Cilostazol-d4 is intended for use as an internal standard for the quantification of cilostazol by GC- or LC-MS. Cilostazol is a phosphodiesterase 3A (PDE3A) inhibitor (IC50 = 0.2 µM for the platelet enzyme).1 It is selective for PDE3A over PDE1, -2, -4, and 5 (IC50s = >5 µM for all). Cilostazol inhibits collagen- or ADP-induced aggregation of isolated rabbit platelets (IC50s = 29 and 31 µM, respectively).2 In vivo, cilostazol (30 mg/kg) reduces thrombus formation by 84% in a mouse model of pulmonary thromboembolism. It reduces cardiac fibrosis and prevents the development of diastolic dysfunction and cardiac hypertrophy induced by a high-fat diet and angiotensin II in mice.3 Formulations containing cilostazol have been used in the treatment of the symptoms of intermittent claudication in peripheral vascular disease.
1.SchrÖr, K.The pharmacology of cilostazolDiabetes Obes. Metab.4 (Suppl 2)S14-S19(2002) 2.Koga, Y., Kihara, Y., Okada, M., et al.2(1H)-Quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activitiesBioorg. Med. Chem. Lett.8(12)1471-1476(1998) 3.Reddy, S.S., Agarwal, H., and Barthwal, M.K.Cilostazol ameliorates heart failure with preserved ejection fraction and diastolic dysfunction in obese and non-obese hypertensive miceJ. Mol. Cell. Cardiol.12346-57(2018)