1. Cytoskeleton
  2. Integrin
  3. Carotegrast methyl

Carotegrast methyl (Synonyms: AJM300)

Cat. No.: HY-124290
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Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of AJM300, is a specific, dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.

For research use only. We do not sell to patients.

Carotegrast methyl Chemical Structure

Carotegrast methyl Chemical Structure

CAS No. : 401905-67-7

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Description

Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of AJM300, is a specific, dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice[1].

IC50 & Target[1]

α4β1

 

α4β7

 

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[1].

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

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].
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].

MCE 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[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.
Molecular Weight

569.44

Formula

C₂₈H₂₆Cl₂N₄O₅

CAS No.

401905-67-7

SMILES

O=C([[email protected]@H](NC(C1=C(C=CC=C1Cl)Cl)=O)CC2=CC=C(C=C2)N3C(N(C4=C(C3=O)C=C(C=C4)N(C)C)C)=O)OC

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Carotegrast methylAJM300AJM 300AJM-300IntegrinorallyHCA2969colitisJurkatRPMI-8866TK-1Inhibitorinhibitorinhibit

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Carotegrast methyl
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HY-124290
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