TG4-155

ChemicalBook > CAS DataBase List > 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 (K_B = 2.4 nM) that is over 1000-fold less effective at EP₄ (K_B = 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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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