ChemicalBook > CAS DataBase List > TG4-155

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
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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.
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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.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1217
Product name
TG4-155
Purity
≥98% (HPLC)
Packaging
5MG
Price
$118
Updated
2024/03/01
Sigma-Aldrich
Product number
SML1217
Product name
TG4-155
Purity
≥98% (HPLC)
Packaging
25MG
Price
$462
Updated
2024/03/01
Cayman Chemical
Product number
17639
Product name
TG4-155
Purity
≥98%
Packaging
5mg
Price
$62
Updated
2024/03/01
Cayman Chemical
Product number
17639
Product name
TG4-155
Purity
≥98%
Packaging
10mg
Price
$109
Updated
2024/03/01
Cayman Chemical
Product number
17639
Product name
TG4-155
Packaging
25mg
Price
$239
Updated
2024/03/01
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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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1164462-05-8, TG4-155Related Search:


  • TG4-155
  • (E)-N-(2-(2-Methyl-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide
  • TG4-155; TG-4-155; TG 4-155; TG4155; TG-4155; TG 4155
  • (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)-
  • inhibit,TG4-155,TG-4-155,TG4155,TG4 155,Prostaglandin Receptor,Inhibitor
  • 1164462-05-8