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Asenapine

Name: Asenapine
Brand: TargetMol
SKU: T21360
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T21360Cas No. 65576-45-6

Alias Org 5222, ME2136, HSDB 8061

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.721483-46-5

Asenapine

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Purity: 99.64%

Catalog No. T21360Alias Org 5222, ME2136, HSDB 8061Cas No. 65576-45-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$32	In Stock	In Stock
5 mg	$72	In Stock	In Stock
10 mg	$98	In Stock	In Stock
25 mg	$168	In Stock	In Stock
50 mg	$247	In Stock	In Stock
100 mg	$365	-	In Stock
1 mL x 10 mM (in DMSO)	$80	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.64%

Appearance:Oil

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

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.721483-46-5
Targets&IC50	5-HT7 receptor:9.9 (pKi), 5-HT6 receptor:9.6 (pKi), H1 Receptor:9.0 (pKi), 5-HT2C receptor:10.5 (pKi), 5-HT1B receptor:8.4 (pKi), H2 receptor:8.2 (pKi), 5-HT5 Receptor:8.8 (pKi), D2 Receptor:8.9 (pKi), α1-adrenoceptor:8.9 (pKi), D4 Receptor:9.0 (pKi), D1 receptor:8.9 (pKi), 5-HT1A receptor:8.6 (pKi), D3 receptor:9.4 (pKi), 5-HT2A receptor:10.2 (pKi), α2B-adrenoceptor:9.5 (pKi), 5-HT2B receptor:9.8 (pKi), α2C-adrenoceptor:8.9 (pKi), α2A-adrenoceptor:8.9 (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, ME2136, HSDB 8061

Chemical Properties

Molecular Weight	285.77
Formula	C₁₇H₁₆ClNO
Cas No.	65576-45-6
Smiles	[H][C@@]12CN(C)C[C@@]1([H])c1cc(Cl)ccc1Oc1ccccc21
Relative Density.	1.231

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

DMSO: 80 mg/mL (279.95 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (11.55 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.4993 mL	17.4966 mL	34.9932 mL	174.9659 mL
5 mM	0.6999 mL	3.4993 mL	6.9986 mL	34.9932 mL
10 mM	0.3499 mL	1.7497 mL	3.4993 mL	17.4966 mL
20 mM	0.1750 mL	0.8748 mL	1.7497 mL	8.7483 mL
50 mM	0.0700 mL	0.3499 mL	0.6999 mL	3.4993 mL
100 mM	0.0350 mL	0.1750 mL	0.3499 mL	1.7497 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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