HY-B0539-1ml | Desloratadine [100643-71-8] Clinisciences

Description

Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities^[1]^[2].

IC₅₀ & Target^[1]

H₁ Receptor

Human Endogenous Metabolite

Essai clinique

Masse moléculaire

310.82

Formule

C₁₉H₁₉ClN₂

CAS No.

100643-71-8

Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C2C(CCC3=CC=CN=C3/C2=C4CCNCC/4)=C1

Structure Classification

Others

Initial Source

Endogenous metabolite

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 25 mg/mL (80.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2173 mL	16.0865 mL	32.1730 mL
5 mM	0.6435 mL	3.2173 mL	6.4346 mL
10 mM	0.3217 mL	1.6086 mL	3.2173 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.

Calculateur de molarité
Calculateur de dilution

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 (8.04 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 (8.04 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 (8.04 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.

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.

Pureté et documentation

Purity: 99.83%

Select Batch:

Fiche technique (278 KB) SDS (394 KB)

COA (254 KB) LCMS (99 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Geha, R.S. and E.O. Meltzer, Desloratadine: A new, nonsedating, oral antihistamine. J Allergy Clin Immunol, 2001. 107(4): p. 751-62. [Content Brief]

[2]. Schroeder, J.T., et al., Inhibition of cytokine generation and mediator release by human basophils treated with desloratadine. Clin Exp Allergy, 2001. 31(9): p. 1369-77. [Content Brief]

[3]. McClellan K, et al. Desloratadine. Drugs. 2001;61(6):789-797. [Content Brief]

[4]. Anthes, J.C., et al., Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol, 2002. 449(3): p. 229-37. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.2173 mL	16.0865 mL	32.1730 mL	80.4324 mL
	5 mM	0.6435 mL	3.2173 mL	6.4346 mL	16.0865 mL
	10 mM	0.3217 mL	1.6086 mL	3.2173 mL	8.0432 mL
	15 mM	0.2145 mL	1.0724 mL	2.1449 mL	5.3622 mL
	20 mM	0.1609 mL	0.8043 mL	1.6086 mL	4.0216 mL
	25 mM	0.1287 mL	0.6435 mL	1.2869 mL	3.2173 mL
	30 mM	0.1072 mL	0.5362 mL	1.0724 mL	2.6811 mL
	40 mM	0.0804 mL	0.4022 mL	0.8043 mL	2.0108 mL
	50 mM	0.0643 mL	0.3217 mL	0.6435 mL	1.6086 mL
	60 mM	0.0536 mL	0.2681 mL	0.5362 mL	1.3405 mL
	80 mM	0.0402 mL	0.2011 mL	0.4022 mL	1.0054 mL

Desloratadine Related Classifications

GPCR/G Protein Neuronal Signaling Immunology/Inflammation Metabolic Enzyme/Protease
Histamine Receptor Endogenous Metabolite

Desloratadine [100643-71-8]

Référence HY-B0539-1ml

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Other Forms of Desloratadine:

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Complete Stock Solution Preparation Table

Desloratadine Related Classifications

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