CFTRinh-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
|Source||Oncotarget (2017). Figure 3. CFTRinh-172|
|Cell Lines||K562 cells|
|Incubation Time||24 h|
|Results||Consistent with the results obtained using imatinib, CFTRinh-172 led to a significant reduction in p-BCR-ABL in both K562 and SUP-B15 cells as well as significant down-regulation oft-BCR-ABL in K562 cells (Figure 3A) but not in SUP-B15 cells (Figure 3C).|
|Related CFTR Products|
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VX-661 is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface.
IOWH032 is a synthetic CFTR inhibitor with IC50 of 1.01 μM in CHO-CFTR cell based assays. Phase 1/2.
VX-809 is a CFTR corrector that improves CFTR processing and maturation in the cell.
Lonidamine is a novel CFTR open channel blocker with an IC50 of 0.85 mM, which inhibits aerobic glycolysis in cancer cells.
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