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WT-TTR inhibitor 1

Cat. No. M42715
WT-TTR inhibitor 1 Structure
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Biological Activity

WT-TTR inhibitor 1 is a wild-type Transthyretin (WT-TTR) inhibitor with 29.05% inhibition at 100 μM.

Chemical Information
Molecular Weight 312.77
Formula C16H9ClN2OS
CAS Number 23983-05-3
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 Dessì et al. Molecules. Rational Design, Synthesis, Characterization and Evaluation of Iodinated 4,4'-Bipyridines as New Transthyretin Fibrillogenesis Inhibitors

[2] Mobina Alemi et al. CNS Neurosci Ther. Transthyretin stability is critical in assisting beta amyloid clearance- Relevance of transthyretin stabilization in Alzheimer's disease

[3] Boyoung Kim et al. Eur J Med Chem. Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors

[4] Sean R Miller et al. Lab Invest. Native state stabilization by NSAIDs inhibits transthyretin amyloidogenesis from the most common familial disease variants

[5] Sara L Adamski-Werner et al. J Med Chem. Diflunisal analogues stabilize the native state of transthyretin. Potent inhibition of amyloidogenesis

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Keywords: WT-TTR inhibitor 1 supplier, Transthyretin (TTR), inhibitors, activators

 
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