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Desloratadine

Cat. No. M2621
Desloratadine Structure
Synonym:

Sch34117

Size Price Availability Quantity
50mg USD 50  USD50 In stock
100mg USD 75  USD75 In stock
500mg USD 280  USD280 In stock
1g USD 430  USD430 In stock
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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 310.82
Formula C19H19ClN2
CAS Number 100643-71-8
Solubility (25°C) DMSO 12 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jian Lu, et al. Antiallergic drug desloratadine as a selective antagonist of 5HT 2A receptor ameliorates pathology of Alzheimer's disease model mice by improving microglial dysfunction

[2] Syuji Yonekura, et al. Efficacy of Desloratadine and Levocetirizine in Patients with Cedar Pollen-Induced Allergic Rhinitis: A Randomized, Double-Blind Study

[3] Tadaho Nakamura, et al. Brain histamine H 1 receptor occupancy after oral administration of desloratadine and loratadine

[4] No authors listed. Desloratadine

[5] Philippe Devillier, et al. Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review

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