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Theonellamide

Cat. No. M40669
Theonellamide Structure
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Biological Activity

Theonellamide is a bicyclic peptide from the sponge genus Theonella, constructed via a histidine alanine bridge. It has antifungal activity and cytotoxic activity.

Chemical Information
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] Ohad Hasin et al. Mar Drugs. Theonellamides J and K and 5- cis-Apoa-theopalauamide, Bicyclic Glycopeptides of the Red Sea Sponge Theonella swinhoei

[2] Yuko Arita et al. Chem Biol. Targeting cholesterol in a liquid-disordered environment by theonellamides modulates cell membrane order and cell shape

[3] Shinichi Nishimura et al. PLoS One. Visualization of sterol-rich membrane domains with fluorescently-labeled theonellamides

[4] Shinichi Nishimura et al. Nat Chem Biol. Marine antifungal theonellamides target 3beta-hydroxysterol to activate Rho1 signaling

[5] S Wada et al. Mar Biotechnol (NY). Interaction of Cytotoxic Bicyclic Peptides, Theonellamides A and F, with Glutamate Dehydrogenase and 17beta-Hydroxysteroid Dehydrogenase IV

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