Carotegrast Methyl (AJM300) is an orally effective and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast Methyl, is a specific dual α4β1/α4β7 integrin antagonist. Carotegrast Methyl prevents colitis in mice.
| Molecular Weight | 569.44 |
| Formula | C28H26Cl2N4O5 |
| CAS Number | 401905-67-7 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Sohita Dhillon. Drugs. Carotegrast Methyl: First Approval
| Related Integrin Products |
|---|
| HSDVHK-NH2
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM). |
| LDV
LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC. |
| Cyclo(RADfK)
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis. |
| Obtustatin
Obtustatin is a non-RGD disintegrin of 41 residues. |
| Integrin Binding Peptide
Integrin Binding Peptide is derived by fibronectin. |
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