| Bioactivity | 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| 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: | ||||||||||||
| Name | TG4-155 | ||||||||||||
| CAS | 1164462-05-8 | ||||||||||||
| Formula | C23H26N2O4 | ||||||||||||
| Molar Mass | 394.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Jiang J, et al. Role of prostaglandin receptor EP2 in the regulations of cancer cell proliferation, invasion, and inflammation. J Pharmacol Exp Ther. 2013 Feb;344(2):360-7. [2]. Ganesh T. Prostanoid receptor EP2 as a therapeutic target. J Med Chem. 2014 Jun 12;57(11):4454-65. [3]. Jiang J, et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):3149-54. |