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  4. DT-678

DT-678 是一种具有口服活性的抗血小板和血栓抑制剂。DT-678 是通过混合二硫键，将 Clopidogrel (HY-15283) 的活性代谢物​与 3-硝基吡啶-2-硫醇​连接而成的共轭物。DT-678 不依赖于 CYP2C19 进行活化，在体内通过硫醇交换反应直接释放出活性物质，展现出优于 Clopidogrel 的疗效。DT-678 可用于急性冠状动脉综合征与血栓形成的相关研究。

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DT-678

DT-678 Chemical Structure

CAS No. : 2230703-82-7

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DT-678 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DT-678 is an orally active antiplatelet and antithrombotic inhibitor. DT-678 is a conjugate formed by linking the active metabolite of Clopidogrel (HY-15283) with 3-nitropyridine-2-thiol via a mixed disulfide bond. DT-678 does not rely on CYP2C19 for activation, and directly releases active substances via thiol exchange reactions in vivo, exhibiting superior efficacy over Clopidogrel. DT-678 can be used in research related to acute coronary syndrome and thrombosis[1][2].

体内研究
(In Vivo)

DT-678 (10 mg/kg；口服；单次给药) 可在饮食诱导肥胖的 C57BL/6 小鼠中对 ADP 诱导的血小板聚集产生 85% 的抑制作用，且活性可持续 24 小时[1]。
DT-678 (0.3-3 mg/kg; i.v.; single dose) 可使 FeCl3 诱导动脉血栓形成的家兔颈动脉血栓重量分别降低 42%、68% 和 81%[1]。
DT-678 (1 mg/kg；静脉注射；单次给药) 可抑制家兔体内由 ADP 诱导的血小板聚集，抑制率达 72%，同时可使出血时间延长 1.2 倍[1]。
DT-678 (0.1-3.0 mg/kg; 静脉推注；单次给药) 可剂量依赖性地抑制 ADP 诱导的兔血小板活化与聚集，且在等效抗血小板剂量下不会显著延长舌出血时间[2]。

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

Animal Model: C57BL/6 (male, diet-induced obesity via 16-week high-fat diet)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Inhibited ADP-induced platelet aggregation by 85% at 2 hours post-administration.
Sustained antiplatelet effect for 24 hours.
Animal Model: New Zealand White (male, FeCl3-induced carotid artery injury)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: i.v.; single dose
Result: Reduced carotid artery thrombus weight by 42% at 0.3 mg/kg i.v.
dose.
Reduced carotid artery thrombus weight by 68% at 1 mg/kg i.v.
dose.
Reduced carotid artery thrombus weight by 81% at 3 mg/kg i.v.
dose.
Animal Model: New Zealand White (male)[1]
Dosage: 1 mg/kg
Administration: i.v.; single dose
Result: Inhibited ADP-induced platelet aggregation by 72% at 1 hour post-administration.
Prolonged bleeding time by only 1.2-fold.
Animal Model: New Zealand white (male, 1.9-2.4 kg)[2]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg
Administration: i.v.，single dose
Result: Reduced percentage of double-positive (CD62P+ fibrinogen+) platelets to 5.96% from baseline 33.36% at 3.0 mg/kg.
Reduced ADP-induced ex vivo platelet aggregation to 27.2% from baseline 83.6% at 3.0 mg/kg.
Caused modest, statistically nonsignificant increases in tongue bleeding time to 155.6% and 172.2% of baseline at 1.0 mg/kg and 3.0 mg/kg, respectively.
Left arachidonic acid- and collagen-induced aggregation relatively unaffected.
分子量

509.98

Formula

C21H20ClN3O6S2
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

DT-678 相关分类

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  • 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:

DT-6782230703-82-7DT678DT 678Drug DerivativeDrug derivativeglutathioneacute coronary syndromesintegrin αIIbβ3platelet aggregationthrombosisCYP102A1 UD6 variantADPplatelet activationP-selectinplatelet P2Y12 receptorInhibitorinhibitorinhibit

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目录号：
HY-182012
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