TR-14035 是一种具有口服活性的 α4β7/α4β1整合素 (α4β7/α4β1integrin) 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。
| 生物活性 | TR-14035 is a orally active dualα4β7/α4β1integrinantagonist, withIC50s of 7 nM and 87 nM for α4β7and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases[1][2]. |
| IC50& Target[1] | α4β7 7 nM (IC50) | α4β1 87 nM (IC50) |
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体外研究
(In Vitro) | TR14035 blocks adhesion of RPMI-8866 cells to MAdCAM-Ig by 100% at 1 μM, with an approximate IC50of 0.01 μM[2].
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体内研究
(In Vivo) | 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[3].
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)[4].
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)[4].
| Animal Model: | Male Brown Norway rats (250-300 g)[3] | | Dosage: | 3 mg/kg | | Administration: | Oral gavage, 1 h before and 3 h after antigen challenge | | Result: | Suppressed antigen-induced airway hyper-responsiveness and inflammation. |
| Animal Model: | Male Sprague-Dawley rats (250-320 g)[4] | | Dosage: | 3 mg/ kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) | | Administration: | Intravenous injection and oral administration | | Result: | Oral bioavailability (17.1%), Cmax(0.18 μg eq./mL), T1/2(0.28 h). |
| Animal Model: | Male beagle dogs[4] | | Dosage: | 3 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis) | | Administration: | Intravenous administration and oral administration | | Result: | Oral bioavailability (13.2%), Cmax( 0.10 μg eq./mL), T1/2(0.81 h). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 41 mg/mL(86.44 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.1082 mL | 10.5412 mL | 21.0824 mL | | 5 mM | 0.4216 mL | 2.1082 mL | 4.2165 mL | | 10 mM | 0.2108 mL | 1.0541 mL | 2.1082 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.27 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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