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CAS No. | 117279-73-9 | Cat. No. | BCP35479 |
Name | Israpafant | ||
Synonyms | Y-24180; Y 24180; Y24180; | ||
SMILES | CC1C2=NN=C(N2C3=C(C=C(S3)CCC4=CC=C(C=C4)CC(C)C)C(=N1)C5=CC=CC=C5Cl)C | ||
Chemical Name | |||
Formula | C28H29ClN4S | M. Wt | 489.08 |
Purity | 98% | Storage | Store at 4-8°C |
Description | Israpafant (Y-24180) is a drug which acts as a selective antagonist for the platelet-activating factor receptor, and was originally developed for the treatment of asthma. Its chemical structure is a thienotriazolodiazepines, closely related to the sedative benzodiazepine derivative etizolam. However, israpafant binds far more tightly to the platelet-activating factor receptor, with an IC50 of 0.84nM for inhibiting PAF-induced human platelet aggregation, while it binds only weakly to benzodiazepine receptors, with a Ki of 3680nM. Israpafant has been found to inhibit the activation of eosinophil cells and consequently delays the development of immune responses. It has also been shown to have anti-nephrotoxic properties and to mobilize calcium transport. |
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