AL 8697
目录号 : GC12646
AL 8697 是一种具有口服活性的特异性 p38α MAPK 抑制剂，IC50 为 6 nM。
Cas No.:1057394-06-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1057394-06-5 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C21H21F3N4O | 分子量 | 402.41 |
| 溶解度 | <40.24mg/ml in DMSO; <20.12mg/ml in ethanol | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.485 mL | 12.4251 mL | 24.8503 mL |
| 5 mM | 0.497 mL | 2.485 mL | 4.9701 mL |
| 10 mM | 0.2485 mL | 1.2425 mL | 2.485 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet