DJT06001
DJT06001 is an orally active, highly selective Factor Xa inhibitor. DJT06001 shows inhibition with Ki of 0.99 nM, IC50 of 2.53 nM in prothrombinase complex and 3.33 nM in human plasma. DJT06001 dose-dependently prolongs PT and APTT, inhibits thrombus formation in vivo. DJT06001 can be used for the research of thromboembolic diseases.
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- CAS. Nr.: 1628182-40-0
- Formel: C21H20ClN3O5S
- Molecular Weight:461.92
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
DJT06001 (72a) potently inhibits human FXa with an IC50 of 4.71 nM[2].
DJT06001 exhibits > 20,000-fold selectivity for human FXa over other related serine proteases, with no detectable inhibition of off-target proteases at concentrations up to 100 μM[2].
DJT06001 displays potent ex vivo anticoagulant activity in rabbit plasma, doubling prothrombin time at 0.37 μM and activated partial thromboplastin time at 0.33 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DJT06001 (0.01-1.00 mg/kg; i.v.; single bolus) dose-dependently inhibits venous stasis-induced thrombus formation in male Sprague-Dawley rats with an ED50 of 0.1 mg/kg, with modest effects on clotting times at the ED50 dose[1].
DJT06001 (3.3-30 mg/kg; p.o.; single dose) dose-dependently increases bleeding time and bleeding amount in male Sprague-Dawley rats[1].
DJT06001 (2.5 mg/kg; p.o.; single dose) exhibits a strong correlation between plasma concentration, FXa activity inhibition, and PT prolongation in fasted male beagle dogs, with maximum FXa inhibition at 1 hour post-dose[1].
DJT06001 (2.5 mg/kg; p.o.; single dose) exhibits a strong correlation between plasma concentration, FXa activity inhibition, and PT prolongation in fasted male cynomolgus monkeys, with maximum FXa inhibition at 4 hours post-dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 210-240 g, arteriovenous-shunt thrombosis model)[1]
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Dosage:2 mg/kg; 4 mg/kg; 8 mg/kg; 16 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited thrombus formation dose-dependently with an ED50 of 4 mg/kg.
Reduced thrombus formation by approximately 44%, 58%, 67%, and 72% at 2, 4, 8, and 16 mg/kg, respectively.
Dose-dependently inhibited plasma FXa activity and prolonged PT and APTT.
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Animal Model:Sprague-Dawley (male, 210-240 g, venous stasis thrombosis model)[1]
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Dosage:0.01 mg/kg; 0.03 mg/kg; 0.10 mg/kg; 0.33 mg/kg; 1.00 mg/kg
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Administration:i.v.; single bolus
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Result:Inhibited venous stasis-induced thrombus formation dose-dependently with an ED50 of 0.1 mg/kg.
Reduced thrombus formation by approximately 20%, 38%, 58%, 82%, and 92% at 0.01, 0.03, 0.10, 0.33, and 1.00 mg/kg, respectively.
Dose-dependently inhibited plasma FXa activity and prolonged PT and APTT.
At its ED50 of 0.1 mg/kg, inhibited FXa activity by 44%, and prolonged PT and APTT by 1.1-fold each.
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Animal Model:Sprague-Dawley (male, 210-240 g, tail-bleeding model)[1]
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Dosage:3.3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Prolonged bleeding time and increased bleeding volume in a dose‑dependent manner.
Prolonged bleeding time by 1.8‑fold and increased bleeding volume by 1.1‑fold at 3.3 mg/kg.
Prolonged bleeding time by 2.5‑fold and increased bleeding volume by 1.3‑fold at 10 mg/kg, with significantly less bleeding than Rivaroxaban (HY-50903) at the same dose.
Prolonged bleeding time by 4.3‑fold and increased bleeding volume by 2.0‑fold at 30 mg/kg.
Chemical Information
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CAS. Nr. 1628182-40-0
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Molecular Weight 461.92
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Formel C21H20ClN3O5S
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SMILES
O=C1N2C3=CC=C(N4C(COCC4)=O)C=C3CC[C@@]2([H])[C@@H](O1)CNC(C5=CC=C(Cl)S5)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Hu X, et al. Characterization of a novel selective factor Xa inhibitor, DJT06001, which reduces thrombus formation with low risk of bleeding. Eur J Pharmacol. 2018;825:85-91. [Content Brief]
[2]. Xue T, et al. Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor. J Med Chem. 2014;57(18):7770-7791. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
DJT06001 Related Classifications
HY-182420 Related Classifications
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