1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Levodropropizine

Levodropropizine  (Synonyms: (S)-(-)-Dropropizine; DF-526)

Cat. No.: HY-B1895 Purity: 99.71%
SDS COA Handling Instructions

Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.

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

Levodropropizine Chemical Structure

Levodropropizine Chemical Structure

CAS No. : 99291-25-5

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Description

Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent[1].

In Vivo

Levodropropizine (14 mg/kg, p.o., 2 weeks) attenuates the chronic cigarette smoke-exposure enhanced cough in guinea pigs[2].
Levodropropizine (20 and 40 mg/kg, i.p.) inhibits seizure activity in rats with Pentylenetetrazol (PTZ)-induced status epilepticus[3].
Levodropropizine (10-200 mg/kg, i.p.) reduces Capsaicin (HY-10448) and Substance P-induced plasma extravasation in the rat trachea[4].

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

Animal Model: Pentylenetetrazol (PTZ)-induced status epilepticus in rats[3]
Dosage: 20 and 40 mg/kg
Administration: i.p.
Result: Decreased Mean electroencephalogram (EEG) spike wave percentage score from 76.8% (placebo) to 13.1% (lower dose) and 7.6% (higher dose).
Decreased Racine's Convulsion Scale (RCS) from a mean of 5.8 (placebo) to 1.83 (lower dose) and 1.16 (higher dose).
Increased time to first myoclonic jerk (TFMJ) from a mean of 65.1 s (placebo), to 247.3 s (lower dose) and 295.5 s (higher dose).
Clinical Trial
Molecular Weight

236.31

Formula

C13H20N2O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H](O)CN1CCN(C2=CC=CC=C2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (211.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 10 mg/mL (42.32 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2317 mL 21.1586 mL 42.3173 mL
5 mM 0.8463 mL 4.2317 mL 8.4635 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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)

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: ≥ 2.5 mg/mL (10.58 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 (10.58 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (211.59 mM); Clear solution; Need ultrasonic

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).
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.2317 mL 21.1586 mL 42.3173 mL 105.7932 mL
5 mM 0.8463 mL 4.2317 mL 8.4635 mL 21.1586 mL
10 mM 0.4232 mL 2.1159 mL 4.2317 mL 10.5793 mL
15 mM 0.2821 mL 1.4106 mL 2.8212 mL 7.0529 mL
20 mM 0.2116 mL 1.0579 mL 2.1159 mL 5.2897 mL
25 mM 0.1693 mL 0.8463 mL 1.6927 mL 4.2317 mL
30 mM 0.1411 mL 0.7053 mL 1.4106 mL 3.5264 mL
40 mM 0.1058 mL 0.5290 mL 1.0579 mL 2.6448 mL
DMSO 50 mM 0.0846 mL 0.4232 mL 0.8463 mL 2.1159 mL
60 mM 0.0705 mL 0.3526 mL 0.7053 mL 1.7632 mL
80 mM 0.0529 mL 0.2645 mL 0.5290 mL 1.3224 mL
100 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0579 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.

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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.

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Levodropropizine
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