Asenapine free base
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 317251

CAS#: 65576-45-6 (free)

Description: Asenapine, also known as Org 5222 and HSDB 8061, 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. It exhibits potent activity in animal models predictive of antipsychotic efficacy.


Chemical Structure

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Asenapine free base
CAS# 65576-45-6 (free)

Theoretical Analysis

MedKoo Cat#: 317251
Name: Asenapine free base
CAS#: 65576-45-6 (free)
Chemical Formula: C17H16ClNO
Exact Mass: 285.09204
Molecular Weight: 285.77
Elemental Analysis: C, 71.45; H, 5.64; Cl, 12.41; N, 4.90; O, 5.60

Size Price Shipping out time Quantity
1g USD 3650 2 Weeks
2g USD 4950 2 Weeks
5g USD 9650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-01. Prices are subject to change without notice.

Asenapine free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Related CAS #: 85650-56-2 (maleate)   65576-45-6 (free)    

Synonym: Org 5222; Org5222; Org-5222; HSDB 8061; HSDB-8061; HSDB8061; Asenapine; Asenapine maleate; trade names Saphris and Sycrest.

IUPAC/Chemical Name: (3aR*,12bR*)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole

InChi Key: VSWBSWWIRNCQIJ-GJZGRUSLSA-N

InChi Code: InChI=1S/C17H16ClNO/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/t14-,15-/m0/s1

SMILES Code: CN1C[C@](C2=CC=CC=C2OC3=CC=C(Cl)C=C34)([H])[C@@]4([H])C1

Appearance:
Oily liquid or waxy semi-solid

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 285.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Scheidemantel T, Korobkova I, Rej S, Sajatovic M. Asenapine for bipolar disorder. Neuropsychiatr Dis Treat. 2015 Dec 4;11:3007-17. doi: 10.2147/NDT.S78043. eCollection 2015. Review. PubMed PMID: 26674884; PubMed Central PMCID: PMC4675633.

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3: Dell'Osso B, Cremaschi L, Palazzo MC, Spagnolin G, Cattaneo A, Grancini B, Maggi M, Altamura AC. Use of asenapine as add-on therapy in the treatment of bipolar disorder: a comprehensive review and case series. Expert Opin Drug Saf. 2014 Sep;13(9):1199-208. doi: 10.1517/14740338.2014.938047. Epub 2014 Aug 1. Review. PubMed PMID: 25084462.

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5: Citrome L. Asenapine review, part II: clinical efficacy, safety and tolerability. Expert Opin Drug Saf. 2014 Jun;13(6):803-30. doi: 10.1517/14740338.2014.908183. Epub 2014 May 3. Review. PubMed PMID: 24793161.

6: Wang SM, Han C, Lee SJ, Patkar AA, Masand PS, Pae CU. Asenapine, blonanserin, iloperidone, lurasidone, and sertindole: distinctive clinical characteristics of 5 novel atypical antipsychotics. Clin Neuropharmacol. 2013 Nov-Dec;36(6):223-38. doi: 10.1097/WNF.0b013e3182aa38c4. Review. PubMed PMID: 24201235.

7: Cortese L, Bressan RA, Castle DJ, Mosolov SN. Management of schizophrenia: clinical experience with asenapine. J Psychopharmacol. 2013 Apr;27(4 Suppl):14-22. doi: 10.1177/1359786813482533. Epub 2013 Mar 27. Review. PubMed PMID: 23535351.

8: Young AH, Altamura AC, González-Pinto AM, Millet B, Wiedemann K. Use of asenapine in clinical practice for the management of bipolar mania. J Psychopharmacol. 2013 Apr;27(4 Suppl):3-13. doi: 10.1177/1359786813482534. Epub 2013 Mar 27. Review. PubMed PMID: 23535350.

9: Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F. Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. Review. PubMed PMID: 23356509.

10: Bobo WV. Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. Review. PubMed PMID: 23272794.

11: Asenapine: a less effective, yet, more dangerous neuroleptic! Prescrire Int. 2012 Oct;21(131):229-32. Review. PubMed PMID: 23185842.

12: Tarazi FI, Neill JC. The preclinical profile of asenapine: clinical relevance for the treatment of schizophrenia and bipolar mania. Expert Opin Drug Discov. 2013 Jan;8(1):93-103. doi: 10.1517/17460441.2013.738193. Epub 2012 Nov 4. Review. PubMed PMID: 23121334.

13: De Hert M, Yu W, Detraux J, Sweers K, van Winkel R, Correll CU. Body weight and metabolic adverse effects of asenapine, iloperidone, lurasidone and paliperidone in the treatment of schizophrenia and bipolar disorder: a systematic review and exploratory meta-analysis. CNS Drugs. 2012 Sep 1;26(9):733-59. doi: 10.2165/11634500-000000000-00000. Review. PubMed PMID: 22900950.

14: Tarazi FI, Stahl SM. Iloperidone, asenapine and lurasidone: a primer on their current status. Expert Opin Pharmacother. 2012 Sep;13(13):1911-22. doi: 10.1517/14656566.2012.712114. Epub 2012 Jul 31. Review. PubMed PMID: 22849428.

15: Samalin L, Tixeront C, Llorca PM. [Asenapine in bipolar disorder: efficacy, safety and place in clinical practice]. Encephale. 2012 Jun;38(3):257-65. doi: 10.1016/j.encep.2012.05.001. Epub 2012 Jun 5. Review. French. Erratum in: Encephale. 2012 Oct;38(5):448-9. PubMed PMID: 22726414.

16: Stoner SC, Pace HA. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40. doi: 10.1016/j.clinthera.2012.03.002. Epub 2012 Apr 10. Review. PubMed PMID: 22494521.

17: Potkin SG. Asenapine: a clinical overview. J Clin Psychiatry. 2011;72 Suppl 1:14-8. doi: 10.4088/JCP.10075su1.03. Review. PubMed PMID: 22217438.

18: McIntyre RS, Wong R. Asenapine: a synthesis of efficacy data in bipolar mania and schizophrenia. Clin Schizophr Relat Psychoses. 2012 Jan;5(4):217-20. doi: 10.3371/CSRP.5.4.6. Review. PubMed PMID: 22182459.

19: Pompili M, Serafini G, Innamorati M, Ambrosi E, Telesforo L, Venturini P, Giordano G, Battuello M, Lester D, Girardi P. Unmet treatment needs in schizophrenia patients: is asenapine a potential therapeutic option? Expert Rev Neurother. 2011 Jul;11(7):989-1006. doi: 10.1586/ern.11.82. Review. PubMed PMID: 21721916.

20: Citrome L. Iloperidone, asenapine, and lurasidone: a brief overview of 3 new second-generation antipsychotics. Postgrad Med. 2011 Mar;123(2):153-62. doi: 10.3810/pgm.2011.03.2273. Review. PubMed PMID: 21474903.



Additional Information

Related:
65576-45-6 (Asenapine free)
1412458-61-7(Asenapine HCl)
85650-56-2 (Asenapine maleate)