Asenapine maleate (Org 5222 maleate)

Alias: HSDB 8061; Org5222; Org-5222; HSDB-8061; Org 5222; HSDB 8061; Org 5222; HSDB8061; Asenapine; Asenapine maleate; trade names: Saphris; Sycrest
Cat No.:V1097 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 maleate (Org 5222 maleate) Chemical Structure CAS No.: 85650-56-2
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Asenapine maleate (Org 5222 maleate):

  • Asenapine (Org 5222)
  • Asenapine HCl (Org 5222 HCl)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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 )
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].
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.
Animal Protocol
Mice: 0.1 or 0.3mg/kg; Rats: 1 mL/kg, injections
Rats: Asenapine maleate is given in a volume of 1 mL/kg body weight, suspended in 10% hydroxypropyl-β-cyclodextrin. Rats are individually trained to fear by putting them in a Skinner box with an electrical foot shock. Thirty minutes prior to the assessment of freezing behavior, animals receive an intraperitoneal (i.p.) injection of asenapine, clozapine, olanzapine, buspirone, or SB242084.

Mice: The male ICR mice undergo repeated injections of asenapine at doses of 0.1 or 0.3 mg/kg. Following treatment, the mice are subjected to a battery of anxiety-related behavioral tests, such as the elevated plus-maze (EPM), defensive marble burying, open-field test, and hyponeophagia test.

References

[1]. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40.

[2]. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.

[3]. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336.

[4]. Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Acta Neuropsychiatr. 2016 Apr;28(2):85-91.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H20CLNO5
Molecular Weight
401.84
Exact Mass
401.1
Elemental Analysis
C, 62.77; H, 5.02; Cl, 8.82; N, 3.49; O, 19.91
CAS #
85650-56-2
Appearance
Solid powder
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
InChi Key
GMDCDXMAFMEDAG-CHHFXETESA-N
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
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
Synonyms
HSDB 8061; Org5222; Org-5222; HSDB-8061; Org 5222; HSDB 8061; Org 5222; HSDB8061; Asenapine; Asenapine maleate; trade names: Saphris; Sycrest
HS Tariff Code
2934.99.9001
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 Data
Solubility (In Vitro)
DMSO: 25~80 mg/mL (62.2~199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
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.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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Clinical Trial Information
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
Biological Data
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