Oral antiplatelet agent 1_product_DataBase

Bioactivity	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].
Target	IC50: 2.94 μM (antiplatelet aggregation)
Invitro	Oral antiplatelet agent 1 (compound 58l) moderately inhibits CYP3A4 with an IC50 of about 1.5 μM, but exhibits weak inhibition in the other main subtypes (IC50>25 μM)[1].Oral antiplatelet agent 1 does not inhibit hERG even at 40 μM, indicating that it has no QT interval prolongation-related cardiac toxicity[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:
Name	Oral antiplatelet agent 1
CAS	2299200-91-0
Formula	C23H24N4O5S
Molar Mass	468.53
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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):

PeptideDB

Oral antiplatelet agent 1

CAS: 2299200-91-0 F: C23H24N4O5S W: 468.53