S87221 |
Fostamatinib Disodium Hexahydrate |
| 源叶(MedMol) | 98% |
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- 产品描述： Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate 是活性代谢产物R406的前药，是一种 Syk 的抑制剂，在无细胞分析中的IC50值为41 nM。
- 靶点： Syk(Cell-free assay):41 nM
- 体内研究： Oral administration of R788 to mice reduces immune complex-mediated inflammation in a reverse-passive Arthus reaction and two antibody-induced arthritis models.In another study, R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolongs survival of the treated animals.R788 demonstrates a significant reduction in major inflammatory mediators such as TNFalpha, IL-1, IL-6 and IL-18, leading to reduced inflammation and bone degradation in models of rheumatoid arthritis.
- 细胞实验： Cell lines: Cultured human mast cells (CHMC) Concentrations: 0-100 μM Incubation Time: 0.5 h Method: Cultured human mast cells (CHMC) are derived from cord blood CD34+ progenitor cells and grown, primed, and stimulated and shown in supplemental data. Before stimulation, cells are incubated with R788 or DMSO for 30 minutes. Cells are then stimulated with either 0.25 to 2 mg/mL anti-IgE or anti-IgG or 2 μM ionomycin. For tryptase measurement, ~1500 cells per well are stimulated for 30 min in modified Tyrode's buffer. For LTC4 and cytokine production, 100,000 cells per well are stimulated for 1 or 7 hours, respectively. Tryptase activity is measured by luminescence readout of a peptide substrate, and LTC4 and cytokines are measured using Luminex multiplex technology.
- 动物实验： Animal Models: Balb/c mice with arthritis Dosages: 1 mg/kg or 5 mg/kg Administration: o.g.
- 参考文献：
1. Braselmann S, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. 2. Chen L, et al. Blood. 2008 Feb 15;111(4):2230-7. 3. Suljagic M, et al. Blood. 2010 Dec 2;116(23):4894-905. 4. Bajpai M. et al. IDrugs. 2009 Mar;12(3):174-85. 5. Sylvia Braselmann, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.
- 溶解性： Soluble in DMSO
- 保存条件： 2-8℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.365 ml 6.826 ml 13.652 ml 5 mM 0.273 ml 1.365 ml 2.73 ml 10 mM 0.137 ml 0.683 ml 1.365 ml 50 mM 0.027 ml 0.137 ml 0.273 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
