Carotegrast methyl AJM300,98.89%

产品编号:Bellancom-124290| CAS NO:401905-67-7| 分子式:C28H26Cl2N4O5| 分子量:569.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-124290
2500.00 杭州 北京(现货)
Bellancom-124290
4500.00 杭州 北京(现货)
Bellancom-124290
8500.00 杭州 北京(现货)
Bellancom-124290
13500.00 杭州 北京(现货)
Bellancom-124290
19500.00 杭州 北京(现货)

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Carotegrast methyl AJM300

产品介绍 Carotegrast methyl (AJM300) 是一种口服有效和选择性 α4 整联蛋白 (α4 integrin) 拮抗剂。HCA2969 是 Carotegrast methyl 的活性代谢产物,是一种特异的双重 α4β1/α4β7 整联蛋白拮抗剂。Carotegrast methyl 可预防小鼠结肠炎。
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.

体外研究

HCA2969 inhibits human α4β1 integrin (KD=0.32 nM; IC50=5.8 nM), human α4β7 integrin (KD=0.46 nM; IC50=1.4 nM) and mouse α4β7 integrin (KD=0.2 nM; IC50=26 nM) in Jurkat, RPMI-8866 and TK-1 cell lines.

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

体内研究

Carotegrast methyl (AJM300; oral; 0.03-1%; for 15 days) prevents the development of colitis induced by transfer of IL-10 deficient CD4+ T cells in mice.
Carotegrast methyl (oral; 0.3, 3, 30, or 30 mg/kg; a single oral) inhibits Lymphocyte homing to Peyer's patches and increases peripheral lymphocyte counts in a dose-dependent manner in BALB/c mice (8 weeks of age, female).

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

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.
体内研究

Carotegrast methyl (AJM300; oral; 0.03-1%; for 15 days) prevents the development of colitis induced by transfer of IL-10 deficient CD4+ T cells in mice.
Carotegrast methyl (oral; 0.3, 3, 30, or 30 mg/kg; a single oral) inhibits Lymphocyte homing to Peyer's patches and increases peripheral lymphocyte counts in a dose-dependent manner in BALB/c mice (8 weeks of age, female).

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

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.
性状Solid
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (175.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7561 mL 8.7806 mL 17.5611 mL
5 mM 0.3512 mL 1.7561 mL 3.5122 mL
10 mM 0.1756 mL 0.8781 mL 1.7561 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    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.25 mg/mL (2.20 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (2.20 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 12.5 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: 1.25 mg/mL (2.20 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (2.20 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 12.5 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 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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