232271-19-1|TR-14035|CsnPharm

CAS No.: 232271-19-1

TR-14035 Catalog No. CSN13433

Synonyms: SB 683698;MDK-1191;QJ-2620

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.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Integrin α4β7

IC50:7nM Integrin α4β1

IC50:87nM
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].

动物研究

剂量

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.)

给药途径

p.o., i.v.

动物药代数据

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.)
AUC_inf	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.)
T_1/2	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.)
T_max	0.39 ± 0.19 h (p.o.)	0.67 ± 0.29 h (p.o.)
CL_tot	3865 ± 459 ml/h/kg (i.v.)	1664 ± 300 ml/h/kg (i.v.)
C_max	0.18 ± 0.01 μg eq./ml (p.o.)	0.10 ± 0.01 μg eq./ml (p.o.)
Vd_ss	767 ± 133 ml/kg (i.v.)	521 ± 327 ml/kg (i.v.)

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1082 mL
- 10.5411 mL
- 21.0822 mL
- 5 mM
- 0.4216 mL
- 2.1082 mL
- 4.2164 mL
- 10 mM
- 0.2108 mL
- 1.0541 mL
- 2.1082 mL

技术信息

CAS号

232271-19-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H21Cl2NO5

运输

蓝冰

分子量

474.33

别名

SB 683698;MDK-1191;QJ-2620

溶解度

DMSO	95.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	20.0 mg/mL (42.2 mM)

动物实验配方

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靶点	Description	IC50
Integrin α4β7		IC50:7nM
Integrin α4β1		IC50:87nM

TR-14035 Catalog No. CSN13433

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