3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-
- Product Name
- 3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-
- CAS No.
- 646530-37-2
- Chemical Name
- 3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-
- Synonyms
- UTL-5;GBL-5g;UGL-5g;UTL-5g;UTL-5g ，S3540;UTL-5g, 10 mM in DMSO;N-(2,4-Dichlorophenyl)-5-methyl-3-isoxazolecarboxamide;N-(2,4-Dichlorophenyl)-5-methylisoxazole-3-carboxamide;3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl-;liver,inhibit,Inhibitor,chemoprotective,Tumor Necrosis Factor Receptor,radioprotective,acute,toxicity,hepatotoxicity,anti-inflammatory,TNF Receptor,UTL 5g,UTL5g,TNFR,UTL-5g
- CBNumber
- CB58146679
- Molecular Formula
- C11H8Cl2N2O2
- Formula Weight
- 271.1
- MOL File
- 646530-37-2.mol
3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl- Property
- Boiling point:
- 336.2±42.0 °C(Predicted)
- Density
- 1.469±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: Sparingly soluble: 1-10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml - form
- Solid
- pka
- 9.45±0.70(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl- Chemical Properties,Usage,Production
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
[4] J. SHAW. Pretreatment with A Small-Molecule Tumor Necrosis Factor-Alpha (TNF-α) Inhibitor, UTL-5g, Reduced Radiation-Induced Acute Liver Toxicity in Mice[J]. American Journal of Biomedical Sciences, 2012, 133 1: 123-131. DOI: 10.5099/aj120200123
3-Isoxazolecarboxamide, N-(2,4-dichlorophenyl)-5-methyl- Preparation Products And Raw materials
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