| AL 8697p38α inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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| 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 | <40.24mg l="" in="" dmso;=""><20.12mg l="" in="" ethanol=""> | 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. | ||
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.
