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| Targets |
The primary target of Cetyl tranexamate hydrochloride is plasminogen. It functions as a plasminogen activation inhibitor, blocking the conversion of plasminogen to plasmin. By inhibiting plasmin activity, it reduces the production of inflammatory mediators like prostaglandins and platelet-activating factor, which in turn decreases vascular dilation and subsequent pigmentation. This mechanism of action interferes with the melanogenesis pathway in melanocytes, reducing the formation of hyperpigmented lesions. It also acts on hemoglobin to reduce erythema. As a derivative of the serine protease inhibitor tranexamic acid, its activity is likely mediated through interactions with serine protease domains in the fibrinolytic system.
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| Enzyme Assay |
Cetyl tranexamate hydrochloride is not typically evaluated in classical enzyme inhibition assays as a drug candidate. Its in vitro activity is assessed by its ability to inhibit UV-induced plasminogen activation in cultured human keratinocytes. The compound reduces the generation of plasminogen, which is necessary for melanocyte activation and pigmentation. It also suppresses the production of inflammatory mediators like prostaglandins and platelet-activating factor in these cell-based models, confirming its dual mechanism against both melanin and hemoglobin-driven dyschromia. Such assays typically use primary human keratinocytes or melanocyte-keratinocyte co-cultures exposed to UVB radiation and treated with varying concentrations of the compound.
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| Cell Assay |
In vitro efficacy is demonstrated in cell culture models designed to mimic hyperpigmentation. Human keratinocytes and/or melanocytes are subjected to UV radiation to induce pigmentation pathways. Treatment with Cetyl tranexamate hydrochloride is shown to reduce melanin production and lower the levels of inflammatory markers. The compound is typically evaluated in the context of cosmetic formulations, with studies measuring tyrosinase activity and melanin content in treated melanocytes co-cultured with UV-irradiated keratinocytes. The compound inhibits the paracrine signals from keratinocytes to melanocytes, thereby reducing pigmentation at non-cytotoxic concentrations. Experimental designs often include measuring prostaglandin E2 levels as a marker of inflammation and cell viability using assays like MTT.
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| Animal Protocol |
Formal in vivo efficacy studies for Cetyl tranexamate hydrochloride are not commonly published in the context of drug development as it is primarily a cosmetic ingredient. However, its parent compound, tranexamic acid, has been studied in animal models of hyperpigmentation. In these models, topical application of tranexamic acid or its derivatives reduces UV-induced pigmentation in guinea pig or mouse skin. Histological analysis shows a decrease in epidermal melanin content and a reduction in the number of active melanocytes. For the ester derivative, efficacy is typically assessed in human clinical trials involving subjects with melasma or post-inflammatory hyperpigmentation, where parameters like the Melasma Area and Severity Index (MASI) are measured. Cetyl tranexamate hydrochloride can be formulated into creams and used in clinical studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies for Cetyl tranexamate hydrochloride are not applicable as it is a topical cosmetic ingredient rather than a systemically administered drug. It is designed to remain in the stratum corneum and upper layers of the epidermis after topical application. For the parent compound, tranexamic acid, systemic absorption following topical application is minimal. The ester derivative is more lipophilic than tranexamic acid, which enhances its skin penetration and retention in the epidermis. Any absorbed compound is likely metabolized to the parent drug tranexamic acid. As it is not intended for systemic circulation, standard PK parameters like half-life, Cmax, and AUC are not relevant or reported for this specific ester derivative.
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| Toxicity/Toxicokinetics |
No significant systemic toxicity is reported for Cetyl tranexamate hydrochloride at the concentrations used in cosmetic products. The parent compound, tranexamic acid, is generally well-tolerated when used topically, with mild and transient local reactions such as erythema, dryness, or peeling being the most common adverse effects. The hydrochloride salt form is stable and non-irritating at typical formulation levels. In clinical studies, the compound has been found to be safe for use as a skin conditioning agent. It is not intended for oral or systemic administration, thereby avoiding the rare risks associated with systemic tranexamic acid, such as thromboembolic events or visual disturbances. The compound is considered safe for use in cosmetic formulations.
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| References | |
| Additional Infomation |
The compound has CAS number 913541-96-5 and is also known as TXC hydrochloride. Its molecular formula is C24H48ClNO2, and its molecular weight is 418.10. It appears as a white to off-white solid powder. The IUPAC name is Cyclohexanecarboxylic acid, 4-(aminomethyl)-, hexadecyl ester, hydrochloride, trans-. It is soluble in DMSO and is often formulated into creams and lotions. The compound should be stored at -20degC in a sealed, dry environment protected from moisture and light. It is used exclusively for research and cosmetic applications.
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| Molecular Formula |
C24H48CLNO2
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| Molecular Weight |
418.10
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| Exact Mass |
417.337
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| CAS # |
913541-96-5
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| PubChem CID |
11962702
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
28
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| Complexity |
337
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCCCCCCCCOC(=O)C1CCC(CC1)CN.Cl
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| InChi Key |
VQDLZTHFZDRHQR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H47NO2.ClH/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-20-27-24(26)23-18-16-22(21-25)17-19-23;/h22-23H,2-21,25H2,1H3;1H
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| Chemical Name |
hexadecyl 4-(aminomethyl)cyclohexane-1-carboxylate;hydrochloride
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| Synonyms |
TXC hydrochloride
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 2.3918 mL | 11.9589 mL | 23.9177 mL | |
| 5 mM | 0.4784 mL | 2.3918 mL | 4.7835 mL | |
| 10 mM | 0.2392 mL | 1.1959 mL | 2.3918 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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