2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. 5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor
  4. Asenapine

Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.

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Asenapine Chemical Structure

Asenapine Chemical Structure

CAS No. : 65576-45-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mg USD 144 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Asenapine:

Asenapine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Asenapine

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α adrenergic receptor β adrenergic receptor

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder[1][2].

IC50 & Target[5]

5-HT1A Receptor

8.6 (pKi)

5-HT1B Receptor

8.4 (pKi)

5-HT2A Receptor

10.2 (pKi)

5-HT2B Receptor

9.8 (pKi)

5-HT2C Receptor

10.5 (pKi)

5-HT5 Receptor

8.8 (pKi)

5-HT6 Receptor

9.6 (pKi)

5-HT7 Receptor

9.9 (pKi)

Alpha-2A adrenergic receptor

8.9 (pKi)

α1-adrenergic receptor

8.9 (pKi)

Alpha-2B adrenergic receptor

9.5 (pKi)

Alpha-2C adrenergic receptor

8.9 (pKi)

D1 Receptor

8.9 (pKi)

D2 Receptor

8.9 (pKi)

D3 Receptor

9.4 (pKi)

D4 Receptor

9.0 (pKi)

H1 Receptor

9.0 (pKi)

H2 Receptor

8.2 (pKi)

In Vivo

Asenapine (0.05-0.2 mg/kg; s.c.) induces a dose-dependent suppression of conditioned avoidance response (CAR) and does not induce catalepsy[2].

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

Animal Model: Adult male Wistar rats (200-250 g)[2]
Dosage: 0.05 mg/kg, 0.1 mg/kg, 0.2 mg/kg
Administration: Subcutaneous injection
Result: Produced suppression of CAR in a dose-dependent manner.
Clinical Trial
Molecular Weight

285.77

Formula

C17H16ClNO
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C2OC3=CC=CC=C3[C@@](C4)([H])[C@](CN4C)([H])C2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (699.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4993 mL 17.4966 mL 34.9932 mL
5 mM 0.6999 mL 3.4993 mL 6.9986 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (8.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (8.75 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4993 mL 17.4966 mL 34.9932 mL 87.4829 mL
5 mM 0.6999 mL 3.4993 mL 6.9986 mL 17.4966 mL
10 mM 0.3499 mL 1.7497 mL 3.4993 mL 8.7483 mL
15 mM 0.2333 mL 1.1664 mL 2.3329 mL 5.8322 mL
20 mM 0.1750 mL 0.8748 mL 1.7497 mL 4.3741 mL
25 mM 0.1400 mL 0.6999 mL 1.3997 mL 3.4993 mL
30 mM 0.1166 mL 0.5832 mL 1.1664 mL 2.9161 mL
40 mM 0.0875 mL 0.4374 mL 0.8748 mL 2.1871 mL
50 mM 0.0700 mL 0.3499 mL 0.6999 mL 1.7497 mL
60 mM 0.0583 mL 0.2916 mL 0.5832 mL 1.4580 mL
80 mM 0.0437 mL 0.2187 mL 0.4374 mL 1.0935 mL
100 mM 0.0350 mL 0.1750 mL 0.3499 mL 0.8748 mL
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Asenapine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Asenapine65576-45-6Org 5222Org5222Org-52225-HT ReceptorAdrenergic ReceptorDopamine ReceptorHistamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptorpsychopharmacologicpsychopharmacologicaldopamineserotoninnoradrenalinenorepinephrinehistaminereceptorsubtypesschizophreniabipolar disorderantidepressantInhibitorinhibitorinhibit

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