OPC-14523 hydrochloride

Name: OPC-14523 hydrochloride
Brand: MedChemExpress
SKU: HY-116594A
Rating: 4.5 (1 reviews)

Cat. No.: HY-116594A Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC₅₀=47/56 nM), the 5-HT1A receptor (IC₅₀=2.3 nM), and the 5-HT transporter (IC₅₀=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.

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

OPC-14523 hydrochloride Chemical Structure

CAS No. : 145969-31-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 385	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 385	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1700	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2560	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of OPC-14523 hydrochloride:

OPC-14523 free base Get quote

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•Related Screening Libraries:

•Related Small Molecules:

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View All Sigma Receptor Isoform Specific Products:

View All Isoforms

Sigma 1 Receptor Sigma 2 Receptor

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

sigma 1

47 nM (IC₅₀)

sigma 2

56 mM (IC₅₀)

5-HT_1A Receptor

2.3 nM (IC₅₀)

In Vitro

OPC-14523 hydrochloride inhibits the in vitro reuptake of 3 H-5-HT (IC₅₀=27 nM), but it shows very weak inhibitory activity on ³H-NE and ³H-DA reuptake^[1].

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

In Vivo

OPC-14523 hydrochloride (0.3-100 mg/kg; p.o.; daily for 0, 2, 4, 7 days) produces a marked antidepressant-like effect in the forced swimming test (FST) with rats and mice without affecting the general locomotor activity^[1].

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

Animal Model:	Wistar strain of rats (140-245 g)^[1]
Dosage:	0.3-100 mg/kg
Administration:	P.o.; daily for 0, 2, 4, 7 days
Result:	A single doses of 1 mg/kg and higher of OPC-14523 reduced immobility time in the FST with an ED₅₀ value of 27 mg/kg. The ED₅₀ value for OPC-14523 on day 7 was 18 mg/kg.

Animal Model:	ICR strain of mice (25-45 g)^[1]
Dosage:	0.3-100 mg/kg
Administration:	P.o.; daily for 0, 2, 4, 7 days
Result:	A single oral dose of OPC-14523 produced a marked reduction in immobility time during the FST at oral doses of 1 mg/kg and higher, with an ED₅₀ value of 20 mg/kg. The potency of OPC-14523 in decreasing immobility time was greater after treatment for seven consecutive days, producing an ED50 value of 2 mg/kg.

Molecular Weight

450.40

Formula

C₂₃H₂₉Cl₂N₃O₂

CAS No.

145969-31-9

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)C4=C(C(OC)=CC=C4)CC1.[H]Cl

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:

DMSO : 83.33 mg/mL (185.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 5 mg/mL (11.10 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2202 mL	11.1012 mL	22.2025 mL
5 mM	0.4440 mL	2.2202 mL	4.4405 mL
10 mM	0.2220 mL	1.1101 mL	2.2202 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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.

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).

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

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

Purity: 99.95%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (250 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Tottori K, et al. Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001;41(8):976-988. [Content Brief]

[2]. Bermack JE, et al. Effects of the potential antidepressant OPC-14523 [1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2-quinolinone monomethanesulfonate] a combined sigma and 5-HT1A ligand: modulation of neuronal activity in the dorsa [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.2202 mL	11.1012 mL	22.2025 mL	55.5062 mL
	5 mM	0.4440 mL	2.2202 mL	4.4405 mL	11.1012 mL
	10 mM	0.2220 mL	1.1101 mL	2.2202 mL	5.5506 mL
DMSO	15 mM	0.1480 mL	0.7401 mL	1.4802 mL	3.7004 mL
	20 mM	0.1110 mL	0.5551 mL	1.1101 mL	2.7753 mL
	25 mM	0.0888 mL	0.4440 mL	0.8881 mL	2.2202 mL
	30 mM	0.0740 mL	0.3700 mL	0.7401 mL	1.8502 mL
	40 mM	0.0555 mL	0.2775 mL	0.5551 mL	1.3877 mL
	50 mM	0.0444 mL	0.2220 mL	0.4440 mL	1.1101 mL
	60 mM	0.0370 mL	0.1850 mL	0.3700 mL	0.9251 mL
	80 mM	0.0278 mL	0.1388 mL	0.2775 mL	0.6938 mL
	100 mM	0.0222 mL	0.1110 mL	0.2220 mL	0.5551 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.