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

Asenapine (Synonyms: Org 5222)

Cat. No.: HY-10121 Purity: 98.81%
Handling Instructions

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.

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

Asenapine Chemical Structure

Asenapine Chemical Structure

CAS No. : 65576-45-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
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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].

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.
Molecular Weight

285.77

Formula

C₁₇H₁₆ClNO

CAS No.

65576-45-6

SMILES

ClC1=CC=C2OC3=CC=CC=C3[[email protected]@](C4)([H])[[email protected]](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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (174.97 mM; Need ultrasonic)

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
10 mM 0.3499 mL 1.7497 mL 3.4993 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 (8.75 mM); Clear solution

  • 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

  • 3.

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

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

AsenapineOrg 5222Org5222Org-52225-HT ReceptorAdrenergic ReceptorDopamine ReceptorHistamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptorpsychopharmacologicpsychopharmacologicaldopamineserotoninnoradrenalinenorepinephrinehistaminereceptorsubtypesschizophreniabipolar disorder,antidepressantInhibitorinhibitorinhibit

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