1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. TG4-155

TG4-155 

Cat. No.: HY-18971
Handling Instructions

TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor.

For research use only. We do not sell to patients.

TG4-155 Chemical Structure

TG4-155 Chemical Structure

CAS No. : 1164462-05-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 130 In-stock
Estimated Time of Arrival: December 31
25 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
100 mg USD 880 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM[1][2]. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1[1]. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor[2].

IC50 & Target[2]

EP2 Receptor

9.9 nM (Ki)

In Vitro

TG4-155 inhibits the serotonin 5-HT2B receptor with IC50=2.6 µM and hERG (human Ether-à-go-go-Related Gene) with IC50=12 µM[1].
PGE2 (0.1-10 μM) stimulation significantly enhances human prostate cancer cell line PC3 cell growth in a concentration-dependent manner with a maximal response being obtained at approximately 1 µM. This PGE2-induced cancer cell proliferation is significantly suppressed by TG4-155 (0.01-1μM ; 48 hours) in a concentration-dependent manner[1].

Cell Viability Assay[1]

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.
In Vivo

Administration of TG4-155 (5 mg/kg, i.p.; at 1 and 12 h) significantly reduces status epilepticus (SE)-induced neurodegeneration scores in C57BL/6 mice[3].
TG4-155 (3 mg/kg; i.p.) displays a bioavailability of 61% (i.p. route compared with i.v.), a plasma half-life (t1/2) of 0.6 h, and a brain/plasma ratio of 0.3 in C57BL/6 mice[3].

Animal Model: C57BL/6 mice (8-12 wk old)[3]
Dosage: 5 mg/kg
Administration: I.p.; at 1 and 12 h
Result: Administration significantly reduced SE-induced neurodegeneration scores by 91% in hippocampal subregions CA1, by 80% in CA3, and by 63% in hilus.
Animal Model: C57BL/6 mice[3]
Dosage: 3 mg/kg
Administration: I.p.
Result: Displayed a bioavailability of 61% (i.p. route compared with i.v.), t1/2 of 0.6 h, and a brain/plasma ratio of 0.3.
Molecular Weight

394.46

Formula

C₂₃H₂₆N₂O₄

CAS No.

1164462-05-8

SMILES

O=C(NCCN1C(C)=CC2=C1C=CC=C2)/C=C/C3=CC(OC)=C(OC)C(OC)=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (316.89 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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TG4-155
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HY-18971
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