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AL 8697 p38α inhibitor,potent and selective

Catalog No.B7784
Size Price Stock Qty
10mg
$316.00
In stock
50mg
$1,327.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AL 8697

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Chemical Properties

Cas No. 1057394-06-5 SDF Download SDF
Chemical Name 3-(3-(tert-butyl)-6,8-difluoro-[1,2,4]triazolo[4,3-a]pyridin-7-yl)-N-cyclopropyl-5-fluoro-4-methylbenzamide
Canonical SMILES FC1=C(C)C(C2=C(F)C3=NN=C(C(C)(C)C)N3C=C2F)=CC(C(NC4CC4)=O)=C1
Formula C21H21F3N4O M.Wt 402.41
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical Appearance White solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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]

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.