220846-33-3

220846-33-3 structure

Name: RO0270608
Chemical Name: Ro 0270608
CAS Number: 220846-33-3
Molecular Formula: C₂₄H₁₉Cl₃N₂O₄
Molecular Weight: 505.77800
Catalog: Signaling Pathways Cytoskeleton Integrin
Create Date: 2018-02-20 23:40:01
Modify Date: 2024-01-10 12:34:38
RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity[1][2].

Name	Ro 0270608
Synonyms	(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

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.