| Identification | Back Directory | [Name]
PNRI 299 | [CAS]
550368-41-7 | [Synonyms]
PNRI 299
PNRI 299,PNRI299
PNRI299;PNRI-299;PNRI 299
2-(3-Cyanophenyl)-2,3,7,8-tetrahydro-1,3,7-trioxo-N-(phenylmethyl)-1H-[1,2,4]triazolo[1,2-a]pyridazine-5-carboxamide
1H-[1,2,4]Triazolo[1,2-a]pyridazine-5-carboxamide, 2-(3-cyanophenyl)-2,3,7,8-tetrahydro-1,3,7-trioxo-N-(phenylmethyl)- | [Molecular Formula]
C21H15N5O4 | [MDL Number]
MFCD19443797 | [MOL File]
550368-41-7.mol | [Molecular Weight]
401.37 |
| Hazard Information | Back Directory | [Uses]
PNRI-299 is a selective AP-1 transcription inhibitor with an IC50 of 20 uM. PNRI-299 is a selective APE/Ref-1 inhibitor. PNRI-299 has no effect on NF-κB transcription or thioredoxin (up to 200 uM). PNRI-299 significantly reduces airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model[1][2][3]. | [in vivo]
PNRI-299 (intranasal; 0.75 or 2.0 mg/kg; 30 min before OVA on days 25-27) reduces the airway inflammatory cell infiltration (arrows) and mucus release in ovalbumin (OVA)-treated (i.p.; 100 μg) female BALB/c mice aged 6-8 wk)[1].
PNRI-299 (3, 10?mg/kg; iv; 5?min before reperfusion) has no significant effect on the translocation of NF-κB in male C57/BL6 mice (8-10 weeks). PNRI-299 has little effect on the inflammatory response that follows intestinal I/R injury[2].
| [IC 50]
IL-4 | [storage]
Store at -20°C | [References]
[1] Nguyen C, et al. Chemogenomic identification of Ref-1/AP-1 as a therapeutic target for asthma. Proc Natl Acad Sci U S A. 2003 Feb 4;100(3):1169-73. DOI:10.1073/pnas.0437889100
[2] Souza DG, et al. NF-kappaB plays a major role during the systemic and local acute inflammatory response following intestinal reperfusion injury. Br J Pharmacol. 2005 May;145(2):246-54. DOI:10.1038/sj.bjp.0706190
[3] Sun Yang, et al. Apurinic/apyrimidinic endonuclease/redox effector factor-1(APE/Ref-1): a unique target for the prevention and treatment of human melanoma. Antioxid Redox Signal. 2009 Mar;11(3):639-50. DOI:10.1089/ars.2008.2226 |
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