2. GPCR/G Protein
  3. P2Y Receptor
  4. Oral antiplatelet agent 1

Oral antiplatelet agent 1 是一种有效的 P2Y12 受体 (P2Y12 receptor) 拮抗剂。Oral antiplatelet agent 1 具有良好的抗血小板聚集作用，IC50 为 2.94 μM，并在大鼠氯化铁致血栓模型中具有抗血栓作用。在大鼠尾出血模型中，Oral antiplatelet agent 1表现出比 Clopidogrel (HY-15283) 更佳的安全性。Oral antiplatelet agent 1 可用于血栓栓塞性疾病的研究。

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Oral antiplatelet agent 1 Chemical Structure

Oral antiplatelet agent 1 Chemical Structure

CAS No. : 2299200-91-0

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Oral antiplatelet agent 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

IC50: 2.94 μM (antiplatelet aggregation)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Platelet IC50
2.94 μM
Compound: 58l
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation by aggregometry
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation by aggregometry
[PMID: 30843696]
体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Oral antiplatelet agent 1 相关抗体:
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
分子量

468.53

Formula

C23H24N4O5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Oral antiplatelet agent 1 相关分类

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Oral antiplatelet agent 12299200-91-0Oral antiplatelet agent1Oral antiplatelet agent-1P2Y ReceptorClopidogrelantiplatelet aggregationthromboembolicantithromboticFeCl3tail-bleedingInhibitorinhibitorinhibit

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