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ER-27319

Cat. No. M43531
ER-27319 Structure
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Biological Activity

ER-27319, an acridone derivative, is a potent and selective SYK inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity.

Chemical Information
Molecular Weight 370.4
Formula C20H22N2O5
CAS Number 201010-95-9
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] Medi Kori et al. J Cell Mol Med. Network medicine approaches for identification of novel prognostic systems biomarkers and drug candidates for papillary thyroid carcinoma

[2] Su'an Tang et al. Expert Opin Investig Drugs. Investigational spleen tyrosine kinase (SYK) inhibitors for the treatment of autoimmune diseases

[3] Petra Lusková et al. Curr Pharm Des. Modulation of the Fcepsilon receptor I signaling by tyrosine kinase inhibitors: search for therapeutic targets of inflammatory and allergy diseases

[4] Yoshitaka Sato et al. Int Arch Allergy Immunol. IgG-mediated signal transduction in canine mastocytoma-derived cells

[5] K Moriya et al. Proc Natl Acad Sci U S A. ER-27319, an acridone-related compound, inhibits release of antigen-induced allergic mediators from mast cells by selective inhibition of fcepsilon receptor I-mediated activation of Syk

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Keywords: ER-27319 supplier, Syk, inhibitors, activators

 
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