产品
编 号：F430044
分子式：C22H21ClN2O4S
分子量：444.93
分子式：C22H21ClN2O4S
分子量：444.93
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 698394-73-9
产品详情
生物活性：
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
体内研究：
Vercirnon (GSK-1605786) (10、50 mg/kg；sc；每天两次；从 2 周龄开始至 12 周龄) 改善 TNFΔARE 小鼠模型中肠道炎症的严重程度。Animal Model:C57BL/6 mice (TNFΔARE Mouse Model of Terminal Ileitis)
Dosage:10, 50 mg/kg
Administration:Subcutaneous; twice per day; starting at 2 weeks of age until 12 weeks of age
Result:Resulted in complete protection from the severe inflammation associated with TNF- overexpression at 50 mg/kg. A similar protective effect was also noted with a lower dose.
体外研究：
Vercirnon (GSK-1605786) 抑制表达 CCR9 的原代细胞向 CCL25 趋化，IC50 为 6.8 nM。Vercirnon 抑制 CCL25 诱导的视黄酸 (RA) 培养人 T 细胞的趋化性。Vercirnon 在 100% 人 AB 血清中抑制 RA 培养细胞 CCL25 介导的趋化性，IC50 为 141 nM。Vercirnon 是一种有效的 CCL25 诱导的小鼠和大鼠胸腺细胞趋化性抑制剂，IC50 值分别为 6.9 nM 和 1.3 nM。
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
体内研究：
Vercirnon (GSK-1605786) (10、50 mg/kg；sc；每天两次；从 2 周龄开始至 12 周龄) 改善 TNFΔARE 小鼠模型中肠道炎症的严重程度。Animal Model:C57BL/6 mice (TNFΔARE Mouse Model of Terminal Ileitis)
Dosage:10, 50 mg/kg
Administration:Subcutaneous; twice per day; starting at 2 weeks of age until 12 weeks of age
Result:Resulted in complete protection from the severe inflammation associated with TNF- overexpression at 50 mg/kg. A similar protective effect was also noted with a lower dose.
体外研究：
Vercirnon (GSK-1605786) 抑制表达 CCR9 的原代细胞向 CCL25 趋化，IC50 为 6.8 nM。Vercirnon 抑制 CCL25 诱导的视黄酸 (RA) 培养人 T 细胞的趋化性。Vercirnon 在 100% 人 AB 血清中抑制 RA 培养细胞 CCL25 介导的趋化性，IC50 为 141 nM。Vercirnon 是一种有效的 CCL25 诱导的小鼠和大鼠胸腺细胞趋化性抑制剂，IC50 值分别为 6.9 nM 和 1.3 nM。
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