TR-14035 是一种具有口服活性的 α₄β₇/α₄β₁ 整合素 (α₄β₇/α₄β₁ integrin) 双重抑制剂，对 α₄β₇ 和 α₄β₁ 作用的 IC₅₀ 值分别为 7 nM 和 87 nM。TR-14035 可用于炎症和自体免疫疾病的研究。

TR-14035 is a orally active dual α 4 β 7 /α 4 β 1 integrin antagonist, with IC 50 s of 7 nM and 87 nM for α 4 β 7 and α 4 β 1 , respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.

Solid

α4β7 7 nM (IC50) α4β1 87 nM (IC50u

TR14035 blocks adhesion of RPMI-8866 cells to MAdCAM-Ig by 100% at 1 μM, with an approximate IC50 of 0.01 μM.
has not independently confirmed the accuracy of these methods. They are for reference only.

TR-14035 (3?mg/kg; i.g.) produces a significant decrease of the airways hyper-responsiveness to 5-hydroxytryptamine (5-HT) in an experimental model of allergic asthma in Brown Norway rats.
TR-14035 exhibits moderate oral bioavailability (rat 17.1%, dog 13.2%) and C max (rat 0.18, dog 0.10 μg eq./mL) following oral administration (rat 10 and dog 10 mg/kg).
TR-14035 exhibits terminal elimination half-lives (rat 0.28 h and, dog 0.81 h) due to high plasma clearance (3865 and 1664 mL/h/kg respectively) following intravenous administration (rat 3 mg/kg and dog 3 mg/kg).
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 41 mg/mL (86.44 mM)配制储备液