TG4-155 |
Catalog No.GC13732
One-Click Copy Product Info
|
brain penetrant EP2 antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1164462-05-8
Sample solution is provided at 25 µL, 10mM.
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IC50: 2.4 nM for KB EP2; 11.4 nM for KB EP4
TG4-155 is a brain penetrant EP2 antagonist.
Prostaglandin E2 (PGE2) evokes distinct responses via four different ‘E prostanoid’ (EP) receptors. EP2, a G protein-coupled receptor, has diverse roles, such as those in cancer, inflammation, and neuroprotection.
In vitro: Using a set of cell-based TR-FRET assays of cAMP formation, a previous study screened a small molecule library and identified TG4-155 and TG4-166 as the most potent ones. TG4-155 and TG4-166 also showed robust inhibition of PGE2 -induced cAMP accumulation in human EP2-overexpressing C6 glioma cells, without affecting prostaglandin EP4 or β2-adrenergic receptors. Both TG4-155 and TG4-166 could cause a robust rightward shift in the PGE2 dose–response curve without affecting the maximal response to PGE2. TG4-155 at 1 μM caused 1,120-fold shift and TG4-166 at 1 μM caused a 651-fold shift in the PGE2 EC50 [1].
In vivo: TG4-155 could significantly reduced neuronal injury in hippocampus when administered in mice beginning 1 h after termination of pilocarpine-induced status epilepticus. The salutary actions of TG4-155 raised the possibility that selective block of EP2 signaling through small molecules can be an innovative therapeutic strategy for inflammation-related brain injury [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Jiang, J. ,Ganesh, T.,Du, Y., et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2. Proceedings of the National Academy of Sciences of the United States of America 109(8), 3149-3154 (2012).
| Cas No. | 1164462-05-8 | SDF | |
| Chemical Name | (2E)-N-[2-(2-methyl-1H-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide | ||
| Canonical SMILES | COC1=CC(/C=C/C(NCCN2C(C)=CC3=C2C=CC=C3)=O)=CC(OC)=C1OC | ||
| Formula | C23H26N2O4 | M.Wt | 394.5 |
| Solubility | ≤5mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5349 mL | 12.6743 mL | 25.3485 mL |
| 5 mM | 507 μL | 2.5349 mL | 5.0697 mL |
| 10 mM | 253.5 μL | 1.2674 mL | 2.5349 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)