r411

Valategrast hydrochloride (R411), a dual antagonist of integrin α4β1 (VLA-4), is used for the potential treatment of asthma.

OICR41114 (PROTAC4) is a PROTAC degrader targeting WDR5. It effectively degrades endogenous WDR5 with an EC50 of 40 nM and a Dmax of 49%. The degradation of HiBiT-tagged WDR5 by OICR41114 occurs in a proteasome-dependent manner. This compound is composed of a target protein ligand, Dimethyl-F-OICR-9429-COOH, an E3 ligase ligand, OICR-8268-acrylic acid, and a PROTAC linker, Amino-PEG9-amine. Notably, the conjugate of the E3 ligase ligand and the linker is OICR-8268-acrylic acid-amino-PEG9-amine.

SSR411298 is a reversible, orally active compound that selectively inhibits fatty acid amide hydrolase (FAAH). Its potential lies in the field of post-traumatic stress disorder (PTSD) research.

RO0270608, the active metabolite of R411, is an orally active dual α4β1 α4β7 integrin antagonist with anti-inflammatory properties, useful for studying allergic inflammatory responses.

RO-02-70608 is the active metabolite of R411. Following a single oral dose escalation of R411, the area under the concentration-time curve for RO-02-70608 increases proportionally from 150 mg to 1200 mg (P > .05).

Valategrast is a potent and orally active dual antagonist of integrin α4β1 (VLA-4) and α4β7, with the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.