美杏高德-药明康德IPP实验海报

i-Pipette自动化工作站是小型多功能液体处理平台的理想之选，满足基于移液功能需求，无需过多编程培训。作为美杏高德的经典产品，i-Pipette历经十几年的市场验证，已获得辉瑞、诺华、阿斯利康、药明康德、清华大学等制药公司、CRO和科研机构的认可。

特征和优势

1. 高性能移液工作站-个性化配置满足您的应用需求；
2. 程序化逐列梯度稀释（8道/16道）；
3. 控制界面简单友好, iPod/iPad 远程控制；
4. 相比手持移液器，速度提升超过8倍；
5. 自动升降台面，可满足自动化编程；
6. 1/2台面可供选择，根据需要选择最佳配置；
7. iPP移液工作站、锁头和EZ-Load吸头三合一，密封良好，保证最佳实验结果；
8. 锁头更换仅需数秒，无需辅助，快捷更换吸头；
9. 适用于符合SBS标准的24/96/384等孔板，进行移液操作；
10. 体积小巧、节省空间，适用于通风橱、生物安全柜。

以下为有关i-Pipette移液工作站与药明康德实验的Poster，请参考：

• MDR1-MDCK cells: Madin Darby canine kidney (MDCK) cells transfect with the MDR1 gene, the gene encoding for the efflux protein, P-gp.

• The MDR1-MDCK permeability assay is an In Vitro Model for Identifying Whether a Drug is a P-gp Substrate, Inhibitor and/or inducer

• Using MDR1-MDCK cells avoids the complexities of multiple transporters by focusing specifically on P-gp, one of the most well recognized efflux transporters in many tissues including the brain, kidney and intestine.

Methodology

By assessing the transport in both the apical to basolateral and basolateral to apical direction an efflux ratio can be calculated which indicates if the compound is a substrate of P-gp.

dCr : The amount of compound in receiver well 
dt   : The incubation time (in second)
Vr    : The volume of the receiver compartment in mL
A   : The area of insert membrane (cm2)
C0    : The concentration of the dosing solution    
       

     Efflux Ratio = Papp (BA) / Papp (AB)

Control makers: High permeability marker : Propranolol
                             low permeability marker: Atenolol 
                             P-glycoprotein substrate: Digoxin
                             P-gp inhibitors : Verapamil, GF120918A, etc 

Permeability Classification:

Papp:  10  x10-6 cm/s                  High
Papp :   2.5 x10-6 cm/s                 Low
Papp:  2.5 - 10 x10-6 cm/s              Medium

 Efflux Potential: Net Efflux Ratio  2.5

Examples: The Identification of Pgp Substrates and Inhibitors in MDCK-MDR1 Cells

As shown in Table 1, low and high permeable comounds were well differentiated and P-gp substrates showed high efflux ratios across the cell monolayers of MDCK-MDR1 cells. 

Table 1: Apparent permeability coefficients (Papp)  and efflux ratios of test compounds in MDCK-MDR1 cell.

Figure 1: Inhibition of Calacein AM efflux in MDCK-MDR1 cell by different test compounds 

Table 2: IC50 of test compounds determined in MDCK-MDR1 cells

As shown in Table 2 and Figur 1, Pgp inhibitors were well identified and differentiated based on their inhibition potency.