| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
|
Asenapine HCl (Org-5222; HSDB 8061; Saphris; Sycrest) is a potent antagonist of multiple targets including serotonin, norepinephrine, dopamine and histamine receptors. It can be used to treat acute mania linked to bipolar disorder and schizophrenia as an atypical antipsychotic.
| Targets |
sPLA2 ( Ki = 0.66 ); 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 )
|
|---|---|
| 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].
|
| 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].
|
| References |
|
| Molecular Formula |
C17H17CL2NO
|
|---|---|
| Molecular Weight |
322.228982686996
|
| Exact Mass |
321.07
|
| CAS # |
1412458-61-7
|
| Related CAS # |
Asenapine; 65576-45-6; Asenapine maleate; 85650-56-2; Asenapine-13C,d3 hydrochloride
|
| Appearance |
Powder
|
| SMILES |
CN1C[C@H]2[C@H](C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24.Cl
|
| InChi Key |
FNJQDKSEIVVULU-CTHHTMFSSA-N
|
| InChi Code |
InChI=1S/C17H16ClNO.ClH/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;/h2-8,14-15H,9-10H2,1H3;1H/t14-,15-;/m1./s1
|
| Chemical Name |
(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;hydrochloride
|
| Synonyms |
Asenapine hydrochloride; Asenapine HCl
|
| 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)
|
| Solubility (In Vitro) |
H2O: ~100 mg/mL (~310.3 mM)
DMSO: ~50 mg/mL (~155.2 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1034 mL | 15.5169 mL | 31.0337 mL | |
| 5 mM | 0.6207 mL | 3.1034 mL | 6.2067 mL | |
| 10 mM | 0.3103 mL | 1.5517 mL | 3.1034 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 |
| NCT01498770 | Completed | Drug: Asenapine Drug: Aripiprazole |
Bipolar Disorder | Organon and Co | April 1, 2013 | N/A |
| NCT00806234 | Completed | Drug: Aripiprazole or Perphenazine Drug: Metformin |
Psychotic Disorders |
Johns Hopkins University | January 2009 | Phase 4 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
