化合物UTL-5G

生物活性体外研究体内研究化合物UTL-5G 试剂级价格

化合物UTL-5G

CAS号:646530-37-2
英文名:3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-
中文名:化合物UTL-5G
CBNumber:CB58146679
分子式:C11H8Cl2N2O2
分子量:271.1
MOL File:646530-37-2.mol

化合物UTL-5G化学性质

沸点 :336.2±42.0 °C(Predicted)
密度 :1.469±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
酸度系数(pKa) :9.45±0.70(Predicted)
形态 :Solid
颜色 :White to off-white

化合物UTL-5G性质、用途与生产工艺

生物活性 UTL-5g (GBL-5g) 是一种抗炎性 TNF-α 抑制剂，具有化学保护和肝脏放射保护作用。UTL-5g 通过抑制 TNF-α 等因子降低顺铂引起的肝毒性、肾毒性和骨髓毒性。
体外研究

RAW 264.7 macrophages are transfected with the respective reporter assay plasmids, pretreated with UTL-5g at 1, 10 or 50 µM for 60 min and then challenged with 100 ng/ml LPS. After a 16 h incubation, transcription factor activity is measured. Transcription factors that shows a UTL-5g dose-dependent decrease in activity in two experiments are categorized as being disrupted by UTL-5g.

体内研究

UTL-5g (GBL-5g) lowers levels of TGF-β and TNF-α elevated by lung irradiation.
UTL-5g (60 mg/kg; p.o.; daily for 4 days) shows positive effects in increasing the survival rates and extending the survival times.

Animal Model:	C57BL/6, male mice (8-10 weeks)
Dosage:	15, 30, and 60 mg/kg
Administration:	I.p.; before irradiation, daily x 5
Result:	Blood levels of TGF-β were lowered.

Animal Model:	BDF1 female mice
Dosage:	P.o.; daily for 4 days
Administration:	60 mg/kg (30 min before i.p. injection of Cisplatin at 10, 15, and 20 mg/kg respectively on Day 0)
Result:	Increased the survival rate and delayed the time to death for mice treated with 150% of the maximum tolerated dose (MTD) of Cisplatin (15 mg/kg). At 200% of the MTD of Cisplatin (20 mg/kg), treatment of UTL-5g increased the survival rate and delayed the time to death.