S23474 |
AS-041164 |
源叶(MedMol) | 98% |
- 产品描述:
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects
- 靶点: PI3Kγ:70 nM (IC50);PI3Kα:240 nM (IC50);PI3Kβ:1.4 μM (IC50);PI3Kδ:1.7 μM (IC50);PI3K
- 体内研究:
AS-041164 (10-100 mg/kg; oral administration; once) treatment results in the reduction of inflammatory swelling in the model of carrageenan-induced paw edema. AS-041164 (3-100 mg/kg p.o.) treatment dose-dependently decreases r-h regulated on activation normal T cell expressed and secreted (RANTES)-induced neutrophil recruitment in mice. The ED50 value for AS-041164 is 27.35 mg/kg. AS-041164 blocks RANTES-induced chemotaxis and reduces the level of AKT phosphorylation. Animal Model: Male Wistar rats (100-150 g) injected with carrageenan Dosage: 10 mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration; once Result: Induced a significant reduction of paw thickness.
- 参考文献:
1. Chiara Ferrandi, et al. Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment. J Pharmacol Exp Ther. 2007 Sep;322(3):923-30.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 4.012 ml 20.061 ml 40.122 ml 5 mM 0.802 ml 4.012 ml 8.024 ml 10 mM 0.401 ml 2.006 ml 4.012 ml 50 mM 0.08 ml 0.401 ml 0.802 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)