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AS1810722

    级别和纯度:
  • ≥98%
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货号 (SKU) 包装规格 是否现货 价格 数量
A647253-1mg
1mg 期货 Stock Image
A647253-5mg
5mg 期货 Stock Image
A647253-10mg
10mg 期货 Stock Image
A647253-25mg
25mg 期货 Stock Image
A647253-50mg
50mg 期货 Stock Image
A647253-100mg
100mg 期货 Stock Image

基本描述

规格或纯度 ≥98%
英文名称 AS1810722
生化机理 AS1810722 是一种具有口服活性的强效 STAT6 抑制剂,IC 50 为 1.9 nM。AS1810722 对 CYP3A4 有良好的抑制作用。AS1810722 是融合双环嘧啶的衍生物,具有治疗过敏性疾病(如哮喘和特应性哮喘)的潜力。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


AS1810722 is an orally active and potent STAT6 inhibitor with an IC 50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research

In Vitro

AS1810722 (compound 24) inhibits production of IL-4 with an IC 50 of 2.4 nM, but shows no effect on production of IFN-γ. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AS1810722 (compound 24; 0.03-0.3 mg/kg; orally; 30 min before, and 24h and 48 h after OVA exposure) suppress eosinophil infiltration in the lung in a dose-dependent manner in an antigen-induced mouse asthmatic model . AS1810722 inhibits in vitro Th2 differentiation with an IC 50 of 2.4 nM without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Balb/c mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel Dosage: 0.03-0.3 mg/kg Administration: Orally; 30 min before, and 24 and 48 h after OVA exposure Result: Suppressed eosinophil infiltration in the lung in a dose-dependent manner.

Form:Solid

IC50& Target:STAT6 1.9 nM (IC 50 ) CYP3A4

纯度 ≥98%

关联靶点(人)

STAT6 Tchem 信号转导和转录激活因子 6(Signal transducer and activator of transcription 6) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IIUPAC Name 2-[4-[4-[[7-[(3,5-difluorophenyl)methyl]pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]acetamide
INCHI 1S/C25H25F2N7O/c26-19-11-17(12-20(27)13-19)15-34-6-5-18-14-29-25(31-24(18)34)30-21-1-3-22(4-2-21)33-9-7-32(8-10-33)16-23(28)35/h1-6,11-14H,7-10,15-16H2,(H2,28,35)(H,29,30,31)
InChi Key IJFRMEXSGYTWGY-UHFFFAOYSA-N
Smiles C1CN(CCN1CC(=O)N)C2=CC=C(C=C2)NC3=NC=C4C=CN(C4=N3)CC5=CC(=CC(=C5)F)F
Isomeric SMILES C1CN(CCN1CC(=O)N)C2=CC=C(C=C2)NC3=NC=C4C=CN(C4=N3)CC5=CC(=CC(=C5)F)F
PubChem CID 44208030
分子量 477.51

化学和物理性质

溶解性 DMSO : 62.5 mg/mL (130.89 mM; Need ultrasonic)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器