TG4-155
- Product Name
- TG4-155
- CAS No.
- 1164462-05-8
- Chemical Name
- TG4-155
- Synonyms
- TG4-155;TG4-155; TG-4-155; TG 4-155; TG4155; TG-4155; TG 4155;inhibit,TG4-155,TG-4-155,TG4155,TG4 155,Prostaglandin Receptor,Inhibitor;(E)-N-(2-(2-Methyl-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide;(2E)-N-[2-(2-Methyl-1H-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-2-propenamide;2-Propenamide, N-[2-(2-methyl-1H-indol-1-yl)ethyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-
- CBNumber
- CB13067584
- Molecular Formula
- C23H26N2O4
- Formula Weight
- 394.46
- MOL File
- 1164462-05-8.mol
TG4-155 Property
- Boiling point:
- 641.3±55.0 °C(Predicted)
- Density
- 1.14±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 10 mg/ml).
- pka
- 14.04±0.46(Predicted)
- form
- solid
- color
- Off-white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- SML1217
- Product name
- TG4-155
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $118
- Updated
- 2024/03/01
- Product number
- SML1217
- Product name
- TG4-155
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $462
- Updated
- 2024/03/01
- Product number
- 17639
- Product name
- TG4-155
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 17639
- Product name
- TG4-155
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- 17639
- Product name
- TG4-155
- Packaging
- 25mg
- Price
- $239
- Updated
- 2024/03/01
TG4-155 Chemical Properties,Usage,Production
Description
Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection. TG4-155 is a 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 blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost alone or with LPS and IFNγ. TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine . It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.
Uses
TG4-155 is a pharmacological agent which reduces neurodegeneration in a mouse model status of epilepticus induced by pilocarpine. Inhibits proliferation, inflammatory cytokine expression in cancer cells.
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].
IC 50
2.4 nm for kb ep2; 11.4 nm for kb ep4
storage
Store at +4°C
References
1) Jiang and Dingledine (2013),?Role of prostaglandin receptor EP2 in the regulations of cancer cell proliferation, invasion, and inflammation; J. Pharmacol. Exp. Ther.?344?360 2) Quan?et al.?(2013),?EP2 Receptor Signaling Pathways Regulate Classical Activation of Microglia; J. Biol. Chem.?288?9293
TG4-155 Preparation Products And Raw materials
Raw materials
Preparation Products
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