Carotegrast methyl|401905-67-7|-陌孚医药/Medlife

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Carotegrast methyl

目录号: PL14865 纯度: ≥99%

CAS No. :401905-67-7

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中文名称	Carotegrast methyl
中文别名	methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-yl]phenyl]propanoate
英文名称	Carotegrast methyl
英文别名	Carotegrast methyl;OYK17DYO9M;(2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-(1-methyl-2,4-dioxoquinazolin-3-yl)phenyl]propanoic acid;methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-yl]phenyl]propanoate;AJM300;yl]phenyl]propanoate;Carotegrast methyl (JAN);GTPL10510;D09799;(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-;Q27285918;Methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-;L-Phenylalanin;Methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-
Cas No.	401905-67-7
分子式	C₂₈H₂₆Cl₂N₄O₅
分子量	569.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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.

性状

Solid

体外研究(In Vitro)

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

体内研究(In Vivo)

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 Peyers patches and increases peripheral lymphocyte counts in a dose-dependent manner in BALB/c mice (8 weeks of age, female).
has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Toshihiko Sugiura, et al. Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice. J Crohns Colitis. 2013 Dec;7(11):e533-42.

溶解度数据	In Vitro: DMSO : 100 mg/mL (175.61 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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