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AS1810722 Sale

目录号 : GC61574

AS1810722是口服有效的STAT6抑制剂,IC50为1.9nM。AS1810722显示出良好的CYP3A4抑制作用。AS1810722是一种稠合双环嘧啶衍生物,具有用于过敏性疾病,例如哮喘和特应性疾病研究的潜力。

AS1810722 Chemical Structure

Cas No.:909561-15-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,835.00
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5 mg
¥2,700.00
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10 mg
¥4,320.00
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25 mg
¥8,550.00
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50 mg
¥13,050.00
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100 mg
¥20,250.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 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[1].

AS1810722 (compound 24) inhibits production of IL-4 with an IC50 of 2.4 nM, but shows no effect on production of IFN-γ[1].

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[1]. AS1810722 inhibits in vitro Th2 differentiation with an IC50 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[1]. Animal Model: Female Balb/c mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel[1]

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

Chemical Properties

Cas No. 909561-15-5 SDF
Canonical SMILES O=C(N)CN1CCN(C2=CC=C(NC3=NC=C4C(N(CC5=CC(F)=CC(F)=C5)C=C4)=N3)C=C2)CC1
分子式 C25H25F2N7O 分子量 477.51
溶解度 DMSO: 62.5 mg/mL (130.89 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.0942 mL 10.471 mL 20.942 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 mL
10 mM 0.2094 mL 1.0471 mL 2.0942 mL
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Research Update

Novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potent and orally active STAT6 inhibitors

Bioorg Med Chem 2009 Oct 1;17(19):6926-36.PMID:19747833DOI:10.1016/j.bmc.2009.08.021

Signal transducers and activators of transcription 6 (STAT6) is an important transcription factor in interleukin (IL)-4 signaling pathway and a key regulator of the type 2 helper T (Th2) cell immune response. Therefore, STAT6 may be an excellent therapeutic target for allergic conditions, including asthma and atopic diseases. Previously, we reported 4-aminopyrimidine-5-carboxamide derivatives as STAT6 inhibitors. To search for novel STAT6 inhibitors, we synthesized fused bicyclic pyrimidine derivatives and identified a 7H-pyrrolo[2,3-d]pyrimidine derivative as a STAT6 inhibitor. Optimization of the pyrrolopyrimidine derivatives led to identification of 2-[4-(4-{[7-(3,5-difluorobenzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino}phenyl)piperazin-1-yl]acetamide (24, AS1810722) which showed potent STAT6 inhibition and a good CYP3A4 inhibition profile. Compound 24 also inhibited in vitro Th2 differentiation without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration.