Integrin α2β1 Inhibitor
BTT 3033 (1) is a selective inhibitor of integrin α2β1 with EC50 = 130 nM on the basis of binding for the integrin to collagen I.1) On the other hand, 1 does not inhibit other integrins like α3β1, α4β1, α5β1 and αvβ1, as shown in Table 1.
1 also has anti-inflammatory effects in a platelet-activating factor (PAF)-stimulated air pouch model and moderate anti-inflammatory effects in an arachidonic acid-induced ear edema model.2)
- 1) Novel α2β1 Integrin Inhibitors Reveal That Integrin Binding to Collagen under Shear Stress Conditions Does Not Require Receptor Preactivation
- 2) Sulfonamide inhibitors of α2β1 integrin reveal the essential role of collagen receptors in in vivo models of inflammation
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