| Identification | Back Directory | [Name]
3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl- | [CAS]
646530-37-2 | [Synonyms]
UTL-5g
UGL-5g
3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl- | [Molecular Formula]
C11H8Cl2N2O2 | [MDL Number]
MFCD08724989 | [MOL File]
646530-37-2.mol | [Molecular Weight]
271.1 |
| Chemical Properties | Back Directory | [Boiling point ]
336.2±42.0 °C(Predicted) | [density ]
1.469±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
9.45±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
UTL-5g (GBL-5g), an anti-inflammatory TNF-α inhibitor, has chemoprotective and liver radioprotective effects. UTL-5g lowers hepatotoxicity, nephrotoxicity, and myelotoxicity induced by Cisplatin through TNF-α inhibition among other factors[1][2]. | [Biological Activity]
UTL-5g (GBL-5g) is an anti-inflammatory TNF-α inhibitor with chemoprotective and hepatic radioprotective effects. It reduces cisplatin-induced hepatotoxicity, nephrotoxicity and bone marrow toxicity by inhibiting factors such as TNF-α. | [in vitro]
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. | [in vivo]
UTL-5g (GBL-5g) lowers levels of TGF-β and TNF-α elevated by lung irradiation.
UTL-5g (60 mg/kg; po; 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 | < /tr> | Administration: | Ip; before irradiation, daily x 5 | | Result: | Blood levels of TGF-β were lowered. | | Animal Model: | BDF1 female mice | | Dosage: | Po; daily for 4 days | | Administration: | 60 mg/kg (30 min before ip 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. | | [References]
[1] Stephen Brown, et al. UTL-5g Lowers Levels of TGF-β and TNF-α Elevated by Lung Irradiation
[2] Carruthers NJ, et al. Phosphoproteome and transcription factor activity profiling identify actions of the anti-inflammatory agent UTL-5g in LPS stimulated RAW 264.7 cells including disrupting actin remodeling and STAT-3 activation. Eur J Pharmacol. 2017;811:66-73. DOI:10.1016/j.ejphar.2017.05.049
[3] Shaw J, et al. The small-molecule TNF-α inhibitor, UTL-5g, delays deaths and increases survival rates for mice treated with high doses of cisplatin. Cancer Chemother Pharmacol. 2013;72(3):703-707. DOI:10.1007/s00280-013-2236-4 |
|
|