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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 60 mg/mL|
|Related Integrin Products|
MK-0429 (L-000845704) is an oral, highly effective, selective, non-peptide integrin ubiquitous antagonist for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1 IC5 0 The values are 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM, and 12.2 nM, respectively.
Zaurategrast (CT7758) is an effective, orally active one α4-integrin depressor.
Pyrintegrin is a beta1 integrin (β1-integrin) agonist and a 2,4-dihydrated pyrimidine that promotes embryonic stem cell survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte protector and has a powerful lipolyogenic effect.
GRGDSP (TFA) is an integrin inhibitor.
Echistatin TFA is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
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