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Asenapine Maleate

Product Name
Asenapine Maleate
CAS No.
85650-56-2
Chemical Name
Asenapine Maleate
Synonyms
Org 5222;NSC62790;NSC 62790;NSC-62790;Asenne maleate;Unii-cu9463U2E2;Org5222 Maleate;Saphris Maleate;Org-5222 Maleate;Org 5222 Maleate
CBNumber
CB2932538
Molecular Formula
C21H20ClNO5
Formula Weight
401.84
MOL File
85650-56-2.mol
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Asenapine Maleate Property

Melting point:
141-145°
Flash point:
9℃
storage temp. 
2-8°C
solubility 
H2O: ≥10mg/mL
pka
pK1 <3, pK2 7.52, pK3 8.51(at 25℃)
form 
powder
color 
white to off-white
Water Solubility 
Water : 6.25 mg/mL (15.55 mM; Need ultrasonic and warming)
InChIKey
GMDCDXMAFMEDAG-CHHFXETESA-N
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Safety

Hazard Codes 
Xn,N,T,F
Risk Statements 
22-36/37/38-50/53-39/23/24/25-23/24/25-11
Safety Statements 
26-60-61-45-36/37-16
RIDADR 
UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany 
3
HS Code 
29339900
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
A7861
Product name
Asenapine maleate
Purity
≥98% (HPLC)
Packaging
10mg
Price
$82.1
Updated
2024/03/01
Sigma-Aldrich
Product number
A7861
Product name
Asenapine maleate
Purity
≥98% (HPLC)
Packaging
50mg
Price
$326
Updated
2024/03/01
Tocris
Product number
3737
Product name
Asenapine maleate
Purity
≥98%(HPLC)
Packaging
50
Price
$588
Updated
2021/12/16
Tocris
Product number
3737
Product name
Asenapine maleate
Purity
≥98%(HPLC)
Packaging
10
Price
$136
Updated
2021/12/16
TRC
Product number
A788025
Product name
Asenapine maleate
Packaging
100mg
Price
$120
Updated
2021/12/16
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Asenapine Maleate Chemical Properties,Usage,Production

Description

Asenapine, a dual antagonist of dopamine D2and serotonin 5-HT2receptors, was launched for the acute treatment of schizophreniaand manic or mixed episodes associated with bipolar I disorder in adults. Asenapine exhibits high affinity for serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors (Ki = 2.5, 4.0, 0.06, 0.16, 0.03, 1.6, 0.25, and 0.13 nM, respectively); dopamine D1, D2, D3, and D4 receptors (Ki = 1.4, 0.42, 1.1, and 1.3 nM, respectively); a1- and a2-adrenergic receptors (Ki = 1.2 and 1.2 nM, respectively); and histamine H1 receptors (Ki = 1.0 nM), and moderate affinity for H2 receptors (Ki = 6.2 nM). In in vitro assays, asenapine acts as an antagonist at these receptors. Asenapine has no appreciable affinity for muscarinic cholinergic receptors (e.g., Ki = 8128 nM for M1). Despite its potent binding affinity for multiple receptors, the efficacy of asenapine in schizophrenia is thought to be primarily mediated through a combination of antagonist activity at D2 and 5-HT2A receptors.

Chemical Properties

White Solid

Originator

Organon (US)

Uses

Antipsychotic;serotonin 5-HT receptors

Uses

Asenapine maleate has been used as a stressor in studying the Fos expression in forebrain structures of rat models.

Uses

Asenapine Maleate is a 5-HT receptor antagonist developed for the treatment of acute schizophrenia and bipolar mania.

Definition

ChEBI: (S,S)-asenapine maleate is a maleate salt obtained by combining equimolar amounts of (S,S)-asenapine and maleic acid. It contains a (S,S)-asenapine(1+). It is an enantiomer of a (R,R)-asenapine maleate.

brand name

Saphris

General Description

Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder. The drug is marketed under the trade names Saphris? and Sycrest. This certified solution standard is suitable for LC/MS or GC/MS applications in clinical toxicology, forensic testing, or pharmaceutical research.

Biochem/physiol Actions

Asenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic.

Side effects

The most common adverse effects associated with asenapine treatment include insomnia, somnolence, nausea, anxiety, agitation, headache, vomiting, constipation, and psychosis. In placebo-controlled trials with risperidone, aripiprazole, and olanzapine in elderly subjects with dementia, there was a higher incidence of cerebrovascular adverse reactions (cerebrovascular accidents and transient ischemic attacks) including fatalities compared to placebo-treated subjects. Asenapine is not approved for the treatment of patients with dementia-related psychosis.

Synthesis

The chemical synthesis of asenapine can be achieved by several different methods. A concise synthesis of asenapine begins with the Horner-Emmons condensation of diethyl (5-chloro-2-fluoro)benzyl phosphonate with salicylaldehyde to produce the corresponding stilbene derivative, which undergoes a 1,3-dipolar cycloaddition reaction with trimethylamine-N-oxide in the presence of lithium diisopropylamide to furnish a trans-3,4-diarylpyrrolidine intermediate. Then, a base-catalyzed intramolecular cyclization involving the nucleophilic displacement of the fluoro group by the phenolic hydroxyl group affords asenapine, which is finally treated with maleic acid in ethanol to yield the corresponding maleate salt.

storage

Store at +4°C

Asenapine Maleate Preparation Products And Raw materials

Raw materials

Preparation Products

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Asenapine Maleate Suppliers

Anqing Runke Biomedical Technology Co., Ltd.
Tel
0556-5282330 18075373931
Fax
0556-5282330
Email
sales@growingchem.com
Country
China
ProdList
306
Advantage
58
Suzhou Zehou Biotechnology Co. , Ltd.
Tel
0512-68716880 18075373931
Fax
18075373931
Email
sales@growingchem.com
Country
China
ProdList
191
Advantage
64
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
94657
Advantage
76
Chemvon Biotechnology Co., Ltd
Tel
021-50790412
Fax
+86-21-50790419
Email
info@chemvon.com
Country
China
ProdList
371
Advantage
57
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
chenyj@titansci.com
Country
China
ProdList
14103
Advantage
59
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2123
Advantage
70
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19172
Advantage
64
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32321
Advantage
50
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View Lastest Price from Asenapine Maleate manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Asenapine Maleate 85650-56-2
Price
US $0.00/Kg/Bag
Min. Order
10g
Purity
99.5%min HPLC
Supply Ability
10KGS
Release date
2021-07-07
Zhuozhou Wenxi import and Export Co., Ltd
Product
Asenapine Maleate 85650-56-2
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Asenapine Maleate 85650-56-2
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09

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