| Hazard Information | Back Directory | [Description]
MIPS-9922 is a potent and selective PI3Kβ inhibitor with antiplatelet activity. MIPS-9922 potently inhibited ADP-induced washed platelet aggregation. It also inhibited integrin αIIbβ3 activation and αIIbβ3 dependent platelet adhesion to immobilized vWF under high shear. MIPS-9922 prevented arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis without inducing prolonged bleeding or excess blood loss. | [Uses]
MIPS-9922 is a potent and selective PI3Kβ inhibitor with an IC50 of 63 nM. MIPS-9922 inhibits PI3Kβ with >30-fold higher potency than PI3Kδ. MIPS-9922 blocks PI3K mediated activation of platelet glycoprotein αIIbβ3 activation and platelet adhesion in vitro. MIPS-9922 shows anti-platelet and anti-thrombotic activities[1]. | [in vivo]
MIPS-9922 (2.5 mg/kg, bolus jugular vein injection; once) prevents arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis without inducing prolonged bleeding or excess blood loss[1]. | Animal Model: | Male C57BL/6 mice bearing electrolytic injury[1] | | Dosage: | 2.5 mg/kg | | Administration: | Bolus jugular vein injection; once | | Result: | Prevented arterial thrombus formation in the in vivo electrolytic mouse model of thrombosis.
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| [IC 50]
PI3Kβ: 63 nM (IC50); PI3Kδ: 2200 nM (IC50) | [References]
[1] Zhaohua Zheng, et al. Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922). Eur J Med Chem. 2016 Oct 21:122:339-351. DOI:10.1016/j.ejmech.2016.06.010 |
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