Referencia número: HY-B0539

Desloratadine

(Synonyms: Sch34117)

14 Cited Publications

Revisión del cliente

Based on 14 publication(s) in Google Scholar

Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (K_i=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria.

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Pureza: 99.98%
No. CAS: 100643-71-8
Fòrmula: C₁₉H₁₉ClN₂
Peso molecular:310.83

Almacenamiento:

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

Desloratadine Chemical Structure

No. CAS: 100643-71-8

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

H₁ Receptor

Ver todos los productos específicos de isoformas Histamine Receptor :

Ver todos los productos específicos de isoformas TNF Receptor :

Ver todos los productos específicos de isoformas Leukotriene Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	172 μM Compound: Desloratadine	Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay	[PMID: 25318072]
HT-29	IC₅₀	11.2 μM Compound: 1	Cytotoxicity against human HT-29 cells after 72 hrs by crystal violet staining Cytotoxicity against human HT-29 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
HT-29	IC₅₀	11.2 μM Compound: 5	Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]
MCF7	IC₅₀	10.5 μM Compound: 1	Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet staining Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
MCF7	IC₅₀	10.5 μM Compound: 5	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]
MDA-MB-231	IC₅₀	12.1 μM Compound: 1	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by crystal violet staining Cytotoxicity against human MDA-MB-231 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
MDA-MB-231	IC₅₀	12.1 μM Compound: 5	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]

In Vitro

Desloratadine (300 nmol/L-100 µmol/L) inhibits the release or production of multiple inflammatory mediators in cells with high affinity receptors for IgE^[1].
Desloratadine (1-10 μM, 15 min) has an inhibitory effect on IGE-induced IL-4 and IL-13 secretion that is nearly 6-7 times greater than its inhibitory effect on histamine and LTC4 release^[2].
Desloratadine (0.1-10 μmol/L, 1 h) dose-dependently inhibits platelet-activating factor (PAF)-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion to human umbilical vein endothelial cells^[5].
Desloratadine (1, 10 and 50 μM, 30 min) inhibits the activation of eosinophils and mast cells in polyp tissues of patients with chronic sinusitis^[6].

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

In Vivo

Desloratadine inhibits histamine-induced paw edema in a mouse inflammatory model in a dose-dependent manner (ED₅₀=0.15 mg/kg; p.o.) and dose-dependently reduces the number of coughs after ovalbumin (HY-W250978) sensitization and antigen challenge in sensitized guinea pigs (the minimum effective antitussive dose is 0.3 mg/kg)^[5].

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

Chemical Information

No. CAS 100643-71-8
Appearance Solid
Peso molecular 310.83
Fòrmula C₁₉H₁₉ClN₂
Color Off-white to light yellow
SMILES

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

Sch34117
Structure Classification
- Others
Initial Source
- Endogenous metabolite
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (14)

All IFWBBio/Physico-chemical Assay

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Journal Impact Factor

Nat Commun

Maprotiline restores ER homeostasis and rescues neurodegeneration via Histamine Receptor H1 inhibition in retinal ganglion cells. [Abstract]

2022 Nov 10;13(1):6796. PMID: 36357388

Desloratadine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Nov 10;13(1):6796. [Abstract]

10 µM Amoxapine (Amo), Desloratadine (Desl) and Maprotiline (Map) are incubated with HEK293T cells for 24 h and significantly inhibits PERK phosphorylation and expression of ATF4 and CHOP .

Desloratadine purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Nov 10;13(1):6796. [Abstract]

Relative (to DMSO) CHOP-Luc activities of 12 compounds and 2 control compounds GSK2606414 and ISRIB at 10 µM in the presence of Tm/Tg (1 µM), 24 h after exposure. Desloratadine significantly inhibited CHOP-luciferase activity induced by ER stress (Tm/Tg) at 10 µM.
Acta Pharmacol Sin

Desloratadine ameliorates paclitaxel-induced peripheral neuropathy and hypersensitivity reactions in mice. [Abstract]

2024 Oct;45(10):2061-2076. PMID: 38789495

Desloratadine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2061-2076. [Abstract]

Representative images with quantifications of immunostaining for neurite outgrowth of DRG neurons (labeled by β-tubulin III, green) from (a, b) PIPN mice and (a, c) AAV-injected mice (n = 5). The results showed that Desloratadine (DLT) (10-20 mg/kg; i.p.; once daily for 4 weeks) targeted 5HTR_2A to promote neurite outgrowth in DRG neurons in PIPN mice.. Scale bar: 50 μm.

