Desloratadine (Sch34117)

Alias: SCH34117, NSC675447; SCH 34117; NSC 675447; SCH-34117; NSC-675447; Desloratadine; Clarinex; Neoclarityn; Descarboethoxyloratadine; Aerius
Cat No.:V1242 Purity: ≥98%
Desloratadine (formerly SCH34117, NSC 675447; SCH-34117, NSC-675447; Clarinex; Neoclarityn; Descarboethoxyloratadine; Aerius) is the active metabolite of loratadine which is an anti-histamine drug of the tricyclic class used to treat allergies.
Desloratadine (Sch34117) Chemical Structure CAS No.: 100643-71-8
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Desloratadine (Sch34117):

  • Desloratadine-d4 (Sch34117-d4)
  • Desloratadine-d9 (Sch34117-d9)
  • Desloratadine-3,3,5,5-d4 (desloratadine d4)
  • Desloratadine-d5
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Desloratadine (formerly SCH34117, NSC 675447; SCH-34117, NSC-675447; Clarinex; Neoclarityn; Descarboethoxyloratadine; Aerius) is the active metabolite of loratadine which is an anti-histamine drug of the tricyclic class used to treat allergies. Desloratadine is a potent antagonist of the human histamine H1 receptor with an IC50 of 51 nM.

Biological Activity I Assay Protocols (From Reference)
Targets
Histamine H1 receptor ( IC50 = 51 nM )
ln Vitro

In vitro activity: Desloratadine is a competitive antagonist of contractions induced by carbachol in isolated rabbit iris smooth muscle with pA2 of 6.67.[1] In order to displace tritiated mepyramine, desloratadine binds to the human H1 receptor with a Ki value of 0.87 nM. Desloratadine (100 nM to 10 μM) inhibits human basophils' production of the cytokines IL-4 and IL-13, both IgE-mediated and non-IgE-mediated. Human peripheral blood basophils' IgE- and non-IgE-mediated histamine release is inhibited by desloratadine (300 nM to 100 μM). Desloratadine (0.1 μM to 10 μM) has also been demonstrated to block the adhesion of eosinophils derived from patients with allergic asthma or rhinitis, as well as the chemotaxis of eosinophils induced by platelet-activating factor and TNF-α.[2] Desloratadine (1 μM–10 μM) inhibits histamine and LTC4 release from human basophils in a dose-dependent manner. Desloratadine (0.1 μM–10 μM) inhibits the release of IL-13 from human basophils that have been activated with IL-3 and PMA in a dose-dependent manner. In cultured basophils, desloratadine (10 μM) pretreatment significantly reduces the induced cytokine message. In cultured basophils, desloratadine (10 μM) pretreatment reduces the IL-4 message accumulated with anti-IgE activation by about 80%. Moreover, desloratadine (10 μM) suppresses the histamine and IL-4 protein released into the cultured basophils' supernatants.[3] [3H]Desloratadine binds to the human histamine H1 receptor that is expressed in CHO cells with Kd of 1.1 nM. In competition-binding studies, desloratadine is 52, 57, 194, and 153 times more potent than cetirizine, ebastine, fexofenadine, and loratadine, respectively.[4]

ln Vivo
Desloratadine (1 mg/mL, 3 mg/mL, and 10 mg/mL) causes a long-lasting, dose-dependent mydriasis in guinea pigs in vivo.[1] Desloratadine has an ED50 of 0.15 mg/kg in mice, which prevents histamine-induced paw edema. For guinea pigs, desloratadine (ED50 = 0.9 μg) prevents the increase in microvascular permeability that occurs when the upper airway is challenged with histamine.[2] In conscious mice, desloratadine (5 mg/kg) inhibits oxotremorine-induced tremor by rupturing the blood-brain barrier. A shift in the dose-response curve to the right in the pithed rat indicates that desloratadine (1.0 mg/kg) significantly inhibits decreases in dP/dt induced by oxotremorine (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg). A shift in the dose-response curve to the right in the pithed rat indicates that desloratadine (1.0 mg/kg) significantly inhibits decreases in dP/dt induced by oxotremorine (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg). [5]
Animal Protocol
Dissolved in 20% polyethylene glycol-300; 10 mg/kg; s.c. injection
Male guinea-pigs
References

[1]. Eur J Pharmacol . 1999 Jun 18;374(2):249-54.

[2]. J Allergy Clin Immunol . 2001 Apr;107(4):751-62.

[3]. Clin Exp Allergy . 2001 Sep;31(9):1369-77.

[4]. Eur J Pharmacol . 2002 Aug 9;449(3):229-37.

[5]. BMC Pharmacol . 2005 Aug 18:5:13.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H19CLN2
Molecular Weight
310.82
Exact Mass
310.12
Elemental Analysis
C, 73.42; H, 6.16; Cl, 11.41; N, 9.01
CAS #
100643-71-8
Related CAS #
Desloratadine-d4; 381727-29-3; Desloratadine-d9; 1795024-82-6; Desloratadine-3,3,5,5-d4; 2713301-38-1; Desloratadine-d5; 1020719-34-9
Appearance
Solid powder
SMILES
C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
InChi Key
JAUOIFJMECXRGI-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2
Chemical Name
13-chloro-2-piperidin-4-ylidene-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
Synonyms
SCH34117, NSC675447; SCH 34117; NSC 675447; SCH-34117; NSC-675447; Desloratadine; Clarinex; Neoclarityn; Descarboethoxyloratadine; Aerius
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 25~26 mg/mL (80.4~83.6 mM)
Water: <1 mg/mL
Ethanol: ~62 mg/mL (~199.5 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (8.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (8.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 30% Propylene glycol , 5% Tween 80 , 65% D5W: 30 mg/mL

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05214911 Not yet recruiting Drug: Desloratadine , Prednisolone
Drug: Desloratadine
Allergic Rhinitis Eurofarma Laboratorios S.A. March 30, 2024 Phase 3
NCT05446480 Recruiting Drug: Desloratadine
Drug: Placebo
Heat Stress, Exertional
Inflammatory Response
University of Victoria July 2022 Not Applicable
NCT01314352 Completed Drug: Desloratadine Fed Dr. Reddy's Laboratories Limited December 2005 Phase 1
NCT01314339 Completed Drug: Desloratadine Fasting Dr. Reddy's Laboratories Limited December 2005 Phase 1
NCT01506037 Completed Drug: Desloratadine Healthy Dr. Reddy's Laboratories Limited January 2006 Phase 1
Biological Data
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