| Identification | Back Directory | [Name]
AL 8697 | [CAS]
1057394-06-5 | [Synonyms]
AL 8697
3-[3-(tert-Butyl)-6,8-difluoro-[1,2,4]triazolo[4,3-a]pyridin-7-yl]-N-cyclopropyl-5-fluoro-4-methylbenzamide
N-Cyclopropyl-3-[3-(1,1-dimethylethyl)-6,8-difluoro-1,2,4-triazolo[4,3-a]pyridin-7-yl]-5-fluoro-4-methylbenzamide
Benzamide, N-cyclopropyl-3-[3-(1,1-dimethylethyl)-6,8-difluoro-1,2,4-triazolo[4,3-a]pyridin-7-yl]-5-fluoro-4-methyl- | [Molecular Formula]
C21H21F3N4O | [MOL File]
1057394-06-5.mol | [Molecular Weight]
402.41 |
| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
<40.24mg/ml in DMSO; <20.12mg/ml in ethanol | [form ]
solid | [pka]
13.57±0.20(Predicted) | [color ]
White |
| Hazard Information | Back Directory | [Uses]
AL 8697 is a selective and potent p38α inibitor and has potential use as antiinflammatory agents against diseases such as arthritis. | [Biological Activity]
al8697 is a selective p38 mapk(mitogen-activated protein kinase) inhibitor, which is also named p38 α inhibitor. it has the function of inhibiting the activity of p38 mapk.[1]mitogen activated protein kinases (mapk) are a group of signaling molecules that appear to play important roles in inflammatory processes. the p38 mapk is one of the best described mapk cascades. the p38 mapk plays a key role in both the synthesis and the signalling of pro-inflammatory cytokines such as tnfa and il-6 by monocyte/macrophages. the p38 mapk are involved in the up-regulation of tnf production by murine macrophages.it has high activity in cardiovascular cells under a variety of cellular stresses. in cardiovascular disease, the p38 mapk signaling pathways are activated.[2,3]al8697 function by the inhibition of p38 mapk. it regulates a variety of cell activities related with p38 mapk.in a rat adjuvant-induced arthritis model, al8697 exhibited a good anti-inflammatory effect and induced leukocytosis and increased total plasma cholesterol, these properties were evidently at 10 mg/kg. in addition, al8697 partially restored the platelet count. the complex profile for al8697 in rat aia (adjuvant-induced arthritis) is not observed in human ra (rheumatoid arthritis).[1] | [in vivo]
AL 8697 (1-30 mg/kg; p.o.; once daily for 10 days) dose-dependently decreases the oedema in right and left paws[1]. | Animal Model: | Male Wistar rats[1] | | Dosage: | 1, 3, 10, 30 mg/kg | | Administration: | Oral gavage; once daily for 10 days | | Result: | Dose-dependently decreased the oedema in right and left paws, causing a larger improvement in the contralateral un-injected paw. |
| [IC 50]
p38α: 6 nM (IC50); p38β: 82 nM (IC50) | [storage]
Store at -20°C | [References]
[1]. balagué c, pont m, prats n, godessart n. profiling of dihydroorotate dehydrogenase, p38 and jak inhibitors in the rat adjuvant-induced arthritis model: a translational study. br j pharmacol. 2012 jun;166(4):1320-32
[2]. ajizian sj, english bk, meals ea.specific inhibitors of p38 and extracellular signal-regulated kinase mitogen-activated protein kinase pathways block inducible nitric oxide synthase and tumor necrosis factor accumulation in murine macrophages stimulated with lipopolysaccharide and interferon-gamma. j infect dis. 1999 apr;179(4):939-44.
[3]. bao w, behm dj, nerurkar ss, ao z, et al. effects of p38 mapk inhibitor on angiotensin ii-dependent hypertension, organ damage, and superoxide anion production. j cardiovasc pharmacol. 2007 jun;49(6):362-8. |
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cjbscvictory
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