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Cyclotheonamide A 

Cat. No. M28118
Cyclotheonamide A  Structure
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Biological Activity

Cyclotheonamide A is a serine protease inhibitor (cyclic polypeptide), which can be obtained from marine sponges of the genus Theonella. Cyclotheonamide A shows potent inhibitory activity against trypsin (Ki=0.023 µM) and streptokinase (Ki=0.035 µM) and moderate inhibitory activity against human α-thrombin (Ki=0.18 µM). Cyclotheonamide A can be used in study of antithrombotic.

Chemical Information
Molecular Weight 731.8
Formula C36H45N9O8
CAS Number 129033-04-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Norbert Schaschke, et al. ChemMedChem. Upgrading a natural product: inhibition of human beta-tryptase by cyclotheonamide analogues

[2] V Ganesh, et al. Protein Sci. Comparison of the structures of the cyclotheonamide A complexes of human alpha-thrombin and bovine beta-trypsin

[3] B E Maryanoff, et al. Proc Natl Acad Sci U S A. Molecular basis for the inhibition of human alpha-thrombin by the macrocyclic peptide cyclotheonamide A

[4] S D Lewis, et al. Thromb Res. Inhibition of thrombin and other trypsin-like serine proteinases by cyclotheonamide A

[5] B E Maryanoff, et al. Bioorg Med Chem. Cyclotheonamide derivatives: synthesis and thrombin inhibition. Exploration of specific structure-function issues

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Keywords: Cyclotheonamide A  supplier, Serine/Threonine Protease, inhibitors, activators


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