 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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