| Identification | Back Directory | [Name]
Oral antiplatelet agent 1 | [CAS]
2299200-91-0 | [Synonyms]
Oral antiplatelet agent 1
4-Piperidinecarboxamide, 1-(3-cyano-5,7-dihydro-5-oxofuro[3,4-b]pyridin-2-yl)-4-methyl-N-[[(4-methylphenyl)methyl]sulfonyl]- | [Molecular Formula]
C23H24N4O5S | [MDL Number]
MFCD32062676 | [MOL File]
2299200-91-0.mol | [Molecular Weight]
468.53 |
| Hazard Information | Back Directory | [Uses]
Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders[1]. | [in vivo]
Oral antiplatelet agent 1 (2.5-80 mg/kg; p.o.; single dosage) decreases thrombus weight in FeCl3 thrombosis model rats[1].
Oral antiplatelet agent 1 (2.5-40 mg/kg; p.o.; single dosage) prolongs the bleeding time in tail-bleeding model rats[1].
Oral antiplatelet agent 1 exhibits great stability in both rat and human liver microsomes with the low clearance values and long half-life [human: T1/2=208.3 min, Clint=10.1 mL/(min g protein); rats: T1/2=89.1 min, Clint=10.6 mL/(min g protein)][1].
Oral antiplatelet agent 1 (5 mg/kg; p.o.; single dosage) exhibits excellent pharmacokinetic properties with relatively low clearance, high plasma exposure and good oral bioavailability in rats[1]. | Animal Model: | Male Wistar rats (250-300 g, n = 10; FeCl3 thrombosis model)[1] | | Dosage: | 2.5, 5, 10, 20, 40 and 80 mg/kg | | Administration: | p.o.; single dosage | | Result: | Decreased thrombus weight in a dose-dependent manner with an ED50 of 27 mg/kg compared to that of 7 mg/kg for Clopidogrel (HY-15283). |
| Animal Model: | Male rats (250-300 g, n = 10; tail-bleeding model)[1] | | Dosage: | 2.5, 5, 10, 20 and 40 mg/kg | | Administration: | p.o.; single dosage | | Result: | Prolonged the bleeding time in a dose-dependent manner. |
| Animal Model: | Male Sprague-Dawley rats (200-220g)[1] | | Dosage: | 5 mg/kg | | Administration: | p.o.; single dosage | | Result: | Pharmacokinetic Parameters of Oral antiplatelet agent 1 (compound 58l) in male Sprague-Dawley rats[1].
| Cmax (ng/mL) | T1/2 (h) | Tmax (h) | AUC0-∞ (ng·h/mL) | MRT (h) | | p.o. 5 mg/kg | 1661 ± 642 | 2.91 ± 1.09 | 0.25 | 4120 ± 2127 | 3.64 ± 0.18 |
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| [References]
[1] Kong D, et al. Optimization of P2Y12 Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties. J Med Chem. 2019 Mar 28;62(6): DOI:10.1021/acs.jmedchem.8b01971 |
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