TR-14035
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货号：A234495
同义名：
SB 683698;MDK-1191
TR-14035 是一种 α4β7 和 α4β1 整合素双重拮抗剂，其 IC50 值分别为 7 nM 和 87 nM，用作抗炎剂。
TR-14035 化学结构
TR-14035 3D分子结构
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TR-14035 纯度/质量文件 产品仅供科研
货号：A234495
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TR-14035 质控信息
TR-14035 生物活性
描述
The integrins α4β1 and α4β7 are heterodimeric cell surface proteins that regulate the physiologic and pathologic responses in inflammation and autoimmune diseases. TR-14035 is a dual antagonist of both α4β1 and α4β7 with IC50 values of 87 nM and 7 nM, respectively[5] 125 I-hMAd-CAM-Ig fusion protein with an IC50 value of 0.75 nM. In RPMI-8866 cells expressing human α4β7, TR-14035 at 1 μM blocked the adhesion of cells to MAdCAM-Ig by 100% with an IC50 value of 0.01 μM. In murine 47-expressing cells, TR-14035 at the dose of 1 μM inhibited the adhesion of cells to murine MAdCAM-Ig by 78% with an IC50 value of 0.1 μM. When tested for the ability to block the adhesion of murine MLN lymphocytes to Peyer’s patch HEVs under shear flow in vivo , intravenous administration of TR-14035 (10mpk) blocked the binding of MLN lymphocytes to Peyer’s patch HEVs by 95% when MLN lymphocytes were pretreated with 100 μM TR-14035 for 10min, and by 88% without the preincubation[6]
TR-14035 动物研究
Dose
Rat: 3 mg/kg[3] [4] [4] [4] [4]
Administration
p.o., i.v.
Pharmacokinetics
Animal
Rats[4]
Dogs[4]
Dose
3 mg/kg (i.v.)
3 mg/kg (i.v.)
Administration
i.v.
i.v.
F
17.1 ± 3.1% (p.o.)
13.2 ± 7.6% (p.o.)
AUCinf
0.78 ± 0.09 μg eq.·h/ml (i.v.)
1.85 ± 0.37 μg eq.·h/ml (i.v.)
T1/2
0.28 ± 0.07 h (i.v.)
0.81 ± 0.38 h (i.v.)
Tmax
0.39 ± 0.19 h (p.o.)
0.67 ± 0.29 h (p.o.)
CLtot
3865 ± 459 ml/h/kg (i.v.)
1664 ± 300 ml/h/kg (i.v.)
Cmax
0.18 ± 0.01 μg eq./ml (p.o.)
0.10 ± 0.01 μg eq./ml (p.o.)
Vdss
767 ± 133 ml/kg (i.v.)
521 ± 327 ml/kg (i.v.)
TR-14035 参考文献
[1] Egger LA, Kidambi U, 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.
[2] Sircar I, Gudmundsson KS, 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.
[3] Cortijo J, Sanz MJ, et al. A small molecule, orally active, alpha4beta1/alpha4beta7 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):661-70.
[4] Tsuda-Tsukimoto M, Ogasawara Y, et al. Pharmacokinetics and metabolism of TR-14035, a novel antagonist of a4ss1/a4ss7 integrin mediated cell adhesion, in rat and dog. Xenobiotica. 2005 Apr;35(4):373-89.
[5] Sircar I, Gudmundsson KS, Martin R, Liang J, Nomura S, Jayakumar H, Teegarden BR, Nowlin DM, Cardarelli PM, Mah JR, Connell S, Griffith RC, Lazarides E. 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. doi: 10.1016/s0968-0896(02)00021-4. PMID: 11937364.
[6] Egger LA, Kidambi U, Cao J, Van Riper G, McCauley E, Mumford RA, Amo S, Lingham R, Lanza T, Lin LS, De Laszlo SE, Young DN, Kopka IE, Tong S, Pikounis B, Benson E, Warwood S, Bargatze RF, Hagmann WK, Schmidt JA, Detmers PA. 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. doi: 10.1124/jpet.302.1.153. Erratum in: J Pharmacol Exp Ther. 2003 May;305(2):796. PMID: 12065712.
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TR-14035 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.11mL
0.42mL
0.21mL
10.54mL
2.11mL
1.05mL
21.08mL
4.22mL
2.11mL
TR-14035 技术信息
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