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• 產(chǎn)品描述： 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.

• 靶點： α4β7:7 nM (IC50);α4β1:87 nM (IC50);Integrin

• 體內(nèi)研究：
  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 Cmax (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)

• 參考文獻：
  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

• 溶解性： DMSO  :  ≥  41  mg/mL  (86.44  mM)

• 保存條件： 2-8℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.108 ml	10.541 ml	21.082 ml
  5 mM	0.422 ml	2.108 ml	4.216 ml
  10 mM	0.211 ml	1.054 ml	2.108 ml
  50 mM	0.042 ml	0.211 ml	0.422 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *