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Trodusquemine

Cat. No. M21392
Trodusquemine Structure
Synonym:

MSI-1436;Aminosterol-1436

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Biological Activity

MSI-1436 is a non-competitive inhibitor of PTP1B with a selective IC50 of 1 μM and an IC50 value of 224 μM for TCPTP.

Chemical Information
Molecular Weight 685.07
Formula C37H72N4O5S
CAS Number 186139-09-3
Solubility (25°C) Soluble in DMSO
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] Claudia Capitini, et al. FASEB J. Studying the trafficking of labeled trodusquemine and its application as nerve marker for light-sheet and expansion microscopy

[2] Oxana Kazakova, et al. Int J Mol Sci. From Marine Metabolites to the Drugs of the Future: Squalamine, Trodusquemine, Their Steroid and Triterpene Analogues

[3] Ryan Limbocker, et al. Nat Prod Rep. Squalamine and trodusquemine: two natural products for neurodegenerative diseases, from physical chemistry to the clinic

[4] Ryan Limbocker, et al. Commun Biol. Trodusquemine displaces protein misfolded oligomers from cell membranes and abrogates their cytotoxicity through a generic mechanism

[5] Ryan Limbocker, et al. Nat Commun. Trodusquemine enhances Aβ42 aggregation but suppresses its toxicity by displacing oligomers from cell membranes

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Keywords: Trodusquemine, MSI-1436;Aminosterol-1436 supplier, Phosphatase, inhibitors, activators


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