Bioactivity | Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment[1][2]. |
Target | Integrin α4β1; Integrin α4β7 |
Invitro | Valategrast contains a common l-phenylalanine-N-aroyl motif where the carboxylic acid is responsible for binding to the metal ion in the metal-ion-dependent adhesion site (MIDAS)[2]. |
Name | Valategrast |
CAS | 220847-86-9 |
Formula | C30H32Cl3N3O4 |
Molar Mass | 604.95 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -80°C, stored under nitrogen |
Reference | [1]. Woodside DG, et al. Cell adhesion antagonists: therapeutic potential in asthma and chronic obstructive pulmonary disease. BioDrugs. 2008;22(2):85-100. [2]. Halland N, et al. Small Macrocycles As Highly Active Integrin α2β1 Antagonists. ACS Med Chem Lett. 2014 Jan 10;5(2):193-8. |