1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Asenapine maleate

Asenapine maleate (Synonyms: Org 5222 maleate)

Cat. No.: HY-11100 Purity: 99.95%
Handling Instructions

Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.

For research use only. We do not sell to patients.

Asenapine maleate Chemical Structure

Asenapine maleate Chemical Structure

CAS No. : 85650-56-2

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Solid
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 120 In-stock
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100 mg USD 168 In-stock
Estimated Time of Arrival: December 31
200 mg USD 288 In-stock
Estimated Time of Arrival: December 31
500 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Description

Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.

IC50 & Target

sPLA2

2.5 nM (Ki)

5-HT2A Receptor

0.06 nM (Ki)

5-HT2C Receptor

0.03 nM (Ki)

5-HT7 Receptor

0.13 nM (Ki)

D2 Receptor

1.3 nM (Ki)

D3 Receptor

0.42 nM (Ki)

D4 Receptor

1.1 nM (Ki)

In Vitro

Relative to its D2 receptor affinity, asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats[3]. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

401.84

Formula

C₂₁H₂₀ClNO₅

CAS No.
SMILES

CN1C[[email protected]]2([H])C3=CC=CC=C3OC4=CC=C(Cl)C=C4[[email protected]]2(C1)[H].O=C(O)/C=C\C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (62.21 mM; Need ultrasonic)

H2O : 6.25 mg/mL (15.55 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.22 mM); Clear solution

  • 4.

    Add each solvent one by one:  PBS

    Solubility: 1.2 mg/mL (2.99 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Animal Administration
[3][4]

Rats: Asenapine maleate is suspended in 10% hydroxypropyl-β-cyclodextrin and administered in a volume of 1 mL/kg body weight . Rats are individually fear conditioned using electrical foot shock in a Skinner box. Animals are injected intraperitoneally (i.p.) with asenapine, clozapine, olanzapine, buspirone, or SB242084 at 30 min before freezing behaviour assessment[3].

Mice: Male ICR mice are repeatedly treated with 0.1 or 0.3mg/kg injections of asenapine and then tested in a battery of behavioural tests related to anxiety including the open-field test, elevated plus-maze (EPM), defensive marble burying and hyponeophagia tests[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.95%

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Keywords:

AsenapineOrg 5222Org5222Org-52225-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Product Name:
Asenapine maleate
Cat. No.:
HY-11100
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