Cat. No.: HY-17390A

Loxapine succinate

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages.

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

Purity: 98.84%
CAS No.: 27833-64-3
Formula: C₂₂H₂₄ClN₃O₅
Molecular Weight:445.90

Storage:

4°C, sealed storage, away from moisture

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

Loxapine succinate Chemical Structure

CAS No.: 27833-64-3

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

human 5-HT₂

Human D₄ Receptor

Human D₁ Receptor

Human D₂ Receptor

All 5-HT Receptor Isoforms :

All Dopamine Receptor Isoforms :

In Vitro

In the presence of Loxapine, [³H]ketanserin binds to 5-HT₂ receptor in Frontal cortex of brain in human and bovine with K_i value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows: 5-HT₂≥D₄>>>D₁>D₂ in comparing competition experiments involving the human membranes^[1].
Loxapine (0-20 μM, 24 h or 72 h) reduces IL-1β secretion by LPS-activated mixed glia cultures, reduces IL-2 secretion in mixed glia cultures, and decreases IL-1β and IL-2 secretion in LPS-induced microglia cultures^[2].
Loxapine (4 μM, 24 h) is active against multiple-antibiotic-resistant or Fluoroquinolone-resistant S. Typhimurium^[6].
Loxapine (1, 2, 4 and 8 μM) suppresses intracellular Methicillin-resistant S. aureus (MRSA), Y. enterocolitica and S. flexneri in RAW264.7^[6].

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

In Vivo

Loxapine (5 mg/kg; i.p.; daily for 4 or 10 weeks) decreases serotonin (S₂) but does not elevate dopamine (D2) receptor numbers in the rat brain^[3].

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

Animal Model:

Adult male Wistar rats (150-175 g)^[3]

Dosage:

5 mg/kg

Administration:

Intraperitoneal injection, daily for 4 or 10 weeks

Result:

Induced a very significant reduction (more than 50%) of serotonin (S₂) receptor density after 4 weeks or 10 weeks of daily injection, but did not produce any significant increase in dopamine receptor density.

Chemical Information

CAS No. 27833-64-3

Appearance Solid

Molecular Weight 445.90

Formula C₂₂H₂₄ClN₃O₅

Color White to off-white

SMILES

O=C(O)CCC(O)=O.CN1CCN(C2=NC3=CC=CC=C3OC4=CC=C(Cl)C=C24)CC1

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)

Publications (1)

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Journal Impact Factor

Most Recent

bioRxiv

2025 Sep 21.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (224.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2.5 mg/mL (5.61 mM; ultrasonic and warming and heat to 60°C)

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2427 mL

11.2133 mL

22.4266 mL

5 mM

0.4485 mL

2.2427 mL

4.4853 mL

10 mM

0.2243 mL

1.1213 mL

2.2427 mL

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

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

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Concentration Concentration

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Volume Volume

×
Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (5.61 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 (5.61 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 (5.61 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 Dosage
mg/kg

Animal Weight (Per Animal) Animal Weight (Per Animal)
g

Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL

Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

%
+

+
%
Tween-80 + +

%
Saline +

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).

Working solution concentration: 0.22 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) .

Tel: 609-228-6898
E-mail: [email protected]
Technical Support: [email protected]

Method for preparing in vivo working solution for animal experiments:
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Saline .

Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)

SDS (480 KB)

English - EN (480 KB)

Français - FR (480 KB)

Deutsch - DE (480 KB)

Norwegian - NO (480 KB)

Español - ES (480 KB)

Swedish - SV (480 KB)

Italian - IT (480 KB)

Korean - KR (480 KB)

Portuguese - PT (480 KB)

COA (2659 KB)

Elemental Analysis Report (2659 KB)

HNMR (2659 KB)

CNMR (2659 KB)

RP-HPLC (2659 KB)

NP-HPLC (2659 KB)

MS (2659 KB)

LCMS (2659 KB)

IR (2659 KB)

GC (2659 KB)

OR (2659 KB)

SDS-PAGE (2659 KB)

