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CBIQ

Cat. No. M7723
CBIQ Structure
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Biological Activity

CBIQ is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) and the intermediate-conductance calcium-sensitive K+ channel (KCNN4). CBIQ is a novel tool for a new ion channel; first activator of ΔF508 CFTR, the mutant form of CFTR chloride channel present in 75% of cystic fibrosis patients. Other benzoquinolines act at the normal CFTR but not at ΔF508 CFTR. CBIQ also activates KCNN4, which hyperpolarizes airway epithelial cells to promote anion flux, a further benefit in cystic fibrosis.

Chemical Information
Molecular Weight 213.66
Formula C13H8NCl
CAS Number 32081-28-0
Solubility (25°C) DMSO: 15 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] Alessandro Passera, et al. Multilocus Genotyping Reveals New Molecular Markers for Differentiating Distinct Genetic Lineages among " Candidatus Phytoplasma Solani" Strains Associated with Grapevine Bois Noir

[2] Zhihao Bao, et al. Structure and mechanism of a group-I cobalt energy coupling factor transporter

[3] Rory A Cameron, et al. Molecular analysis of the nitrile catabolism operon of the thermophile Bacillus pallidus RAPc8

[4] Meena Murthy, et al. 4-Chlorobenzo[F]isoquinoline (CBIQ), a novel activator of CFTR and DeltaF508 CFTR

[5] A J Szkotak, et al. 4-Chloro-benzo[F]isoquinoline (CBIQ) activates CFTR chloride channels and KCNN4 potassium channels in Calu-3 human airway epithelial cells

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