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Purity: ≥98%
TG6-10-1 is a cell-permeable, highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2) with Kb of 17.8 nM. TG6-10-1 possesses adequate pharmacokinetic profiles for in vivo application. Systemic administration of TG6-10-1 completely recapitulates, without altering acute seizures, the effects of conditional ablation of cyclooxygenase-2 from principal forebrain neurons in the mouse pilocarpine model of status epilepticus (SE). These effects include reduced delayed mortality, accelerated recovery from weight loss, reduced brain inflammation, prevention of blood-brain barrier opening, and neuroprotection in the hippocampus. In humans, prolonged seizures are associated with high rates of mortality and morbidity as well as inflammation and injury to the brain. At this time, anticonvulsants are the only effective treatment that can stop seizures quickly enough to prevent brain damage. The findings imply that neuroinflammation and neurodegeneration are significantly influenced by the prostaglandin receptor EP2, and they suggest that treating SE with EP2 receptor antagonism is an additional therapeutic approach.
Targets |
EP2
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ln Vitro |
TG6-10-1 is a cell-permeable, highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2) with Kb of 17.8 nM. TG6-10-1 has sufficient pharmacokinetic profiles to be used in vivo. In the mouse pilocarpine model of status epilepticus (SE), systemic administration of TG6-10-1 completely recapitulates the effects of conditional ablation of cyclooxygenase-2 from principal forebrain neurons, namely reduced delayed mortality, accelerated recovery from weight loss, reduced brain inflammation, prevention of blood-brain barrier opening, and neuroprotection in the hippocampus, without modifying seizures acutely. Prolonged SE in humans causes high mortality and morbidity that are associated with brain inflammation and injury, but currently the only effective treatment is to stop the seizures quickly enough with anticonvulsants to prevent brain damage. The results suggest that the prostaglandin receptor EP2 is critically involved in neuroinflammation and neurodegeneration, and point to EP2 receptor antagonism as an adjunctive therapeutic strategy to treat SE.
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ln Vivo |
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Animal Protocol |
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Molecular Formula |
C23H23F3N2O4
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Molecular Weight |
448.43
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Exact Mass |
448.16
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Elemental Analysis |
C, 61.60; H, 5.17; F, 12.71; N, 6.25; O, 14.27
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CAS # |
1415716-58-3
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Appearance |
Solid powder
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SMILES |
COC1=CC(=CC(=C1OC)OC)/C=C/C(=O)NCCN2C3=CC=CC=C3C=C2C(F)(F)F
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InChi Key |
WUYOECAJFJFUFC-CMDGGOBGSA-N
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InChi Code |
InChI=1S/C23H23F3N2O4/c1-30-18-12-15(13-19(31-2)22(18)32-3)8-9-21(29)27-10-11-28-17-7-5-4-6-16(17)14-20(28)23(24,25)26/h4-9,12-14H,10-11H2,1-3H3,(H,27,29)/b9-8+
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Chemical Name |
(E)-N-[2-[2-(trifluoromethyl)indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)prop-2-enamide
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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: ≥ 3 mg/mL (6.69 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 30.0 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: ≥ 3 mg/mL (6.69 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 30.0 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 | 2.2300 mL | 11.1500 mL | 22.3000 mL | |
5 mM | 0.4460 mL | 2.2300 mL | 4.4600 mL | |
10 mM | 0.2230 mL | 1.1150 mL | 2.2300 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.
EP2 receptor antagonist reduces mortality and weight loss and accelerates functional recovery after SE.Proc Natl Acad Sci U S A.2013 Feb 26;110(9):3591-6. th> |
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EP2 receptor antagonist relieves brain inflammation after SE.Proc Natl Acad Sci U S A.2013 Feb 26;110(9):3591-6. td> |
EP2 receptor antagonist reduces neurodegeneration in hippocampus after SE.Proc Natl Acad Sci U S A.2013 Feb 26;110(9):3591-6. td> |