Israpafant

• CAT Number: M018235
• CAS Number: 117279-73-9
• Molecular Formula: C28H29ClN4S
• Molecular Weight: 489.078
• Purity: ≥95%
• Target: Platelet-Activating Factor Receptor Antagonist
• Storage: Desiccate at -20C
• InChI: InChI=1S/C28H29ClN4S/c1-17(2)15-21-11-9-20(10-12-21)13-14-22-16-24-26(23-7-5-6-8-25(23)29)30-18(3)27-32-31-19(4)33(27)28(24)34-22/h5-12,16-18H,13-15H2,1-4H3
• InChIKey: RMSWMRJVUJSDGN-UHFFFAOYSA-N
• SMILES: CC1C2=NN=C(N2C3=C(C=C(S3)CCC4=CC=C(C=C4)CC(C)C)C(=N1)C5=CC=CC=C5Cl)C

Israpafant (also known as 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.