Adriforant hydrochloride ≥98%
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| 包装规格: | 5mg 10mg 50mg 100mg in glass bottle |
| 产品简介: | 一种新型组胺H4受体亲和型拮抗剂(Ki=2.4nM),也是一种H4受体功能性拮抗剂(Ki=1.56 nM)。 |
| 溶解性: | 溶于DMSO(≥ 83.33 mg/mL) |
| 储备液保存: | -80°C, 6 months -20°C, 1 month (sealed storage, away from moisture) |
| 体内实验: | 1、请依序添加每种溶剂: PBS Solubility: 100 mg/mL (269.01 mM); 澄清溶液; 超声助溶 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。 |
| 靶点: | Ki: 2.4 nM (H4R bind); 1.56 nM (H4R func) |
| 体外研究: | Adriforant is tested and observed binding Ki=2.4 nM and functional Ki=1.56 nM for H4R. Data from functional assays produce convergent projections of the free plasma efficacious concentration and Adriforant (Compound 13) is fast on/fast off on rhH4R. The in vitro IC50 on human native isolated eosinophils assessing actin polymerisation is 1.16 nM and assuming need 10 times the IC50 for >90% receptor occupancy (and therefore near complete inhibition of the response) suggested a concentration of 12 nM. The data in the whole blood GAFS assay demonstrates that the imetit induced shape change is completely blocked at a total blood concentration of 30 nM (which correcting for PPB and blood partitioning equates to approximately 10 nM free). For the purpose of dose projection and safety margin calculation, a Ceff/Cmin concentration of 10-15 nM is used. |
| 保存条件: | -20℃ |
| 注意事项: | 1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。 |
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