| Identification | Back Directory | [Name]
Cositecan | [CAS]
401905-67-7 | [Synonyms]
AJM-300
RPMI-8866,HCA2969,Jurkat,inhibit,TK-1,colitis,AJM-300,Integrin,Inhibitor,Carotegrast methyl,orally,AJM 300
methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-yl]phenyl]propanoate | [Molecular Formula]
C28H26Cl2N4O5 | [MDL Number]
MFCD34167496 | [MOL File]
401905-67-7.mol | [Molecular Weight]
569.44 |
| Chemical Properties | Back Directory | [density ]
1.382±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (175.61 mM; Need ultrasonic) | [form ]
Solid | [pka]
11.51±0.46(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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[1].
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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)[1].
| Animal Model: | Mouse model of colitis induced by adoptive transfer of IL-10 deficient CD4+ T cells[1] | | 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.
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| [References]
[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. DOI:10.1016/j.crohns.2013.03.014 |
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