UTL-5g

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].

Research Areas >> Inflammation/Immunology

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.

UTL-5g (GBL-5g) lowers levels of TGF-β and TNF-α elevated by lung irradiation[1]. UTL-5g (60 mg/kg; p.o.; daily for 4 days) shows positive effects in increasing the survival rates and extending the survival times[3]. Animal Model: C57BL/6, male mice (8-10 weeks)[1] 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[3] 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.

[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.

[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.