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Cyclotriazadisulfonamide

Cat. No. M28929
Cyclotriazadisulfonamide Structure
Synonym:

CADA

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Biological Activity

Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way. Cyclotriazadisulfonamide is also a Sec61 translocon inhibitor.

Chemical Information
Molecular Weight 581.79
Formula C31H39N3O4S2
CAS Number 182316-44-5
Form Solid
Solubility (25°C) DMSO 33.33 mg/mL (Need ultrasonic and warming)
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] Eva Pauwels, et al. Int J Mol Sci. Reduced DNAJC3 Expression Affects Protein Translocation across the ER Membrane and Attenuates the Down-Modulating Effect of the Translocation Inhibitor Cyclotriazadisulfonamide

[2] Karoline Berger, et al. J Med Chem. Reduction of Progranulin-Induced Breast Cancer Stem Cell Propagation by Sortilin-Targeting Cyclotriazadisulfonamide (CADA) Compounds

[3] Elisa Claeys, et al. Front Immunol. Small Molecule Cyclotriazadisulfonamide Abrogates the Upregulation of the Human Receptors CD4 and 4-1BB and Suppresses In Vitro Activation and Proliferation of T Lymphocytes

[4] Victor Van Puyenbroeck, et al. Traffic. Preprotein signature for full susceptibility to the co-translational translocation inhibitor cyclotriazadisulfonamide

[5] Violeta G Demillo, et al. J Med Chem. Unsymmetrical cyclotriazadisulfonamide (CADA) compounds as human CD4 receptor down-modulating agents

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Keywords: Cyclotriazadisulfonamide, CADA supplier, HIV Protease, inhibitors, activators


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