|4-(3-氯苯基)-1,7-二乙基吡啶并[2,3-d]嘧啶-2(1H)-酮|CsnPharm

CAS No.: 191219-80-4

Synonyms: Ym 976

YM976 is an orally active PDE4 inhibitor (IC50 = 2.2 nM). YM976 has low emetogenic activity, suggested to be due to poor brain penetration.

规格	价格	促销价格	库存	数量

400-920-2911

加入购物车大规格询价

产品咨询

400-920-2911

纯度 & 质量文件批次:

生物活性

描述YM-976 is an anti-inflammatory compound that shows potent inhibitory activity against phosphodiesterase type 4 purified from human peripheral leukocytes with an IC50 of 2.2nM. YM-976 augmented cAMP accumulation-induced prostaglandin E(2) in a human mononuclear cell line, U937. It also inhibited lipopolysaccharide-induced production of tumor necrosis factor-alpha from human peripheral blood mononuclear cells. In a rat model of carrageenan-induced pleurisy, YM-976 inhibited the cell infiltration into the pleural cavity with an oral ED₃₀ value of 9.1mg/kg. No emesis was observed in rats treated with YM-976 at doses up to 10 mg/kg. YM-976 at doses of 1, 3, and 10mg/kg also reduced carrageenan-induced leukocyte infiltration in a concentration-dependent manner^[1]. The evaluation of the effect of YM-976 on antigen-induced eosinophil infiltration into the lungs showed that YM976 inhibited the accumulation of eosinophils at ED₅₀ values of 1.7, 5.8, and 1.2mg/kg in rats, C57Black/6 mice, and ferrets, respectively. In a rat model of eosinophilia induced by repeated antigen exposure, chronic administration with YM-976 demonstrated more potent inhibition (ED₅₀ = 0.32mg/kg) than a single dose (ED₅₀ = 1.4mg/kg)^[2].
参考文献

实验方案

技术信息

CAS号	191219-80-4	储存条件	粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C17H16ClN3O	运输	蓝冰
分子量	313.78	别名	Ym 976

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

请登录您的专属账户