2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. 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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DJT06001

DJT06001 Chemical Structure

CAS No. : 1628182-40-0

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DJT06001 Related Antibodies

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Description

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[1][2].

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-∞ F CLplasma Vss
Rat[2] 10 mg/kg p.o. 3020 ng/mL 2.3 h 3.54 h 14200 ng·h/mL 20.4 % / /
Rat[2] 3 mg/kg i.v. / / 0.74 h 20450 ng·h/mL / 0.149 L/h/kg 0.144 L/kg
In Vivo

DJT06001 (2-16 mg/kg; p.o.; single dose) dose-dependently inhibits arteriovenous-shunt thrombus formation in male Sprague-Dawley rats with an ED50 of 4 mg/kg, while also reducing plasma FXa activity and prolonging clotting times[1].
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.

Animal Model: Sprague-Dawley (male, 210-240 g, arteriovenous-shunt thrombosis model)[1]
Dosage: 2 mg/kg; 4 mg/kg; 8 mg/kg; 16 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Sprague-Dawley (male, 210-240 g, venous stasis thrombosis model)[1]
Dosage: 0.01 mg/kg; 0.03 mg/kg; 0.10 mg/kg; 0.33 mg/kg; 1.00 mg/kg
Administration: i.v.; single bolus
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.
Animal Model: Sprague-Dawley (male, 210-240 g, tail-bleeding model)[1]
Dosage: 3.3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

461.92

Formula

C21H20ClN3O5S
CAS No.
SMILES

O=C1N2C3=CC=C(N4C(COCC4)=O)C=C3CC[C@@]2([H])[C@@H](O1)CNC(C5=CC=C(Cl)S5)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DJT06001 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:

DJT060011628182-40-0DJT 06001DJT-06001Factor XaFxathrombus formationplatelet activating factorprothrombinase complexADPactivated partial thromboplastin timeprothrombin timeplatelet aggregationcollagenserine proteasesInhibitorinhibitorinhibit

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