Desloratadine

High affinity H1 antagonist; anti-inflammatory. CAS# 100643-71-8

Desloratadine

Catalog No. BCC4540----Order now to get a substantial discount!

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Chemical structure

Desloratadine

3D structure

Chemical Properties of Desloratadine

Cas No. 100643-71-8 SDF Download SDF
PubChem ID 124087 Appearance Powder
Formula C19H19ClN2 M.Wt 310.82
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Sch34117
Solubility DMSO : 25 mg/mL (80.43 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 8-chloro-11-piperidin-4-ylidene-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridine
SMILES C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
Standard InChIKey JAUOIFJMECXRGI-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Desloratadine

DescriptionHigh affinity histamine H1 receptor antagonist (Ki = 0.87 nM); active metabolite of loratadine. Anti-inflammatory.

Desloratadine Dilution Calculator

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Desloratadine Molarity Calculator

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Preparing Stock Solutions of Desloratadine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.2173 mL 16.0865 mL 32.173 mL 64.3459 mL 80.4324 mL
5 mM 0.6435 mL 3.2173 mL 6.4346 mL 12.8692 mL 16.0865 mL
10 mM 0.3217 mL 1.6086 mL 3.2173 mL 6.4346 mL 8.0432 mL
50 mM 0.0643 mL 0.3217 mL 0.6435 mL 1.2869 mL 1.6086 mL
100 mM 0.0322 mL 0.1609 mL 0.3217 mL 0.6435 mL 0.8043 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Desloratadine

Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.

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References on Desloratadine

Comparative efficacy of bilastine, desloratadine and rupatadine in the suppression of wheal and flare response induced by intradermal histamine in healthy volunteers.[Pubmed:27659218]

Curr Med Res Opin. 2017 Jan;33(1):129-136.

OBJECTIVE: To compare the peripheral antihistaminic activity of bilastine, rupatadine and Desloratadine in inhibiting the histamine-induced wheal and flare (W&F) response. RESEARCH DESIGN AND METHODS: Twenty-four healthy volunteers aged 18-40 years participated in this crossover, randomized, double-blind, placebo-controlled clinical study. Subjects received single doses of bilastine 20 mg, Desloratadine 5 mg, rupatadine 10 mg and placebo. W&F responses induced by intradermal injection of histamine 5 mug were evaluated before treatment (basal value) and at 0.5, 1, 2, 4, 6, 9, 12 and 24 hours after treatment. Fifteen minutes after histamine injection, W&F surface areas (cm(2)) were quantified using the Visitrak System. Itching sensation was evaluated using a 100 mm visual analog scale. EudraCT number: 2015-000790-13. MAIN OUTCOME MEASURES: The primary outcome measure was the percentage reduction in W&F areas after each active treatment compared with corresponding basal values. RESULTS: Bilastine induced the greatest inhibition in wheal area and was significantly superior to Desloratadine and rupatadine from 1 to 12 hours (both p < .001). Rupatadine and Desloratadine were better than placebo without differences between them. Maximum wheal inhibition occurred at 6 hours (bilastine 83%, Desloratadine 38%, rupatadine 37%). Onset of action was 1 hour for bilastine and 4 hours for Desloratadine and rupatadine. Bilastine was significantly superior to Desloratadine and rupatadine for flare inhibition from 1-24 hours (both p < .001) with an onset of action at 30 minutes. Bilastine was significantly better than Desloratadine (2-12 hours; at least p < .05) and rupatadine (2-9 hours; at least p < .01) for reducing itching sensation. Neither Desloratadine nor rupatadine significantly reduced itching compared to placebo. All active treatments were well tolerated. CONCLUSIONS: Bilastine 20 mg induced significantly greater inhibition of the W&F response compared with Desloratadine 5 mg and rupatadine 10 mg throughout the 24 hour study period, and had the fastest onset of action. Only bilastine significantly reduced itching sensation versus placebo.

The pharmacologic profile of desloratadine: a review.[Pubmed:11243504]

Allergy. 2001;56 Suppl 65:7-13.

Desloratadine is a new agent for the treatment of diseases such as seasonal allergic rhinitis and chronic urticaria. The pharmacologic profile of Desloratadine offers particular benefits in terms of histamine H1-receptor binding potency and H1 selectivity. Desloratadine has a half-life of 21-24 h, permitting once-daily dosing. No specific cautions are required with respect to administration in renal or hepatic failure, and food or grapefruit juice have no effect on the pharmacologic parameters. No clinically relevant racial or sex variations in the disposition of Desloratadine have been noted. In combination with the cytochrome P450 inhibitors, ketoconazole and erythromycin, the AUC and Cmax of Desloratadine were increased to a small extent, but no clinically relevant drug accumulation occurred. With high-dose treatment (45 mg/day for 10 days), no significant adverse events were observed, despite the sustained elevation of plasma Desloratadine levels. Specifically, Desloratadine had no effects on the corrected QT interval (QTc) when administered alone, at high dose, or in combination with ketoconazole or erythromycin. Preclinical studies also show that Desloratadine does not interfere with HERG channels or cardiac conduction parameters even at high dose. Desloratadine is nonsedating and free of antimuscarinic/anticholinergic effects in preclinical and clinical studies. Novel antiallergic and anti-inflammatory effects have also been noted with Desloratadine, a fact which may be relevant to its clinical efficacy.

Description

Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.

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