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Purity: ≥98%
Defensamide (formerly known as MHP and methyl caprooyl tyrosinate) is a novel and potent activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC. MHP activation of SPHK1, a target enzyme of CAMP production, can stimulate innate immunity. Treatment with MHP directly activated SPHK1 and increased cellular S1P content in normal cultured human KC. Because MHP did not inhibit S1P lyase activity, which hydrolyses S1P, augumented S1P levels could be attributed to increased synthesis rather than blockade of S1P degradation.
| ln Vitro |
In keratinocytes, MHP (50-250 μM) for 24 hours raises the levels of CAMP mRNA [1]. MHP (100 μM) elevates the levels of CAMP protein in keratinocytes for a 24-hour period [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Keratinocytes Tested Concentrations: 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Increased CAMP protein levels in keratinocytes. |
| References |
| Molecular Formula |
C16H23NO4
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|---|---|---|
| Molecular Weight |
293.36
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| Exact Mass |
293.163
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| CAS # |
1104874-94-3
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| Related CAS # |
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| PubChem CID |
56652925
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| Appearance |
White to off-white solid powder
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| LogP |
3.013
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
21
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| Complexity |
324
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCCCCC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)OC
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| InChi Key |
GBTVWZMJUZJPBU-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C16H23NO4/c1-3-4-5-6-15(19)17-14(16(20)21-2)11-12-7-9-13(18)10-8-12/h7-10,14,18H,3-6,11H2,1-2H3,(H,17,19)/t14-/m0/s1
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| Chemical Name |
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.52 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 25.0 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: ≥ 2.5 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (8.52 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 | 3.4088 mL | 17.0439 mL | 34.0878 mL | |
| 5 mM | 0.6818 mL | 3.4088 mL | 6.8176 mL | |
| 10 mM | 0.3409 mL | 1.7044 mL | 3.4088 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.
Inhibition ofS. aureusinvasion into murine skin.J Dermatol Sci. 2015 Sep; 79(3): 229–234 |
NF-κB activation is required for MHP-induced upregulation of CAMP production.J Dermatol Sci. 2015 Sep; 79(3): 229–234. |
MHP increases CAMP mRNA and protein expression.J Dermatol Sci. 2015 Sep; 79(3): 229–234. |
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