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Asenapine Maleate

Catalog No. T1951 CAS 85650-56-2

Synonyms: Org 5222 maleate, Org 5222

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.

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Asenapine Maleate, CAS 85650-56-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 73.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 137.00
200 mg	In stock	$ 237.00
500 mg	In stock	$ 392.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.73%

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Description	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.
Targets&IC50	5-HT2B:9.75(pKi), 5-HT2C:10.46(pKi), 5-HT6:9.6(pKi), 5-HT2A:10.15(pKi), 5-HT7:9.94(pKi)
In vitro	Asenapine (0.01 mg/kg, i.v.) preferentially increased dopamine outflow in the shell compared to the nucleus accumbens (NAc) core, with no difference observed at a higher dosage (0.05 mg/kg, i.v.). Asenapine significantly enhanced the response to NMDA in pyramidal cells within the medial prefrontal cortex. In freely moving rats, Asenapine (0.05-0.2 mg/kg, subcutaneous injection) induced dose-dependent conditioned avoidance response (CAR) inhibition (without recording escape failures) and did not induce cataleptic fainting. Moreover, Asenapine (0.05-0.2 mg/kg, subcutaneous injection) increased dopamine outflow in both the medial prefrontal cortex and the nucleus accumbens in rats.
In vivo	Asenapine demonstrates a higher affinity for 5-HT 2C, 5-HT 2A, 5-HT 2B, 5-HT 7, 5-HT 6, alpha2B, and D3 receptors compared to its affinity for D2 receptors, indicating a closer interaction with these targets at therapeutic doses. Asenapine is an effective antagonist for a range of receptors, including 5-HT 1A (7.4), 5-HT 1B (8.1), 5-HT 2A (9.0), 5-HT 2B (9.3), 5-HT 2C (9.0), 5-HT 6 (8.0), 5-HT 7 (8.5), D2 (9.1), D3 (9.1), alpha2A (7.3), alpha2B (8.3), alpha2C (6.8), and H 1 receptors (8.4), as indicated by their respective pKB values.
Kinase Assay	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.

Synonyms	Org 5222 maleate, Org 5222
Molecular Weight	401.84
Formula	C21H20ClNO5
CAS No.	85650-56-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

DMSO: 74 mg/mL (184.2 mM)

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

References and Literature

1. Shahid M, et al. J Psychopharmacol,2009, 23(1), 65-73. 2. Frånberg O, et al. Psychopharmacology (Berl). 2008 Feb;196(3):417-29.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library EMA Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Neurotransmitter Receptor Compound Library Anti-Obesity Compound Library

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Viloxazine Onitisin Pizotifen Malate Cinchonidine Lorcaserin HCl AVN-101 6-fluoro-DL-Tryptophan Perospirone

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Keywords

Asenapine Maleate 85650-56-2 GPCR/G Protein Neuroscience 5-HT Receptor inhibit Org5222 Inhibitor Org-5222 Org 5222 maleate Org 5222 Org 5222 Maleate 5-hydroxytryptamine Receptor Serotonin Receptor Asenapine inhibitor

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