TG6-10-1
Modify Date: 2024-01-08 18:49:49
TG6-10-1 structure
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Common Name | TG6-10-1 | ||
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| CAS Number | 1415716-58-3 | Molecular Weight | 448.435 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 631.8±55.0 °C at 760 mmHg | |
| Molecular Formula | C23H23F3N2O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 335.9±31.5 °C | |
Use of TG6-10-1TG6-10-1 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. IC50 value: 7.5 μMTarget: serotonin 5-HT2B receptorin 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.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. |
| Name | (2E)-N-{2-[2-(Trifluoromethyl)-1H-indol-1-yl]ethyl}-3-(3,4,5-trimethoxyphenyl)acrylamide |
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| Synonym | More Synonyms |
| 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. IC50 value: 7.5 μMTarget: serotonin 5-HT2B receptorin 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.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. |
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| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
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| Boiling Point | 631.8±55.0 °C at 760 mmHg |
| Molecular Formula | C23H23F3N2O4 |
| Molecular Weight | 448.435 |
| Flash Point | 335.9±31.5 °C |
| Exact Mass | 448.160980 |
| LogP | 4.49 |
| Appearance of Characters | white solid |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.536 |
| Storage condition | -20℃ |
| (2E)-N-{2-[2-(Trifluoromethyl)-1H-indol-1-yl]ethyl}-3-(3,4,5-trimethoxyphenyl)acrylamide |
| 2-Propenamide, N-[2-[2-(trifluoromethyl)-1H-indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)- |
| TG6-10-1 |