Asenapine
S1283
5~200mg
Brand
Selleckchem
Description
Asenapine
Asenapine inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
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Biological Activity
Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder.
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors. Asenapine behaves as an antagonist at all receptors. [1]
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators |
Start Date | Phases |
|---|---|---|---|---|---|
| NCT02072954 | Active, not recruiting | Schizophrenia | Amneal Pharmaceuticals, LLC|Accutest Research Laboratories (I) Pvt. Ltd. | Phase 2|Phase 3 | |
| NCT01807741 | Recruiting | Bipolar Depression | University of Cincinnati|University of Louisville|Merck Sharp & Dohme Corp. | Phase 2 | |
| NCT01948024 | Completed | Schizophrenia|Bipolar Disorder | bioRASI, LLC|Sun Pharmaceutical Industries Limited | Phase 1 | |
| NCT01495741 | Active, not recruiting | Bipolar Disorder|Schizophrenia | Merck Sharp & Dohme Corp. |
Chemical Information
| Molecular Weight (MW) | 401.84 |
|---|---|
| Formula |
C17H16ClNO.C4H4O4 |
| CAS No. | 85650-56-2 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | Saphris |
| Solubility (25°C) * | In vitro | DMSO | 80 mg/mL (199 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Chemical Name | H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-, (3aS,12bS)- |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.40184 | 4.0184 | 8.0368 | 12.0552 |
Application
Reactivity
