RO0270608

Names

[ CAS No. ]:
220846-33-3

[ Name ]:
RO0270608

[Synonym ]:
(S)-2-(2-Chloro-6-methyl-benzoylamino)-3-[4-(2,6-dichloro-benzoylamino)-phenyl]-propionic acid
4-[[(2,6-dichlorophenyl)carbonyl]amino]-N-[(2-chloro-6-methylphenyl)carbonyl]-L-phenylalanine
(S)-2-(2-chloro-6-methyl-benzoylamino)-3-[4-(2,6-dichloro-benzoylamino)-phenyl]-propionic acid
N-(2-chloro-6-methylbenzoyl)-4-[(2,6-dichlorobenzoyl)amino]-L-phenylalanine

Biological Activity

[Description]:

RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity[1][2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cytoskeleton >> Integrin

[Target]

α4β1

α4β7

[In Vitro]

RO0270608 inhibits α4/β7 mediated cell adhesion with an IC50 of 33 nM. In a human T-cell VCAM/anti CD3 costimulation assay RO0270608 causes a pronounced inhibition of T-cell proliferation (IC50=30 nM)[2].

[In Vivo]

In a murine OVA-model of airway inflammation, RO0270608 i.n. abolishes allergen-induced inflammatory cell accumulation[2]

[References]

[1]. Hijazi Y, et al. Pharmacokinetics, safety, and tolerability of R411, a dual alpha4beta1-alpha4beta7 integrin antagonist after oral administration at single and multiple once-daily ascending doses in healthy volunteers. J Clin Pharmacol. 2004;44(12):1368-1378.

[2]. M. Renzetti, et al. Dual α4/β1–α4/β7 vs α4/β1 selective antagonism is required for attenuation of allergic inflammatory responses. Journal of Allergy and Clinical Immunology. Volume 113, Issue 2, Supplement, February 2004, Page S221.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₁₉Cl₃N₂O₄

[ Molecular Weight ]:
505.77800

[ Exact Mass ]:
504.04100

[ PSA ]:
95.50000

[ LogP ]:
6.09710

Related Compounds

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