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AS1949490 

Cat. No. M27934
AS1949490  Structure
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Biological Activity

AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC50 values of 0.34, 0.62, 13, >50, >50, and >50 µM for Mouse SHIP2, Human SHIP2, Human SHIP1, Human PTEN, Human synaptojanin, and Human myotubularin, respectively. AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake. AS1949490 activates intracellular insulin signalling pathways. AS1949490 can be used for research of diabetes.

Chemical Information
Molecular Weight 371.88
Formula C20H18ClNO2S
CAS Number 1203680-76-5
Form Solid
Solubility (25°C) DMSO 50 mg/mL (Need ultrasonic and warming)
Storage Powder -20°C
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] Irena Hlushchuk, et al. Biomolecules. Cell Culture Media, Unlike the Presence of Insulin, Affect α-Synuclein Aggregation in Dopaminergic Neurons

[2] Abdelhalim Azzi. Arch Biochem Biophys. Scaffold dependent role of the inositol 5'-phosphatase SHIP2, in regulation of oxidative stress induced apoptosis

[3] Humeyra Sidal, et al. J Tissue Eng Regen Med. Development of small-molecule-induced fibroblast expansion technologies

[4] Hiroshi Tsuneki, et al. Eur J Pharmacol. AS1949490, an inhibitor of 5'-lipid phosphatase SHIP2, promotes protein kinase C-dependent stabilization of brain-derived neurotrophic factor mRNA in cultured cortical neurons

[5] Pauliina Saurus, et al. Sci Rep. Inhibition of SHIP2 in CD2AP-deficient podocytes ameliorates reactive oxygen species generation but aggravates apoptosis

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  Catalog
Abmole Inhibitor Catalog




Keywords: AS1949490  supplier, Phosphatase, inhibitors, activators


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