Desloratadine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2061-2076. [Abstract]

Western blot analysis with its quantification of c-Fos, NLRP3, Casapse1, c-Casapse1 and IL-1β protein expression levels in primary spinal astrocytes (n = 3). The results demonstrated that Desloratadine (DLT, 5-10 μM; 4 h) antagonized the PTX/ATP-induced upregulation of protein levels of c-Fos, NLRP3, c-Caspase1 and IL-1β.

Desloratadine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2061-2076. [Abstract]

Representative images with its quantification of immunostaining for c-Fos nuclear translocation in primary spinal astrocytes (n = 3). The immunofluorescence assay results indicated that Desloratadine (DLT, 5-10 μM; 4 h) inhibited the PTX/ATP-induced increase in c-Fos nuclear translocation . Scale bar: 5 μm.
J Med Chem

Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]

2021 Mar 11;64(5):2725-2738. PMID: 33619967
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Mol Neurobiol

Desloratadine Rescues Schizophrenia-like Phenotypes by Inhibiting the Pathogenic 5-HT2AR-PI3K/AKT/mTOR Signaling Axis. [Abstract]

2026 Jun 24;63(1):716. PMID: 42340538
ACS Infect Dis

Loratadine Derivative Lo-7: A Weapon against Drug-Resistant Enterococcus and Streptococcal Infections. [Abstract]

2024 Aug 9;10(8):2961-2977. PMID: 39066703
iScience

Loratadine inhibits Staphylococcus aureus virulence and biofilm formation. [Abstract]

2022 Jan 5;25(2):103731. PMID: 35098100
FASEB J

MRGPRX2 Mediates Mast Cell-Induced Endometriosis Pain Through the Sensitization of Sensory Neurons via Histamine/HRH1/TRPV1 Signaling Pathway. [Abstract]

2025 Jul 15;39(13):e70778. PMID: 40600649
Pharm Res

Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]

2025 Aug;42(8):1315-1329. PMID: 40760405
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
Genes (Basel)

Influence and Optimization of Diverse Culture Systems on Chicken Embryonic Stem Cell Culture. [Abstract]

2024 Oct 30;15(11):1400. PMID: 39596599
J Clin Psychopharmacol

A Potential Drug-Gene-Drug Interaction Between Cannabidiol, CYP2D6*4, and Fluoxetine: A Case Report. [Abstract]

2022 Jul-Aug;42(4):422-424. PMID: 35652796
Technol Cancer Res Treat

Desloratadine, a Novel Antigrowth Reagent for Bladder Cancer. [Abstract]

2020 Jan-Dec:19:1533033820926591. PMID: 32406319
Patent

US20250295610A1.

Solvente y solubilidad

In Vitro:

DMSO : 6.67 mg/mL (21.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

3.2172 mL

16.0860 mL

32.1719 mL

5 mM

0.6434 mL

3.2172 mL

6.4344 mL

10 mM

0.3217 mL

1.6086 mL

3.2172 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, 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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: ≥ 0.67 mg/mL (2.16 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.67 mg/mL (2.16 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.67 mg/mL (2.16 mM); Clear solution

This protocol yields a clear solution of ≥ 0.67 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 (6.7 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)
Instrucciones de manejo (2659 KB)

Referencias

[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]

[5]. Agrawal, et al. "Pharmacology and clinical efficacy of desloratadine as an anti-allergic and anti-inflammatory drug." Expert opinion on investigational drugs 10.3 (2001): 547-560. [Content Brief]

[6]. Kowalski, et al. "Inhibition of nasal polyp mast cell and eosinophil activation by desloratadine." Allergy 60.1 (2005): 80-85. [Content Brief]

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

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
DMSO	1 mM	3.2172 mL	16.0860 mL	32.1719 mL	80.4298 mL
	5 mM	0.6434 mL	3.2172 mL	6.4344 mL	16.0860 mL
	10 mM	0.3217 mL	1.6086 mL	3.2172 mL	8.0430 mL
	15 mM	0.2145 mL	1.0724 mL	2.1448 mL	5.3620 mL
	20 mM	0.1609 mL	0.8043 mL	1.6086 mL	4.0215 mL

Keywords

Desloratadine

14 Cited Publications

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Desloratadine

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Publications Citing Use of MedChemExpress (MCE) Desloratadine

Ver todos los productos específicos de isoformas Histamine Receptor

Ver todos los productos específicos de isoformas TNF Receptor

Ver todos los productos específicos de isoformas Leukotriene Receptor

Actividad biológica

Chemical Information

Publications (14)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Desloratadine Related Classifications

HY-B0539 Related Classifications