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  4. DT-678

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.

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DT-678

DT-678 Chemical Structure

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Description

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].

In Vivo

DT-678 (10 mg/kg; p.o.; single dose) produces 85% inhibition of ADP-induced platelet aggregation in diet-induced obese C57BL/6 mice, with sustained activity for 24 hours[1].
DT-678 (0.3-3 mg/kg; i.v.; single dose) reduces carotid artery thrombus weight by 42%, 68%, and 81%, respectively, in rabbits with FeCl3-induced arterial thrombosis[1].
DT-678 (1 mg/kg; i.v.; single dose) inhibits ADP-induced platelet aggregation by 72% in rabbits, with a 1.2-fold prolongation of bleeding time[1].
DT-678 (0.1-3.0 mg/kg; i.v.; single dose) dose-dependently inhibits ADP-induced rabbit platelet activation and aggregation, without significantly prolonging tongue bleeding times at equally effective antiplatelet doses[2].

MedChemExpress (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.
Molecular Weight

509.98

Formula

C21H20ClN3O6S2
SMILES

O=C(OC)[C@H](C1=C(Cl)C=CC=C1)N(C/C2=C/C(O)=O)CC[C@H]2SSC3=NC=CC=C3[N+]([O-])=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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DT-678 Related Classifications

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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:

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

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