Asenapine hydrochloride

Name: Asenapine hydrochloride
Brand: MedChemExpress
SKU: HY-16567
Rating: 4.5 (1 reviews)

Cat. No.: HY-16567 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D₂, D₃, D₄) receptor antagonist with K_i values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.

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

Asenapine hydrochloride Chemical Structure

CAS No. : 1412458-61-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 252	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Asenapine hydrochloride:

Asenapine In-stock
Asenapine maleate In-stock
Asenapine-¹³C,d₃ hydrochloride Get quote

1 Publications Citing Use of MCE Asenapine hydrochloride

•Int J Biol Macromol. 2023 Jul 4;125703. [Abstract]

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

View All Dopamine Receptor Isoform Specific Products:

View All Isoforms

Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

sPLA2

2.5 nM (Ki)

5-HT_2A Receptor

0.06 nM (Ki)

5-HT_2C 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-HT_2C, 5-HT_2A, 5-HT_2B, 5-HT₇, 5-HT₆, α_2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pK_B) at 5-HT_1A (7.4), 5-HT1B (8.1), 5-HT_2A (9.0), 5-HT_2B (9.3), 5-HT_2C (9.0), 5-HT₆ (8.0), 5-HT₇ (8.5), D2 (9.1), D3 (9.1), α_2A (7.3), α_2B (8.3), α_2C (6.8) and H1 (8.4) receptors^[2].

MedChemExpress (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].

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

Clinical Trial

Molecular Weight

322.23

Formula

C₁₇H₁₇Cl₂NO

CAS No.

1412458-61-7

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.ClC1=CC2=C(C=C1)OC3=C(C=CC=C3)[C@](C4)([H])[C@]2([H])CN4C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (310.34 mM; Need ultrasonic)

DMSO : 50 mg/mL (155.17 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	3.1034 mL	15.5169 mL	31.0337 mL
5 mM	0.6207 mL	3.1034 mL	6.2067 mL
10 mM	0.3103 mL	1.5517 mL	3.1034 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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 (7.76 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 (7.76 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 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (282 KB) SDS (0 KB)

COA (259 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Stoner SC, Pace HA. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40. [Content Brief]

[2]. Shahid M, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. [Content Brief]

[3]. Ohyama M,et al. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336. [Content Brief]

[4]. Ene HM, et al. Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Acta Neuropsychiatr. 2016 Apr;28(2):85-91. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	3.1034 mL	15.5169 mL	31.0337 mL	77.5843 mL
	5 mM	0.6207 mL	3.1034 mL	6.2067 mL	15.5169 mL
	10 mM	0.3103 mL	1.5517 mL	3.1034 mL	7.7584 mL
	15 mM	0.2069 mL	1.0345 mL	2.0689 mL	5.1723 mL
	20 mM	0.1552 mL	0.7758 mL	1.5517 mL	3.8792 mL
	25 mM	0.1241 mL	0.6207 mL	1.2413 mL	3.1034 mL
	30 mM	0.1034 mL	0.5172 mL	1.0345 mL	2.5861 mL
	40 mM	0.0776 mL	0.3879 mL	0.7758 mL	1.9396 mL
	50 mM	0.0621 mL	0.3103 mL	0.6207 mL	1.5517 mL
	60 mM	0.0517 mL	0.2586 mL	0.5172 mL	1.2931 mL
	80 mM	0.0388 mL	0.1940 mL	0.3879 mL	0.9698 mL
	100 mM	0.0310 mL	0.1552 mL	0.3103 mL	0.7758 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.