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ER 27319 maleate

Cat. No. M6715
ER 27319 maleate Structure
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Quality Control & Documentation
Biological Activity

ER 27319 maleate is a selective inhibitor of Syk kinase. Inhibits tyrosine phosphorylation of Syk initiated by the engagement of FcεRI in rat and human mast cells. Results in the abrogation of degranulation, TNF-α production (IC50 = 10 μM) and other related signaling events.

Chemical Information
Molecular Weight 396.17
Formula C18H20N2O.C4H4O4
CAS Number 1204480-26-1
Solubility (25°C) Water 29.71 mg/mL
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] Saka, et al. J Cardiovasc Pharmacol. Pitavastatin improves cardiac function and survival in association with suppression of the myocardial endothelin system in a rat model of hypertensive heart failure.

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