貨號	規格	價格	上海	北京	武漢	南京
S84570-2mg	99.4%	￥100.00 S84570-2mg ￥100.00 現貨	5 5	-	-	-
S84570-5mg	99.4%	￥160.00 S84570-5mg ￥160.00 現貨	6 6	-	-	-
S84570-10mg	99.4%	￥260.00 S84570-10mg ￥260.00 現貨	6 6	-	-	-
S84570-50mg	99.4%	￥760.00 S84570-50mg ￥760.00 現貨	3 3	-	-	-
S84570-100mg	≥95%	￥1300.00 S84570-100mg ￥1300.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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.

產品描述：

靶點：

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

體內研究：

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：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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TR-14035

(S)-2-(2,6-Dichlorobenzamido)-3-(2',6'-dimethoxy-[1,1'-biphenyl]-4-yl)propanoic acid