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Vercirnon sodium

产品编号 T41016 CAS 886214-18-2

别名: GSK-1605786 sodium, CCX282-Bsodium, 维塞诺钠盐, Traficet-ENsodium

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9 . Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC 50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC 50 s<10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC 50 values of 2.8 and 2.6 nM, respectively.

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Vercirnon sodium, CAS 886214-18-2

规格	价格/CNY	货期
2 mg	￥ 1,950	5日内发货
5 mg	￥ 2,890	5日内发货
25 mg	￥ 9,540	6-8周
50 mg	￥ 12,400	6-8周
100 mg	￥ 17,400	6-8周
1 mL * 10 mM (in DMSO)	￥ 3,580	5日内发货

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Vercirnon sodium 的其他形式现货产品:

Vercirnon

其他形式的 Vercirnon sodium:

Vercirnon
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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent CCR9 antagonist. It effectively inhibits CCR9-mediated calcium mobilization and chemotaxis in Molt-4 cells, exhibiting IC50 values of 5.4 nM and 3.4 nM, respectively. Demonstrating high selectivity, Vercirnon sodium does not significantly affect CCR1-12 or CX3CR1-7, with IC50 values exceeding 10 µM for these receptors. Additionally, it inhibits CCL25-directed chemotaxis equally well in both CCR9 splice variants, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively.
靶点活性	CCR9:10 nM (IC50)
体外活性	Vercirnon (GSK-1605786) sodium inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC 50 of 6.8 nM. Vercirnon sodium inhibits CCL25-Induced Chemotaxis of retinoic acid (RA)-Cultured Human T Cells. Vercirnon sodium inhibits RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum resulted in an IC 50 of 141 nM. Vercirnon sodium is a potent inhibitor of CCL25-induced mouse and rat thymocyte chemotaxis with IC 50 values of 6.9 nM and 1.3 nM, respectively[1].
体内活性	Vercirnon (GSK1605786A) sodium (10, 50 mg/kg; s.c.; twice per day; starting at 2 weeks of age until 12 weeks of age) ameliorates the severity of intestinal inflammation in the TNFΔARE mouse model[1]. Animal Model: C57BL/6 mice (TNFΔARE Mouse Model of Terminal Ileitis)[1]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.

别名	GSK-1605786 sodium, CCX282-Bsodium, 维塞诺钠盐, Traficet-ENsodium
分子量	467.92
分子式	C22H21ClN2NaO4S
CAS No.	886214-18-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Walters MJ, et al. Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine receptor, for treatment of inflammatory bowel disease. J Pharmacol Exp Ther. 2010 Oct;335(1):61-9. 2. Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340. 3. Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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