α4β1 Antagonist

TR-14035 is a orally active dual α₄β₇/α₄β₁ integrin antagonist, with IC₅₀ s of 7 nM and 87 nM for α₄β₇ and α₄β₁, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.

GW559090 is a selective, competitive, and high-affinity α4 integrin antagonist with a K_d of 0.19 nM for α4β1. GW559090 can effectively block the binding of α4β1 to vascular cell adhesion molecule 1 (VCAM-1) and fibronectin with IC₅₀ values of 7.72 and 8.04 nM. GW559090 also inhibits the interaction between α4β7 and mucosal addressin cell adhesion molecule 1 (MAdCAM-1) (IC₅₀ = 23 nM). GW559090 can inhibit inflammatory infiltration in the eyes, repair the corneal barrier and restore the function of goblet cells. GW559090 can be used for research of Sjögren's syndrome associated dry eye.

RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity.

α₄β₁ antagonist-1 (Compound 4) is a highly selective α₄β₁ integrin antagonist (IC₅₀=15 nM). α4β1 antagonist-1 inhibits integrin-mediated cell adhesion and ERK1/2 signaling activation. α₄β₁ antagonist-1 also exhibits partial agonism toward α_Mβ₂ integrin (EC₅₀=23 nM). α₄β₁ antagonist-1 is promising for research of chronic inflammatory diseases (e.g., rheumatoid arthritis, multiple sclerosis) and cancers.

TBC-4746 is a α4β1/α4β7 integrin antagonist. TBC-4746 can be used in the research of asthma and multiple sclerosis.

Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a K_i of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).

CP-664511 is an orally active and potent α4β1 integrin antagonist with anti-inflammatory effects (IC₅₀=0.52 nM). CP-664511 inhibits the interaction between α4β1 and vascular cell adhesion molecule-1 (VCAM-1), significantly reducing eosinophil infiltration into lung tissue. CP-664511 is promising for research of asthma and allergic airway diseases.

IVL 745 (XRP 1745A) is a very late antigen 4 (VLA-4, integrin α4β1) antagonist. IVL 745 reduces the airway inflammatory response of sensitized rats and sheep. IVL 745 can be used for airway inflammation and asthma research.

Valategrast hydrochloride (R-411) is a potent integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast hydrochloride has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.