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TR-14035 {[allProObj[0].p_purity_real_show]}

货号:A234495 同义名: SB 683698;MDK-1191

TR-14035 is a dual antagonist of both integrin α4β7 and integrin α4β1 with IC50 values of 7 nM and 87 nM, respectively, used as an anti-inflammatory agent.

TR-14035 化学结构 CAS号:232271-19-1
TR-14035 化学结构
CAS号:232271-19-1
TR-14035 3D分子结构
CAS号:232271-19-1
TR-14035 化学结构 CAS号:232271-19-1
TR-14035 3D分子结构 CAS号:232271-19-1
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TR-14035 纯度/质量文件 产品仅供科研

货号:A234495 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Integrin 其他靶点 纯度
Tirofiban 99%+
ATN-161 98%
RGD 98%
A-205804 ++

E-selectin, IC50: 20 nM

ICAM-1, IC50: 25 nM

98%
SB-273005 ++++

αvβ5 receptor, IC50: 0.3 nM

αvβ3 receptor, IC50: 1.2 nM

98+%
Lifitegrast 97%
Cilengitide TFA +++

αvβ5 receptor, IC50: 79 nM

αvβ3 receptor, IC50: 4.1 nM

99%+
Cyclo(-RGDfK) TFA 99%+
Cyclo(RGDyK) trifluoroacetate ++

αVβ3 integrin, IC50: 20 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

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]. It blocks the binding of human α4β7 to an 125I-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 47-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] (p.o.), 10 mg/kg[4] (p.o.); 3 mg/kg[4] (i.v.) Dog: 10 mg/kg[4] (p.o.); 3 mg/kg[4] (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Rats[4] Dogs[4]
Dose 3 mg/kg (i.v.)
10 mg/kg (p.o.)
3 mg/kg (i.v.)
10 mg/kg (p.o.)
Administration i.v.
p.o.
i.v.
p.o.
F 17.1 ± 3.1% (p.o.) 13.2 ± 7.6% (p.o.)
AUCinf 0.78 ± 0.09 μg eq.·h/ml (i.v.)
0.44 ± 0.05 μg eq.·h/ml (p.o.)
1.85 ± 0.37 μg eq.·h/ml (i.v.)
0.76 ± 0.35 μg eq.·h/ml (p.o.)
T1/2 0.28 ± 0.07 h (i.v.)
3.17 ± 0.96 h (p.o.)
0.81 ± 0.38 h (i.v.)
9.54 ± 3.33 h (p.o.)
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.

TR-14035 实验方案

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

CAS号232271-19-1
分子式C24H21Cl2NO5
分子量 474.333
别名 SB 683698;MDK-1191;QJ-2620
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 40 mg/mL(84.33 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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