646530-37-2
中文名稱
化合物UTL-5G
英文名稱
3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-
CAS
646530-37-2
分子式
C11H8Cl2N2O2
分子量
271.1
MOL 文件
646530-37-2.mol
更新日期
2024/11/04 09:21:23
646530-37-2 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點336.2±42.0 °C(Predicted)
密度1.469±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
酸度系數(shù)(pKa)9.45±0.70(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
UTL-5g (GBL-5g) 是一種抗炎性 TNF-α 抑制劑，具有化學(xué)保護(hù)和肝臟放射保護(hù)作用。UTL-5g 通過抑制 TNF-α 等因子降低順鉑引起的肝毒性、腎毒性和骨髓毒性。體外研究
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.
體內(nèi)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. |