TR-14035

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[1][2].

Product Specifications

CAS Number

[232271-19-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Integrin

Type

Reference compound

Related Pathways

Cytoskeleton

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/TR-14035.html

Purity

99.87

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

COC1=C(C2=CC=C(C[C@@H](C(O)=O)NC(C3=C(Cl)C=CC=C3Cl)=O)C=C2)C(OC)=CC=C1

Molecular Formula

C24H21Cl2NO5

Molecular Weight

474.33

Precautions

H302, H315, H319, H335

References & Citations

[1]Sircar I, et al. Synthesis and SAR of N-benzoyl-L-biphenylalanine derivatives: discovery of TR-14035, a dual alpha (4) beta (7) /alpha (4) beta (1) integrin antagonist. Bioorg Med Chem. 2002 Jun;10 (6) :2051-66.|[2]Egger LA, et al. Alpha (4) beta (7) /alpha (4) beta (1) dual integrin antagonists block alpha (4) beta (7) -dependent adhesion under shear flow. J Pharmacol Exp Ther. 2002 Jul;302 (1) :153-62.|[3]Julio Cortijo, et al. A small molecule, orally active, α4β1/α4β7 dual antagonist reduces leukocyte infiltration and airway hyper-responsiveness in an experimental model of allergic asthma in Brown Norway rats. Br J Pharmacol. 2006 Mar; 147 (6) : 661–670.|[4]M Tsuda-Tsukimoto, et al. Pharmacokinetics and metabolism of TR-14035, a novel antagonist of a4ss1/a4ss7 integrin mediated cell adhesion, in rat and dog. Xenobiotica