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VP3.15 

Cat. No. M28113
VP3.15  Structure
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Quality Control & Documentation
Biological Activity

VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).

Chemical Information
Molecular Weight 366.48
Formula C20H22N4OS
CAS Number 1281681-54-6
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] Rocio Benítez-Fernández, et al. Int J Mol Sci. The Dual PDE7-GSK3β Inhibitor, VP3.15, as Neuroprotective Disease-Modifying Treatment in a Model of Primary Progressive Multiple Sclerosis

[2] Heena Khan, et al. Inflammopharmacology. Pharmacological modulation of phosphodiesterase-7 as a novel strategy for neurodegenerative disorders

[3] Alonso Sánchez-Cruz, et al. Adv Exp Med Biol. GSK-3 Inhibitors: From the Brain to the Retina and Back Again

[4] Alonso Sánchez-Cruz, et al. Mol Neurodegener. Modulation of GSK-3 provides cellular and functional neuroprotection in the rd10 mouse model of retinitis pigmentosa

[5] R Martín-Álvarez, et al. J Chem Neuroanat. A preliminary investigation of phoshodiesterase 7 inhibitor VP3.15 as therapeutic agent for the treatment of experimental autoimmune encephalomyelitis mice

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  Catalog
Abmole Inhibitor Catalog




Keywords: VP3.15  supplier, PDE, inhibitors, activators


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