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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- Formule: C21H20ClN3O6S2
- Masse moléculaire:509.98
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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Animal Model:C57BL/6 (male, diet-induced obesity via 16-week high-fat diet)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited ADP-induced platelet aggregation by 85% at 2 hours post-administration.
Sustained antiplatelet effect for 24 hours.
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Animal Model:New Zealand White (male, FeCl3-induced carotid artery injury)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.v.; single dose
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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.
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Animal Model:New Zealand White (male)[1]
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Dosage:1 mg/kg
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Administration:i.v.; single dose
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Result:Inhibited ADP-induced platelet aggregation by 72% at 1 hour post-administration.
Prolonged bleeding time by only 1.2-fold.
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Animal Model:New Zealand white (male, 1.9-2.4 kg)[2]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg
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Administration:i.v.，single dose
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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.
Chemical Information
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Masse moléculaire 509.98
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Formule C21H20ClN3O6S2
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Sun Y, et al. Computational Design of CYP102A1 Variants for Biosynthesis of a Next-Generation Antiplatelet Drug DT-678. ACS Synth Biol. 2026;15(3):1082-1089. [Content Brief]
[2]. Lauver DA, et al. DT-678 inhibits platelet activation with lower tendency for bleeding compared to existing P2Y12 antagonists. Pharmacol Res Perspect. 2019;7(4):e00509. Published 2019 Jul 25. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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