生物活性

AS1810722, a fused bicyclic pyrimidine derivative, is an orally active and potent inhibitor of STAT6, demonstrating an IC50 of 1.9 nM. It exhibits effective inhibition of CYP3A4, positioning it as a promising candidate for research into allergic diseases, including asthma and atopic conditions.

体外研究

AS1810722 (化合物 24) 抑制 IL-4 的产生，IC50 为 2.4 nM，但对 IFN-γ的产生没有影响。

体内研究

1. Please add each solvent in order: 10% DMSO → 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.36 mM);
 Suspension; ultrasonic dissolution aid
This scheme can obtain a uniform suspension of 2.08 mg/mL, which can be used for oral administration and intraperitoneal injection.
Taking 1 mL of working solution as an example, 100 μL of 20.8 mg/mL clear DMSO stock solution is added to 900 μL of 20% SBE-β-CD physiological saline aqueous solution, and mixed evenly.
<1mg/ml indicates slight solubility or insolubility.
Please select the appropriate solvent to prepare the stock solution based on the solubility of the product in different solvents. Once the solution is prepared, please aliquot and store it to avoid product degradation caused by repeated freeze-thaw cycles.

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

1.Novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potent and orally active STAT6 inhibitors.2009 Oct 1;17(19):6926-36.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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