TG4-155

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TG4-155 是一种脑渗透性 EP2 拮抗剂 (KB = 2.4 nM)，其对 EP4 (KB = 11.4 μM) 和一组其他受体和通道的作用要低 1000 倍以上。

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 μM) and a panel of other receptors and channels.

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.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. Cell Viability Assay 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.

Administration of TG4-155 (5 mg/kg, i.p.; at 1 and 12 h) significantly reducesstatus epilepticus (SE)-induced neurodegeneration scores in C57BL/6 mice.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. Animal Model:C57BL/6 mice (8-12 wk old)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 miceDosage: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.

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GPCR/G Protein

Prostaglandin Receptor

EP2

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1164462-05-8

394.47

C23H26N2O4

>98% (HPLC)

DMSO:125 mg/mL?(316.89 mM)

COc1cc(\C=C\C(=O)NCCn2c(C)cc3ccccc23)cc(OC)c1OC

(E)-N-[2-(2-methylindol-1-yl)ethyl]-3-(345-trimethoxyphenyl)prop-2-enamide

(-20℃)

With Ice Pack

≥ 2 years