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Home > Inhibitors & Agonists > GPCR > Prostaglandin Receptor

TG6-10-1

  Cat. No.:  DC8348   Featured
Chemical Structure
1415716-58-3
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More than 5000 active chemicals with high quality for research!
Field of application
TG6-10-1 is a cell-permeable,highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1415716-58-3
Chemical Name: (E)-N-(2-(2-(trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trimethoxyphenyl)acrylamide
SMILES: C(NCCN1C2=C(C=CC=C2)C=C1C(F)(F)F)(=O)/C=C/C1=CC(OC)=C(OC)C(OC)=C1
Formula: C23H23F3N2O4
M.Wt: 448.43
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.
In Vivo: TG6-10-1 displayed a plasma half-life of 1.6 h and a brain:plasma ratio of 1.6 after systemic administration (5 mg/kg, i.p.) in mice. A significant increase in survival was observed in post-SE mice that received TG6-10-1 compared with those in the vehicle group. Administration of TG6-10-1 improved 1-wk survival from 60 to 90% after SE.
In Vitro: TG6-10-1, an analog of TG4-155 (a prostaglandin receptor EP2 antagonist, with a relatively short plasma half-life (0.6 h) and low brain:plasma ratio (0.3) after systemic administration in mice), which has a superior pharmacokinetic profile making it suitable for more extensive testing. TG6-10-1 had negligible effect on a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s > 10 μM), except that TG6-10-1 weakly inhibited the serotonin 5-hydroxytryptamine 2B (5-HT2B) receptor with IC50 = 7.5 μM. At a high concentration (10 μM), TG6-10-1 had little or no effect on the enzymatic activity of COX-1 (7% inhibition) and COX-2 (14% inhibition), and inhibited the leukotriene B4 (LTB4) receptor BLT1 by 1% .EP2 receptor activation by PGE2 stimulates adenylate cyclase to elevate cytoplasmic cAMP level. TG6-10-1 has a competitive mechanism of antagonism of the EP2 receptor with an equilibrium dissociation constant for the antagonist-receptor complex (KB) of 17.8 nM.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC48172 BAY-6672 BAY-6672 is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.
DC10475 Grapiprant Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2)
DC8348 TG6-10-1 TG6-10-1 is a cell-permeable,highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM).
DC9609 Terutroban Terutroban is a thromboxane/prostaglandin endoperoxide receptor antagonist.
DC8624 Setipiprant(ACT129968) Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.
DC8353 PF-04418948 PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).
DC11043 Omidenepag Omidenepag is a potent, selective agonist human EP2 receptor with binding IC50/EC50 of 10/1.7 nM, >500-fold selectivity over EP1, EP3 and EP4 receptors; Omidenepag is the active form of Omidenepag Isopropyl (OMDI).
DC10437 MRE-269 MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
DC10785 MK-7246 MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
DC1009 Laropiprant MK 0524 is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.
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