产品
编 号:F348870
分子式:C28H26Cl2N4O5
分子量:569.44
产品类型
结构图
CAS No: 401905-67-7
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产品详情
生物活性:
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
体内研究:
Carotegrastmethyl(AJM300;口服;0.03-1%;持续 15 天)可预防小鼠体内因 IL-10 缺陷型 CD4+ T 细胞转移而诱发的结肠炎。 Carotegrastmethyl(口服;0.3、3、30 或 30 mg/kg;单次口服)可抑制 BALB/c 小鼠(8 周龄,雌性)淋巴细胞归巢至派尔氏淋巴结,并以剂量??依赖性方式增加外周淋巴细胞计数)。 Animal Model:Mouse model of colitis induced by adoptive transfer of IL-10 deficient CD4+ T cells
Dosage:Diet; 0.03, 0.1, 0.3 or 1%
Administration:For 15 days
Result:Had a histological improvement in epithelial cell hyperplasia, reduced inflammatory cell infiltration and a decrease in mucus production.Prevented an increase in the colon weight in a model of colitis induced by adoptive transfer of CD4+CD45RBhigh T cells.
体外研究:
HCA2969 抑制人 α4β1 整合素 (KD=0.32 nM;IC50=5.8 nM),人 α4β7 整合素 (KD=0.46 nM;IC50=1.4 nM) 和小鼠 α4β7 整合素 (KD=0.2 nM;IC50=26 nM) 在 Jurkat,RPMI-8866和 TK-1 细胞系。