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CAS No.: 906805-42-3

SCH 546738 Catalog No. CSN13174

Synonyms: Sch-546738

SCH 546738 is a potent and non-competitive small molecule CXCR3 antagonist with Ki of 0.4 nM .

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实验方案

技术信息

生物活性

描述CXCR3 is a seven-transmembrane G-protein coupled chemokine receptor involved in multiple immunological and inflammatory responses. SCH-546738 is a selective, potent, and non-competitive CXCR3 antagonist that binds to human CXCR3 with a K_i value of 0.4nM. SCH-546738 prevented CXCL10 and CXCL11 from binding to human CXCR3 with IC50 values ranging from 0.8 to 2.2nM independent of the input concentrations. The IC50 values of SCH-546738 on the binding of [¹²⁵hCXCL10 to the CXCR3 of human, monkey, dog, mouse and rat origin were 0.8, 1.3, 6.4, 5.9, and 4.2nM, respectively. SCH-546738 at 1–100nM inhibited human activated T cell chemotaxis induced by three CXCR3 ligands (CXCL9, CXCL10 and CXCL11). SCH-546738 at the concentration of 10 nM inhibited CXCR3 ligands-induced T cell chemotaxis by about 90%. In a mouse model of collagen-induced arthritis, oral administration of SCH-546738 at 40mpk (twice daily) significantly reduced the disease score on days 4, 7, and 9, and SCH-546738 administered at 10mpk showed protective activity against disease development on days 7 and 9. Compared with the vehicle-treated group, mice received 40mpk SCH-546738 displayed significantly attenuated leukocyte infiltration into the joint and alleviated structural damage to the bone and cartilage^[3].
作用机制SCH 546738 binds to an allosteric site of CXCR3 and changes its conformation, thereby inhibiting the binding of both CXCL10 and CXCL11 to CXCR3.
参考文献

[1] Zhang X, Han J, et al. CXC chemokine receptor 3 promotes steatohepatitis in mice through mediating inflammatory cytokines, macrophages and autophagy. J Hepatol. 2016 Jan;64(1):160-70.
[2] Jenh CH, Cox MA, et al. A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection. BMC Immunol. 2012 Jan 10;13:2.
[3] Jenh CH, Cox MA, Cui L, Reich EP, Sullivan L, Chen SC, Kinsley D, Qian S, Kim SH, Rosenblum S, Kozlowski J, Fine JS, Zavodny PJ, Lundell D. A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection. BMC Immunol. 2012 Jan 10;13:2. doi: 10.1186/1471-2172-13-2. PMID: 22233170; PMCID: PMC3298469.

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
- 2.0307 mL
- 10.1534 mL
- 20.3069 mL
- 5 mM
- 0.4061 mL
- 2.0307 mL
- 4.0614 mL
- 10 mM
- 0.2031 mL
- 1.0153 mL
- 2.0307 mL

技术信息

CAS号

906805-42-3

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H31Cl2N7O

运输

蓝冰

分子量

492.44

别名

Sch-546738

溶解度

DMSO	4.0 mg/mL (8.1 mM) warming
Water	Insoluble

动物实验配方

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