Vercirnon 维塞诺; GSK-1605786; CCX282-B; Traficet-EN|cas:698394-73-9|西域试剂

Vercirnon 维塞诺; GSK-1605786; CCX282-B; Traficet-EN,98.19%

产品编号：Bellancom-15724| CAS NO：698394-73-9| 分子式：C₂₂H₂₁ClN₂O₄S| 分子量：444.93

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货号	价格	库存与货期
Bellancom-15724	￥2600.00	杭州北京（现货）
Bellancom-15724	￥3950.00	杭州北京（现货）
Bellancom-15724	￥7900.00	杭州北京（现货）
Bellancom-15724	￥12600.00	杭州北京（现货）

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Vercirnon 维塞诺; GSK-1605786; CCX282-B; Traficet-EN

产品介绍

Vercirnon (GSK-1605786) 是一种具有口服活性的，选择性的 CCR9 拮抗剂。Vercirnon 抑制 CCR9 介导的 Molt-4 细胞上 Ca²⁺ 移动和趋化性，IC₅₀ 值分别为 5.4 和 3.4 nM。Vercirnon 对 CCR9 的选择性高于 CCR1-12 和 CX3CR1-7 (IC₅₀s=>10 µM)。Vercirnon 是 CCR9 的两种剪接形式 (CCR9A 和 CCR9B) 的 CCL25 定向趋化性的等效抑制剂，IC₅₀ 值分别为 2.8 和 2.6 nM。

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.

体外研究

Vercirnon (GSK-1605786) inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC₅₀ of 6.8 nM. Vercirnon inhibits CCL25-Induced Chemotaxis of retinoic acid (RA)-Cultured Human T Cells. Vercirnon inhibits RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum resulted in an IC₅₀ of 141 nM. Vercirnon is a potent inhibitor of CCL25-induced mouse and rat thymocyte chemotaxis with IC₅₀ values of 6.9 nM and 1.3 nM, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Vercirnon (GSK-1605786) (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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

Vercirnon (GSK-1605786) (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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 25 mg/mL (56.19 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2475 mL	11.2377 mL	22.4754 mL
5 mM	0.4495 mL	2.2475 mL	4.4951 mL
10 mM	0.2248 mL	1.1238 mL	2.2475 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。