SEC-HPLC (2659 KB)

Other Report (2659 KB)

Handling Instructions (2659 KB)

References

[1]. Singh AN, et al. A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes. J Psychiatry Neurosci. 1996 Jan;21(1):29-35. [Content Brief]

[2]. Labuzek K, et al. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures. Eur Neuropsychopharmacol. 2005 Jan;15(1):23-30. [Content Brief]

[3]. Lee T, et al. Loxapine and clozapine decrease serotonin (S2) but do not elevate dopamine (D2) receptor numbers in the rat brain. Psychiatry Res. 1984 Aug;12(4):277-85. [Content Brief]

[4]. Keating GM. Loxapine inhalation powder: a review of its use in the acute treatment of agitation in patients with bipolar disorder or schizophrenia. CNS Drugs. 2013 Jun;27(6):479-89. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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.

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

H₂O / DMSO 1 mM 2.2427 mL 11.2133 mL 22.4266 mL 56.0664 mL

5 mM 0.4485 mL 2.2427 mL 4.4853 mL 11.2133 mL

DMSO 10 mM 0.2243 mL 1.1213 mL 2.2427 mL 5.6066 mL

15 mM 0.1495 mL 0.7476 mL 1.4951 mL 3.7378 mL

20 mM 0.1121 mL 0.5607 mL 1.1213 mL 2.8033 mL

25 mM 0.0897 mL 0.4485 mL 0.8971 mL 2.2427 mL

30 mM 0.0748 mL 0.3738 mL 0.7476 mL 1.8689 mL

40 mM 0.0561 mL 0.2803 mL 0.5607 mL 1.4017 mL

50 mM 0.0449 mL 0.2243 mL 0.4485 mL 1.1213 mL

60 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.9344 mL

80 mM 0.0280 mL 0.1402 mL 0.2803 mL 0.7008 mL

100 mM 0.0224 mL 0.1121 mL 0.2243 mL 0.5607 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.

Loxapine succinate Related Classifications

HY-17390A Related Classifications

GPCR/G Protein Neuronal Signaling

5-HT Receptor Dopamine Receptor

Disease Areas

Infection Neurological, Eye or Ear Disease

Neurodegenerative Disease Bacterial Infection

Alzheimer's Disease Parkinson's Disease

Neurological Disease Infection

Powered by Bioz See more details on Bioz

Keywords

Loxapine
27833-64-3
5-HT Receptor
Dopamine Receptor
IL-1β
IL-2
antipsychotics
serotonin
schizophrenia
Inhibitor
inhibitor
inhibit

Your Recently Viewed Products

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.2427 mL	11.2133 mL	22.4266 mL	56.0664 mL
5 mM	0.4485 mL	2.2427 mL	4.4853 mL	11.2133 mL
DMSO	10 mM	0.2243 mL	1.1213 mL	2.2427 mL	5.6066 mL
15 mM	0.1495 mL	0.7476 mL	1.4951 mL	3.7378 mL
20 mM	0.1121 mL	0.5607 mL	1.1213 mL	2.8033 mL
25 mM	0.0897 mL	0.4485 mL	0.8971 mL	2.2427 mL
30 mM	0.0748 mL	0.3738 mL	0.7476 mL	1.8689 mL
40 mM	0.0561 mL	0.2803 mL	0.5607 mL	1.4017 mL
50 mM	0.0449 mL	0.2243 mL	0.4485 mL	1.1213 mL
60 mM	0.0374 mL	0.1869 mL	0.3738 mL	0.9344 mL
80 mM	0.0280 mL	0.1402 mL	0.2803 mL	0.7008 mL
100 mM	0.0224 mL	0.1121 mL	0.2243 mL	0.5607 mL

Loxapine succinate

1 Cited Publications

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Loxapine succinate

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Publications Citing Use of MedChemExpress (MCE) Loxapine succinate

All 5-HT Receptor Isoforms

All Dopamine Receptor Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Loxapine succinate Related Classifications

HY-17390A Related Classifications