| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Myristyl nicotinate is enzymatically hydrolyzed to release nicotinic acid (vitamin B3) and myristyl alcohol. Nicotinic acid activates the G-protein-coupled receptor GPR109A (also known as HM74A), leading to vasodilation (flushing), inhibition of lipolysis in adipocytes, and anti-inflammatory effects. It may also modulate lipid metabolism. The myristyl moiety enhances skin penetration and provides emollient properties.
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|---|---|
| ln Vitro |
Myristyl niacin, also known as myristyl nicotinate, is used to treat and prevent skin barrier-damaging conditions like atopic dermatitis and chronic photodamage. It is also used to relieve the side effects of medications like steroids and retinoids that damage the skin barrier[2].
In vitro studies have demonstrated that Myristyl nicotinate is hydrolyzed by esterases in skin homogenates, releasing nicotinic acid. Nicotinic acid stimulates GPR109A in cultured keratinocytes and fibroblasts, leading to increased intracellular calcium and reduced pro-inflammatory cytokine production (e.g., IL-6, TNF-α). It also shows antioxidant activity by scavenging free radicals. The compound is non-cytotoxic to human skin cells at concentrations up to 100 μM. It may improve skin barrier function and hydration by increasing ceramide synthesis. |
| ln Vivo |
In vivo studies in animal models and humans have shown that topical application of Myristyl nicotinate (0.1-2% formulations) improves skin elasticity, reduces wrinkles, and decreases transepidermal water loss, indicating improved barrier function. It also reduces erythema and inflammation in models of UV-induced skin damage. In human trials, it has been used as a niacin source for skin rejuvenation. The vasodilatory effect of released niacin may cause transient flushing, but this is typically mild compared to oral niacin.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for Myristyl nicotinate typically involve esterase hydrolysis studies. The compound is incubated with porcine liver esterase or human skin homogenate in phosphate buffer at 37°C, and the release of nicotinic acid is measured by HPLC or LC-MS. For GPR109A binding, radioligand binding assays using ³H-nicotinic acid and membranes expressing GPR109A can be performed, with Myristyl nicotinate competing for binding (though it is a prodrug). Alternatively, nicotinic acid released is quantified. Antioxidant activity: DPPH or ABTS assays.
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| Cell Assay |
For in vitro cell-based assays, human keratinocytes (HaCaT) or fibroblasts are cultured and treated with Myristyl nicotinate (1-100 μM) for 24-48 hours. Cell viability by MTT. Inflammatory cytokines: cells are stimulated with LPS or UVB, and IL-6, TNF-α, IL-1β measured by ELISA. Intracellular calcium measured using Fluo-4 AM. Ceramide synthesis monitored by HPLC. Skin penetration studied using Franz diffusion cells with human skin; the amount of nicotinic acid in receptor fluid is quantified.
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| Animal Protocol |
In vivo animal studies: For skin anti-aging, hairless mice are exposed to UVB radiation (3 times/week) and topically treated with Myristyl nicotinate (1-2% cream) for 8 weeks. Skin wrinkling score, epidermal thickness (histology), and collagen content (Masson’s trichrome) are assessed. For anti-inflammatory, mice are treated with topical compound after acute UV irradiation, and skin edema and myeloperoxidase activity measured. For pharmacokinetics, animals are dosed topically and plasma/nicotinic acid levels measured. Human clinical studies are common for cosmetic products.
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| ADME/Pharmacokinetics |
Myristyl nicotinate (MW ~ 325 g/mol, formula C₂₀H₃₃NO₂) is lipophilic, soluble in oils and organic solvents, insoluble in water. In topical formulations, it penetrates the stratum corneum efficiently due to its fatty ester structure. Once absorbed, esterases hydrolyze it to nicotinic acid, which is then metabolized via normal niacin pathways. Systemic absorption is low, so plasma levels of nicotinic acid are minimal, reducing systemic side effects. Half-life in skin is a few hours.
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| Toxicity/Toxicokinetics |
Myristyl nicotinate is considered safe for topical use in cosmetics. In animal studies, no skin irritation or sensitization at concentrations up to 10%. No systemic toxicity due to low absorption. In human patch tests, it is non-irritating at 2%. The released niacin may cause mild transient flushing, but generally well-tolerated. Not intended for oral use. Approved as a cosmetic ingredient.
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| References |
[1]. Catz P, et al. Simultaneous determination of myristyl nicotinate, nicotinic acid, and nicotinamide in rabbit plasma by liquid chromatography-tandem mass spectrometry using methyl ethyl ketone as a deproteinization solvent. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Dec 27;829(1-2):123-35.
[2]. Jacobson MK, et al. Effect of myristyl nicotinate on retinoic acid therapy for facial photodamage. Exp Dermatol. 2007 Nov;16(11):927-35. |
| Additional Infomation |
Myristyl nicotinate is a niacin ester prodrug used in skincare products for anti-aging and skin conditioning. It delivers niacin to the skin topically, avoiding systemic side effects of oral niacin (flushing, hepatotoxicity). It is used in creams, serums, and lotions. It is not a drug but a cosmetic ingredient. Also known as myristyl nicotinate.
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| Molecular Formula |
C20H33NO2
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|---|---|
| Molecular Weight |
319.4815
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| Exact Mass |
319.251
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| CAS # |
273203-62-6
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| PubChem CID |
531641
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| Appearance |
White to yellow solid powder
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| Density |
0.953g/cm3
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| Boiling Point |
411.7ºC at 760 mmHg
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| Flash Point |
202.8ºC
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| Vapour Pressure |
5.46E-07mmHg at 25°C
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| Index of Refraction |
1.486
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| LogP |
5.939
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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 |
15
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| Heavy Atom Count |
23
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| Complexity |
281
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(C1=C([H])N=C([H])C([H])=C1[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H]
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| InChi Key |
TVGLGJWCZSCAEM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H33NO2/c1-2-3-4-5-6-7-8-9-10-11-12-13-17-23-20(22)19-15-14-16-21-18-19/h14-16,18H,2-13,17H2,1H3
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| Chemical Name |
tetradecyl pyridine-3-carboxylate
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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 : ~9.62 mg/mL (~30.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.96 mg/mL (3.00 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 9.6 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: ≥ 0.96 mg/mL (3.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 9.6 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1301 mL | 15.6504 mL | 31.3009 mL | |
| 5 mM | 0.6260 mL | 3.1301 mL | 6.2602 mL | |
| 10 mM | 0.3130 mL | 1.5650 mL | 3.1301 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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