产品
编 号：F052472
分子式：C23H26N2O4
分子量：394.46
分子式：C23H26N2O4
分子量：394.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1164462-05-8
产品详情
生物活性：
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1. 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.
体内研究：
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 mice
Dosage: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.
体外研究：
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.
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1. 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.
体内研究：
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 mice
Dosage: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.
体外研究：
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.
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