2. Neuronal Signaling GPCR/G Protein
  3. Sigma Receptor mAChR
  4. Pentoxyverine citrate

Pentoxyverine citrate  (Synonyms: Carbetapentane citrate)

Cat. No.: HY-B1055 Purity: 99.63%
COA Handling Instructions

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Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.

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

Pentoxyverine citrate Chemical Structure

Pentoxyverine citrate Chemical Structure

CAS No. : 23142-01-0

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Based on 1 publication(s) in Google Scholar

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Pentoxyverine citrate Related Antibodies

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Description

Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].

IC50 & Target[1]

σ1

41 nM (Ki)

σ2

894 nM (Ki)

In Vivo

Pentoxyverine (Carbetapentane; 1-32 mg/kg; SC) citrate dose-dependently potentiates the sensitizing effect of capsaicin to the mechanical stimulus when the mice were stimulated in the paw injected with Capsaicin (HY-10448)[4].
Pentoxyverine (16 mg/kg; SC) citrate shows strong potentiation of Capsaicin-induced secondary mechanical allodynia[4].
Pentoxyverine (50 mg/kg; orally; ) citrate, used for positive control, increases the percentage of the aqueous ammonia-induced latent period of cough by 121.72%, inhibits cough frequency by 45.45% after administration for 7 days in mice of either sex (22-25 g)[5].

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

Animal Model: Female wild-type weighing 25 to 30 g[4]
Dosage: 0.5, 1, 2, 4, 8, 16, 32 mg/kg
Administration: SC; 30 min before the intraplantar (i.pl.) administration of capsaicin (0.125 μg)
Result: Dose-dependently potentiated the sensitizing effect of capsaicin to the mechanical stimulus when the mice were stimulated in the paw injected with capsaicin.
Clinical Trial
Molecular Weight

525.59

Formula

C26H39NO10
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1(C2=CC=CC=C2)CCCC1)OCCOCCN(CC)CC.O=C(CC(C(O)=O)(O)CC(O)=O)O
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 : ≥ 36 mg/mL (68.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9026 mL 9.5131 mL 19.0262 mL
5 mM 0.3805 mL 1.9026 mL 3.8052 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.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (3.96 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 (3.96 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.63%

COA (256 KB) HNMR (171 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

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
DMSO 1 mM 1.9026 mL 9.5131 mL 19.0262 mL 47.5656 mL
5 mM 0.3805 mL 1.9026 mL 3.8052 mL 9.5131 mL
10 mM 0.1903 mL 0.9513 mL 1.9026 mL 4.7566 mL
15 mM 0.1268 mL 0.6342 mL 1.2684 mL 3.1710 mL
20 mM 0.0951 mL 0.4757 mL 0.9513 mL 2.3783 mL
25 mM 0.0761 mL 0.3805 mL 0.7610 mL 1.9026 mL
30 mM 0.0634 mL 0.3171 mL 0.6342 mL 1.5855 mL
40 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1891 mL
50 mM 0.0381 mL 0.1903 mL 0.3805 mL 0.9513 mL
60 mM 0.0317 mL 0.1586 mL 0.3171 mL 0.7928 mL
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Pentoxyverine citrate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pentoxyverine23142-01-0CarbetapentaneSigma ReceptormAChRMuscarinic acetylcholine receptorsigma-1 receptorσ1σ2muscarinicantitussiveanticonvulsantspasmolyticbronchial interceptorcough reflexbronchial smooth muscle relaxationairway resistanceInhibitorinhibitorinhibit

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