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Frentizole

Cat. No. M20682
Frentizole Structure
Synonym:

Frentizol

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Biological Activity

Frentizole is a novel inhibitor of amyloid beta peptide (Abeta) binding alcohol dehydrogenase (ABAD) interaction with IC50 of 200 μM. Frentizole is a nontoxic antiviral and immunosuppressive agent used clinically in rheumatoid arthritis and systemic lupus erythematosus.

Chemical Information
Molecular Weight 299.35
Formula C15H13N3O2S
CAS Number 26130-02-9
Solubility (25°C) DMSO 60 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] Martha Cecilia Rosales-Hernndez, et al. Molecules. Synthesis and Biological Importance of 2-(thio)ureabenzothiazoles

[2] Lukas Hroch, et al. Bioorg Med Chem. Synthesis and evaluation of frentizole-based indolyl thiourea analogues as MAO/ABAD inhibitors for Alzheimer's disease treatment

[3] D R Kay, et al. Arthritis Rheum. Frentizole therapy of active systemic lupus erythematosus

[4] U K Sabharwal, et al. Arthritis Rheum. Frentizole therapy in systemic lupus erythematosus

[5] I I Scheetz ME, et al. Infect Immun. Frentizole, a novel immunosuppressive, and azathioprine: their comparative effects on host resistance to Pseudomonas aeruginosa, Candida albicans, herpes simplex virus, and influenza (Ann Arbor) virus

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