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TG6-10-1 TG6-10-1, a potent and selective antagonist for the prostaglandin E2 receptor subtype EP2, has been shown antagonist activity at human EP2 receptor expressed in rat C6 cells. It shows low-nanomolar antagonist activity against EP2 (>300-fold selectivity ov. Synonyms: (E)-N-[2-[2-(trifluoromethyl)indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)prop-2-enamideTG6-10-1; TG 6-10-1; TG-6-10-1; TP6101; TP-6101; TP 6101. CHEMBL32642041415716-58-3C23H23F3N2O4BDBM50016950AKOS0274399 55CS-4637; AK-499428; HY-16978; CS 4637; AK 499428; HY 16978; CS4637; AK499428; HY16978(E)-N-(2-(2-(Trifluoromethyl)-1H-indol-1-yl)ethyl)-3-(3,4,5-trime. CAS No. 1415716-58-3. Molecular formula: C23H23F3N2O4. Mole weight: 448.43. BOC Sciences 10
Prostaglandin EP2 Receptor Antagonist, TG6-10-1 ( (E) -N- (2- (2- (trifluoromethyl) -1H-indol-1-yl) ethyl) -3- (3, 4, 5-trimethoxyphenyl) acrylamide, EP2 Antagonist, TG6-10-1) A cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8nM). Exhibits about 300-fold selectivity for the EP2 receptor over human EP3, EP4, and IP receptors, about 100- fold selectivity over human EP1, 25-fold selectivity against human FP and TP, and 10-fold selectivity against human DP1 receptors. Does not affect the activity of about 40 enzymes, ion channels, receptors, and neurotransmitters even at higher concentrations (˜10uM). Shown to significantly reduce the induction of several inflammatory cytokines and chemokines and reduces the opening of blood-brain barrier during neuronal inflammation. Displays good pharmacokinetic properties with a half-life of 1.6 h and brain to plasma ratio of 1.6 in a murine model (5mg/kg i.p.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??F?N?O?. US Biological Life Sciences. USBiological 4
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