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| Targets |
NF-κB mTOR
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| ln Vitro |
TML-6 (0.65–5.24 µg/mL; for 24 hours) increases the expression of ApoE protein while decreasing that of APP and phospho-NF-κB. TML-6 suppresses phospho-mTOR, which in turn inhibits the mTOR signaling pathway[1]. With an IC50 of 4.19 µg/mL (8 μM), TML-6 (0.31, 0.63, 2.5, 5, 10, 20 μM; 24 h) exhibits minimal cytotoxicity in Huh-7 cells at concentrations below 5 μM[1]. In N2a/APPswe cells, TML-6 (1.05, 2.09, 3.14, 4.19 μg/mL; 24 h) dose-dependently decreases the production of Aβ40 and Aβ42 between 1.05, 2.09, and 3.14 μg/mL (equivalent to 2, 4 and 6 μM)[1]. TML-6 has the ability to activate the Nrf2 gene transcriptionally in a dose-dependent manner; the maximum activity is observed at 1.32 µg/mL[1].
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| ln Vivo |
Treatment with TML-6 (diet; 150 mg/kg/day; for four months) significantly improves learning and reduces Aβ in the brain and the microglial activation marker Iba-1[1]. The T1/2, Cmax, and AUC of TML-6 (oral; 150 mg/kg) are 1.27 hours, 35.9 ng/mL, and 177 ng·hr/mL, respectively[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Huh-7 cells Tested Concentrations: 0.65, 1.31, 1.96, 2.61, 3.93, 5.24 µg/mL Incubation Duration:For 24 hrs (hours) Experimental Results: diminished the amyloid precursor protein (APP) protein expression level by 60 % and diminished the level of phosphorylated NF-κB by about 50% at a dose of 1.96 µg/mL after 24 h treatment. Induced the protein expression level of ApoE by approximately 44% at a dose of 2.62 µg/mL. |
| Animal Protocol |
Animal/Disease Models: Six-month-old 3xTg (mutations: APPKM670 /671NL, MAPTP301L and PSEN1M146V) AD transgenic mice[1]
Doses: 150 mg/kg Route of Administration: Diet; daily; for four months Experimental Results: Improved the learning behaviors, Dramatically suppressed the Aβ levels and Iba-1 expression in the brain of 3xTg AD transgenic mice. Animal/Disease Models: SD rats[1] Doses: 150 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Oral Experimental Results: Had a T1/2 of 1.27 hrs (hours), a Cmax of 35.9 ng/mL and an AUC of 177 ng• hr/mL. |
| References |
[1]. Ih-Jen Su, et al. A Curcumin Analog Exhibits Multiple Biologic Effects on the Pathogenesis of Alzheimer's Disease and Improves Behavior, Inflammation, and β-Amyloid Accumulation in a Mouse Model. Int J Mol Sci. 2020 Jul 30;21(15):5459.
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| Molecular Formula |
C30H37NO7
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|---|---|
| Molecular Weight |
523.62
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| CAS # |
1462868-88-7
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| Related CAS # |
TML-6-d3;2673270-28-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(CC(C(/C=C/C1C=CC(=C(C=1)OC)OC)=O)(C(/C=C/C1C=CC(=C(C=1)OC)OC)=O)C)N(CC)CC
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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. |
| 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: 120 mg/mL (229.17 mM)
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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 | 1.9098 mL | 9.5489 mL | 19.0978 mL | |
| 5 mM | 0.3820 mL | 1.9098 mL | 3.8196 mL | |
| 10 mM | 0.1910 mL | 0.9549 mL | 1.9098 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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