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Purity: ≥98%
TG4-155 is a novel, potent and brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels. It prevents microglial cells treated with LPS and IFNγ or the selective EP2 agonist butaprost alone from expressing inflammatory markers. In a mouse model of pilocarpine-induced status epilepticus, TG4-155 dramatically lessens neurodegeneration. It prevents butaprost-treated cancer cells from proliferating, invading, or expressing inflammatory cytokines.
| Targets |
PTGER2 ( Ki = 9.9 nM )
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|---|---|
| ln Vitro |
TG4-155 suppresses the hERG (human Ether-à-go-go-Related Gene) at IC50=12 µM and the serotonin 5-HT2B receptor at IC50=2.6 µM[1].
PGE2 (0.1-10 μM) stimulation dramatically increases the growth of the human prostate cancer cell line PC3 cell in a concentration-dependent manner, with a maximal response occurring at about 1 µM. TG4-155 (0.01-1μM; 48 hours) dramatically suppresses this PGE2-induced cancer cell proliferation in a concentration-dependent manner[1]. |
| ln Vivo |
TG4-155 (5 mg/kg, i.p.; at 1 and 12 h) administration significantly lowers the neurodegeneration scores caused by status epilepticus (SE) TG4-155 (5 mg/kg, i.p.; at 1 and 12 h) administration significantly lowers the neurodegeneration scores caused by status epilepticus (SE)[3].
TG4-155 (3 mg/kg; intraperitoneal; i.p.) exhibits a plasma half-life (t1/2) of 0.6 h, a brain/plasma ratio of 0.3, and a bioavailability of 61% (i.p. route relative to i.v.) in C57BL/6 mice[3]. |
| Cell Assay |
Cell Line: PC3 cells
Concentration: 48 hours Incubation Time: 0.01, 0.1, and 1 μM Result: Significantly suppressed PGE2-induced cancer cell proliferation in a concentration-dependent manner. |
| Animal Protocol |
C57BL/6 mice (8-12 wk old)
5 mg/kg I.p.; at 1 and 12 h |
| References |
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| Molecular Formula |
C23H26N2O4
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|---|---|
| Molecular Weight |
394.463546276093
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| Exact Mass |
394.19
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| Elemental Analysis |
C, 70.03; H, 6.64; N, 7.10; O, 16.22
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| CAS # |
1164462-05-8
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| Appearance |
Solid powder
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| SMILES |
CC1=CC2=CC=CC=C2N1CCNC(=O)/C=C/C3=CC(=C(C(=C3)OC)OC)OC
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| InChi Key |
YBHUXHFZLMFETJ-MDZDMXLPSA-N
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| InChi Code |
InChI=1S/C23H26N2O4/c1-16-13-18-7-5-6-8-19(18)25(16)12-11-24-22(26)10-9-17-14-20(27-2)23(29-4)21(15-17)28-3/h5-10,13-15H,11-12H2,1-4H3,(H,24,26)/b10-9+
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| Chemical Name |
(E)-N-[2-(2-methylindol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)prop-2-enamide
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| Synonyms |
TG4155; TG4-155; TG-4-155; TG-4155; TG 4-155; TG 4155
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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 |
| 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: 79~125 mg/mL (200.3~316.9 mM)
Ethanol: ~5 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.27 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 20.8 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: ≥ 2.08 mg/mL (5.27 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5%DMSO + Corn oil: 4.0mg/ml (10.14mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5351 mL | 12.6756 mL | 25.3511 mL | |
| 5 mM | 0.5070 mL | 2.5351 mL | 5.0702 mL | |
| 10 mM | 0.2535 mL | 1.2676 mL | 2.5351 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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