Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

5-HT2A:10.15(pKi), D4 Receptor:1.1 nM (Ki), D3 receptor:0.42 nM (Ki), 5-HT6:9.6(pKi), sPLA2:2.5 nM (Ki), 5-HT2B:9.75(pKi), D2 Receptor:1.3 nM (Ki), 5-HT2C:10.46(pKi), 5-HT7:9.94(pKi)

In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.

马来酸阿塞那平, 阿塞那平马来酸盐, Org 5222 maleate, Org 5222

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (149.31 mM), Sonication is recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.98 mM), Sonication is recommended.