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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1164462-05-8
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥990.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥360.0 |
| 规格: | 5 mg | 产品价格: | ¥900.0 |
| 规格: | 10 mg | 产品价格: | ¥1500.0 |
| 规格: | 25 mg | 产品价格: | ¥3000.0 |
| 规格: | 50 mg | 产品价格: | ¥5200.0 |
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TG4-155
CAS No. : 1164462-05-8
MCE 国际站:TG4-155
产品活性:TG4-155 是一种有效的脑渗透性的选择性 EP2 受体拮抗剂,Ki 为 9.9 nM。TG4-155 只对 EP2 和 DP1 具有低纳摩尔的拮抗活性。TG4-155 作用于 EP2 的 KB 为 2.4 nM,比对 DP1 受体的选择性高 14 倍,比对 EP1,EP3,EP4 和 IP 的选择性比高 550-4750 倍。
研究领域:GPCR/G Protein
作用靶点:Prostaglandin Receptor
In Vitro: 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.
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.
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.
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