Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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Other Sizes |
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Purity: ≥98%
Asenapine maleate (Org5222; Org-5222; HSDB-8061; HSDB8061; Saphris and Sycrest), an atypical antipsychotic, is a potent and high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors. Asenapine has been authorized for use as an atypical antipsychotic in the treatment of acute mania brought on by bipolar disorders and schizophrenia. Based on initial data, it appears to have negligible side effects related to anticholinergic and cardiovascular systems, along with negligible weight gain. The FDA gave it their approval in August 2009.
Targets |
sPLA2 ( Ki = 2.5 nM ); 5-HT2A Receptor ( Ki = 0.06 nM ); 5-HT2C Receptor ( Ki = 0.03 nM ); 5-HT7 Receptor ( Ki = 0.13 nM ); D2 Receptor ( Ki = 1.3 nM ); D3 Receptor ( Ki = 0.42 nM ); D4 Receptor ( Ki = 1.1 nM )
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ln Vitro |
Asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B, and D3 receptors than it does for D2 receptors. This suggests that these targets will be more strongly engaged at therapeutic doses. At 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8), and H1 (8.4) receptors, asenapine exhibits potent antagonist (pKB) behavior[2].
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ln Vivo |
Asenapine is an atypical antipsychotic that is being used to treat bipolar I disorder and schizophrenia. Compared to other agents, asenapine may have a better therapeutic effect on anxiety symptoms in rats[3]. In the defensive marble burying test and the EPM, asenapine exhibits anxiolytic-like effects in mice[4].
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Enzyme Assay |
Asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B, and D3 receptors than it does for D2 receptors. This suggests that these targets will be more strongly engaged at therapeutic doses. At 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8), and H1 (8.4) receptors, asenapine exhibits potent antagonist (pKB) behavior.
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Animal Protocol |
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References |
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Molecular Formula |
C21H20CLNO5
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Molecular Weight |
401.84
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Exact Mass |
401.1
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Elemental Analysis |
C, 62.77; H, 5.02; Cl, 8.82; N, 3.49; O, 19.91
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CAS # |
85650-56-2
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Appearance |
Solid powder
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SMILES |
CN1C[C@H]2[C@H](C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O
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InChi Key |
GMDCDXMAFMEDAG-CHHFXETESA-N
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InChi Code |
InChI=1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,15-;/m1./s1
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Chemical Name |
(Z)-but-2-enedioic acid;(2S,6S)-9-chloro-4-methyl-13-oxa-4-azatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),7(12),8,10,14,16-hexaene
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Synonyms |
HSDB 8061; Org5222; Org-5222; HSDB-8061; Org 5222; HSDB 8061; Org 5222; HSDB8061; Asenapine; Asenapine maleate; trade names: Saphris; Sycrest
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4886 mL | 12.4428 mL | 24.8855 mL | |
5 mM | 0.4977 mL | 2.4886 mL | 4.9771 mL | |
10 mM | 0.2489 mL | 1.2443 mL | 2.4886 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01460290 | Completed | Drug: Asenapine | Bipolar Disorder | University Hospitals Cleveland Medical Center |
October 2011 | Phase 4 |
NCT01400113 | Completed | Drug: Asenapine Drug: Placebo |
Radiation Injuries | Unity Health Toronto | April 2012 | Phase 4 |
NCT01349907 | Completed | Drug: Asenapine Drug: Rescue medication |
Bipolar Disorder | Organon and Co | June 16, 2011 | Phase 3 |
NCT01395992 | Completed | Drug: asenapine | Bipolar I Disorder | Forest Laboratories | April 2012 | Phase 3 |
NCT01396291 | Completed | Drug: asenapine Drug: placebo |
Bipolar 1 Disorder | Forest Laboratories | December 2011 | Phase 3 |