Home Tools

Asenapine

Catalog No. T21360 CAS 65576-45-6

Synonyms: Org 5222, HSDB 8061, ME2136

Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.CAS 번호721483-46-5

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Asenapine, CAS 65576-45-6

Pack Size	Availability	Price/USD
1 mg	5 days	$ 34.00
5 mg	5 days	$ 72.00
10 mg	5 days	$ 98.00
25 mg	5 days	$ 168.00
50 mg	5 days	$ 247.00
100 mg	5 days	$ 365.00
1 mL * 10 mM (in DMSO)	5 days	$ 129.00

Bulk Inquiry

Select Batch

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.CAS 번호721483-46-5
Targets&IC50	5-HT2A receptor:10.2 (pKi), 5-HT1B receptor:8.4 (pKi), 5-HT2B receptor:9.8 (pKi), 5-HT1A receptor:8.6 (pKi)
In vitro	In comparison with the antipsychotics, asenapine showed high affinity and a different rank order of binding affinities (pKi) for serotonin receptors (5-HT1A [8.6], 5-HT1B [8.4], 5-HT2A [10.2], 5-HT2B [9.8], 5-HT2C [10.5], 5-HT5 [8.8], 5-HT6 [9.6] and 5-HT7 [9.9]), adrenoceptors (alpha1 [8.9], alpha2A [8.9], alpha2B [9.5] and alpha2C [8.9]), dopamine receptors (D1 [8.9], D2 [8.9], D3 [9.4] and D4 [9.0]) and histamine receptors (H1 [9.0] and H2 [8.2])[2].
In vivo	Asenapine (0.05-0.2 mg/kg, s.c.) induced a dose-dependent suppression of CAR (no escape failures recorded) and did not induce catalepsy. Additionally, it increased dopamine efflux in both the medial prefrontal cortex (mPFC) and the nucleus accumbens (NAc)[2].

Synonyms	Org 5222, HSDB 8061, ME2136
Molecular Weight	285.77
Formula	C17H16ClNO
CAS No.	65576-45-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 80 mg/mL (279.94 mM), Sonication is recommended.

References and Literature

1. M Shahid, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. 2. Olivia Frånberg, et al. Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology (Berl). 2008 Feb;196(3):417-29. 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. 4. Citrome L. Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism. Expert Opin Drug Metab Toxicol. 2014 Jun;10(6):893-903. doi: 10.1517/17425255.2014.908185. Epub 2014 May 3. Review. PubMed PMID: 24793403.

Related Products

Related compounds with same targets

Spiperone Dexchlorpheniramine Maleate Trimipramine maleate Domperidone (-)-Isocorypalmine L-741626 Etilevodopa hydrochloride Spiroxatrine

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Asenapine 65576-45-6 GPCR/G Protein Immunology/Inflammation Neuroscience Dopamine Receptor 5-HT Receptor Norepinephrine Histamine Receptor Asenapine free base Org-5222 Org 5222 HSDB-8061 HSDB 8061 HSDB8061 Org5222 ME2136 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.