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    Immunology/Inflammation
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  3. Vercirnon sodium

Vercirnon sodium (Synonyms: GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium)

目录号: HY-15724A 纯度: 98.76%
产品使用指南

Vercirnon (GSK-1605786) sodium 是一种具有口服活性的,选择性的 CCR9 拮抗剂。Vercirnon sodium 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 sodium 对 CCR9 的选择性高于 CCR1-12 和 CX3CR1-7 (IC50s=>10 µM)。Vercirnon sodium 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。

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Vercirnon sodium Chemical Structure

Vercirnon sodium Chemical Structure

CAS No. : 886214-18-2

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Description

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium 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[1].

IC50 & Target[3]

CCR9

10 nM (IC50)

In Vitro

Vercirnon (GSK-1605786) sodium inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC50 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 IC50 of 141 nM. Vercirnon sodium is a potent inhibitor of CCL25-induced mouse and rat thymocyte chemotaxis with IC50 values of 6.9 nM and 1.3 nM, respectively[1].

In Vivo

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.
Molecular Weight

466.91

Formula

C₂₂H₂₀ClN₂NaO₄S

CAS No.

886214-18-2

中文名称

维塞诺钠盐

SMILES

O=S(C1=CC=C(C(C)(C)C)C=C1)([N-]C2=CC=C(Cl)C=C2C(C3=CC=[N+]([O-])C=C3)=O)=O.[Na+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1417 mL 10.7087 mL 21.4174 mL
5 mM 0.4283 mL 2.1417 mL 4.2835 mL
10 mM 0.2142 mL 1.0709 mL 2.1417 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 (stored under nitrogen)。 -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    40% PEG300    5% Tween-80    45% saline

    Solubility: 5 mg/mL (10.71 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (10.71 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (10.71 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (10.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
References
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Keywords:

VercirnonGSK-1605786CCX282-BTraficet-ENGSK1605786GSK 1605786CCRCC chemokine receptororalbioavailableinflammatoryboweldiseasechemotaxischemokineInhibitorinhibitorinhibit

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产品名称:
Vercirnon sodium
目录号:
HY-15724A
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