TR-14035

Research use only, not for human use.

A potent, orally bioavailable, dual α4β7/α4β1 integrin antagonist with IC50 of 7/87 nM.

A potent, orally bioavailable, dual α4β7/α4β1 integrin antagonist with IC50 of 7/87 nM; blocks the binding of human α4β7 to an (125)I-MAdCAM-Ig fusion protein with IC50 of 0.75 nM; suppresses antigen-induced lung interleukin (IL)-5 mRNA upregulation, inhibits the leukocyte rolling flux, adhesion and emigration induced by IL4 in rats.Asthma Phase 1 Discontinued.

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Animal Model:Male Brown Norway rats (250-300?g)Dosage:3?mg/kg Administration:Oral gavage, 1?h before and 3?h after antigen challenge Result:Suppressed antigen-induced airway hyper-responsiveness and inflammation. Animal Model:Male Sprague-Dawley rats (250-320 g)Dosage:3 mg/ kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) Administration:Intravenous injection and oral administration Result:Oral bioavailability (17.1%), Cmax (0.18 μg eq./mL), T1/2 (0.28 h).Animal Model:Male beagle dogs Dosage:3 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) Administration:Intravenous administration and oral administration Result:Oral bioavailability (13.2%), Cmax ( 0.10 μg eq./mL), T1/2 (0.81 h).

TR 14035 | TR14035

Cell Cycle/DNA Damage

Integrin

α4β7integrin|α4β1integrin

Inflammation/Immunology

Asthma

232271-19-1

474.3333

C24H21Cl2NO5

>98% (HPLC)

DMSO：≥ 41 mg/mL

O=C(O)[C@H](CC1=CC=C(C2=C(OC)C=CC=C2OC)C=C1)NC(C3=C(Cl)C=CC=C3Cl)=O

[1,1'-Biphenyl]-4-propanoic acid, α-[(2,6-dichlorobenzoyl)amino]-2',6'-dimethoxy-,(αS)-

(-20℃)

With Ice Pack

≥ 2 years