1. Cytoskeleton
  2. Integrin
  3. Carotegrast methyl

Carotegrast methyl (Synonyms: AJM300)

Cat. No.: HY-124290 Purity: 99.72%
Handling Instructions

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.

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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Based on 1 publication(s) in Google Scholar

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Description

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 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.
Clinical Trial
Molecular Weight

569.44

Formula

C₂₈H₂₆Cl₂N₄O₅

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

*All of the co-solvents are provided by MCE.
References
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Product Name:
Carotegrast methyl
Cat. No.:
HY-124290
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