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Purity: ≥98%
TMS (Tetramethoxystilbene), an analogue of resveratrol, is a potent and selective CYP1B1 inhibitor with an IC50 of 6 nM. TMS may inhibit r7, t8, t9-trihydroxy-c-10-(N(2)deoxyguanosyl)-7,8,9,10-tetrahydro-benzo[a]pyrene (BPdG) adduct formation in cells exposed to benzo[a]pyrene (BP). TMS reversed increased BP in SHR (207 ± 7 vs. 129 ± 2 mmHg) without altering BP in Wistar-Kyoto rats. Increased CYP1B1 activity in SHR was inhibited by TMS (RLU: aorta, 5.4 ± 0.7 vs. 3.7 ± 0.7; heart, 6.0 ± 0.8 vs. 3.4 ± 0.4; kidney, 411 ± 45 vs. 246 ± 10). TMS can suppress adipogenic differentiation of C3H10T1/2 cells by inhibiting PPARγ. 2,3',4,5'-Tetramethoxystilbene prevents deoxycorticosterone-salt-induced hypertension: contribution of cytochrome P-450 1B1.
| ln Vitro |
Because TMS is a strong CYP1B1 inhibitor, it is regarded as a possible cancer preventative drug and an equivalent of resveratrol. Cells were cultured for up to 72 hours without changing the media in order to assess the survival of MCF-7 cells exposed to 1 μM benzo[a]pyrene (BP), 1 μM BP + 1 μM TMS, and 1 μM BP + 4 μM TMS. cells exposed to light expressed as a percentage of cells treated with solvent (DMSO) at the same time interval in terms of luminescence units. For the first 24 hours, cell viability in all exposure groups was >90%; however, by the 72nd hour, it had decreased to 60–70% [1].
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| ln Vivo |
The effect of TMS was investigated in SHR and WKY rats in order to ascertain the function of CYP1B1 in the development of hypertension in spontaneously hypertensive rats (SHR). Starting at 4 weeks of age, the systolic blood pressure in SHR grew gradually. Daily TMS injections started to lower the SHR's systolic blood pressure at 8 weeks of age, returning it to the initial values (207±7 vs. 129±2 mmHg). In WKY treated with TMS or its carrier, systolic blood pressure did not alter (129±7 vs. 127±4 mmHg) [1].
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| References |
[1]. Sanghee Kim, et al. Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors. J Med Chem. 2002 Jan 3;45(1):160-4.
[2]. Einem Lindeman T, et al. The resveratrol analogue, 2,3',4,5'-tetramethoxystilbene, does not inhibit CYP gene expression, enzyme activity and benzo[a]pyrene-DNA adduct formation in MCF-7 cells exposed to benzo[a]pyrene. Mutagenesis. 2011 Sep;26(5):629-35. [3]. Jennings BL, et al. Cytochrome P450 1B1 contributes to increased blood pressure and cardiovascular and renal dysfunction in spontaneously hypertensive rats. Cardiovasc Drugs Ther. 2014 Apr;28(2):145-61 |
| Molecular Formula |
C18H20O4
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| Molecular Weight |
300.35
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| CAS # |
24144-92-1
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| SMILES |
COC1=CC(OC)=CC(/C=C/C2=CC=C(OC)C=C2OC)=C1
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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 (8.32 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 (8.32 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 25.0 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 | 3.3294 mL | 16.6472 mL | 33.2945 mL | |
| 5 mM | 0.6659 mL | 3.3294 mL | 6.6589 mL | |
| 10 mM | 0.3329 mL | 1.6647 mL | 3.3294 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.
TMS reduced vascular oxidative stress and NADPH oxidase activity in SHR.Cardiovasc Drugs Ther.2014 Apr;28(2):145-61. |
TMS reduced increased CYP1B1 activity in SHR, which is not associated with changes in protein expression.Cardiovasc Drugs Ther.2014 Apr;28(2):145-61. |
TMS decreased cardiac and renal fibrosis in SHR.Cardiovasc Drugs Ther.2014 Apr;28(2):145-61. |
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