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CFTRinh-172

Cat. No. M2504
CFTRinh-172 Structure
Synonym:

CFTR inhibitor 172

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 40  USD40 In stock
5mg USD 60  USD60 In stock
10mg USD 110  USD110 In stock
25mg USD 200  USD200 In stock
50mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 3. CFTRinh-172
Method Western-blot assay
Cell Lines K562 cells
Concentrations 20–50 μM
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).
Chemical Information
Molecular Weight 409.4
Formula C18H10F3NO3S2
CAS Number 307510-92-5
Solubility (25°C) DMSO 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Mingfeng Liu, et al. Treatment of human T-cell acute lymphoblastic leukemia cells with CFTR inhibitor CFTRinh-172

[2] N Melis, et al. Revisiting CFTR inhibition: a comparative study of CFTRinh -172 and GlyH-101 inhibitors

[3] David N Sheppard. CFTR channel pharmacology: insight from a flock of clones. Focus on "Divergent CFTR orthologs respond differently to the channel inhibitors CFTRinh-172, glibenclamide, and GlyH-101"

[4] Maximilian Stahl, et al. Divergent CFTR orthologs respond differently to the channel inhibitors CFTRinh-172, glibenclamide, and GlyH-101

[5] Zoia Kopeikin, et al. On the mechanism of CFTR inhibition by a thiazolidinone derivative

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