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| 50mg |
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| 100mg |
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| ln Vitro |
In cerebellar granule cells, (E)-3,4,5-Trimethoxycinnamic Acid (10 μg/mL, 1 h) enhances the expression of GAD65 and GABAA receptor γ subunit [3]. Cl-influx significantly increased in response to (E)-3,4,5-Trimethoxycinnamic acid (0–10 μg/mL, 1 h) [3].
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| ln Vivo |
(E)-3,4,5-Trimethoxycinnamic acid (0–20 mg/kg IP once) exhibits antiepileptic properties [2]. (E)-3,4,5-Trimethoxycinnamic Acid (0–10 mg/kg, orally administered once) can increase the hypnotizing effect in mice administered pentobarbital [3].
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| Cell Assay |
Western Blot analysis [3]
Cell Types: primary cultured cerebellar granule cells Tested Concentrations: 10 μg/mL Incubation Duration: 1 h Experimental Results: The expression of GAD65 (glutamic acid decarboxylase) and GABAA receptor γ subunit increased, but not Affects the content of a and b subunits in GABAA receptors. Cell viability assay [3] Cell Types: Primary cultured cerebellar granule cells Tested Concentrations: 1, 3, 5, 10 μg/mL Incubation Duration: 1 hour Experimental Results: Cl- influx increased Dramatically. |
| Animal Protocol |
Animal/Disease Models: Adult male Kunming mice (18-20 g, maximum electroshock (MES) and pentylenetetrazole (PTZ) models) [2]
Doses: 5, 10 and 20 mg/kg; 10 mL/kg Route of Administration: IP, primary Experimental Results: The incidence of MES-induced THE (tetanic hindlimb extension) was Dramatically diminished to 50% and 20% of vehicle control values at 10 and 20 mg/kg. At the 5 mg/kg dose, the incidence of MES-induced THE was only diminished by 80%. In a PTZ seizure model, the onset of myoclonic jerks (MJ) was Dramatically delayed and seizure severity and mortality were diminished compared with vehicle-treated animals. The incidence of generalized clonic convulsions (stage 4) disappeared at both 10 and 20 mg/kg doses. Animal/Disease Models: ICR male mice (25-28 g, 10-12 per group) [3] Doses: 2, 5 and 10 mg/kg Route of Administration: oral (po), once, 15 minutes and 1 before injection hour, results of pentobarbital injection: significant decrease in locomotor activity at 10 mg/kg. NREM and total sleep time increased, but wakefulness decreas |
| References |
[1]. Zhao Z, et al. Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. Eur J Med Chem. 2019 Jul 1;173:213-227.
[2]. Chen CY, et al. 3,4,5-Trimethoxycinnamic acid, one of the constituents of Polygalae Radix exerts anti-seizure effects by modulating GABAAergic systems in mice. J Pharmacol Sci. 2016 May;131(1):1-5. [3]. Lee CI, et al. 3,4,5-Trimethoxycinnamic acid (TMCA), one of the constituents of Polygalae Radix enhances pentobarbital-induced sleeping behaviors via GABAAergic systems in mice. Arch Pharm Res. 2013 Oct;36(10):1244-51. |
| Molecular Formula |
C12H14O5
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|---|---|
| Molecular Weight |
238.2366
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| CAS # |
20329-98-0
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| SMILES |
O(C([H])([H])[H])C1C(=C([H])C(/C(/[H])=C(\[H])/C(=O)O[H])=C([H])C=1OC([H])([H])[H])OC([H])([H])[H]
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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 : ~100 mg/mL (~419.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.49 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 (10.49 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 (10.49 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 | 4.1974 mL | 20.9872 mL | 41.9745 mL | |
| 5 mM | 0.8395 mL | 4.1974 mL | 8.3949 mL | |
| 10 mM | 0.4197 mL | 2.0987 mL | 4.1974 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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