TAK-024
TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.
For research use only. We do not sell to patients.
- CAS No.: 186971-69-7
- Formula: C27H34N10O6
- Molecular Weight:594.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 31 nM (human platelet), 79 nM (monkey platelet), 51 nM (pig platelet)[1]
TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively. In a preliminary experiment, the IC50 value of TAK-024 in the heparinized blood sample is 230 nM, 4.5-fold less potent than that in the citrated physiological blood sample. The ID50 value of TAK-024 on ex vivo ADP-induced platelet aggregation in guinea pigs is 0.18 μg/kg/min, the dissociation ratio of TAK-024 is found to be 32[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 186971-69-7
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Molecular Weight 594.62
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Formula C27H34N10O6
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SMILES
O=C(O)CN1C([C@H](CCCNC(C2=CC=C(NC(N)=N)C=C2)=O)N(C(CNC(C3=CC=C(NC(N)=N)C=C3)=O)=O)CC1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
Blood is collected from guinea pigs and used in this study. Blood is withdrawn into a plastic syringe containing 3.8% (human and monkey) or 3.15% (guinea pig) sodium citrate (1:10 citrate/blood, v/v). Platelet rich plasma (PRP) and platelet poor plasma (PPP) are obtained by centrifugation at 1000 g for 3 to 5 s and 1000 g for 20 min at room temperature, respectively. PRP (250 μL), in a cuvette stirred at 1000 rpm, is prewarmed for 2 min at 37°C with various concentrations of TAK-024 (25 μL). The change in light transmittance is measured after the addition of aggregating agents (25 μL) to the cuvette[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male guinea pigs (250 to 400 g) are used in this study. TAK-024 is given as continuous iv infusions, and the vehicle is given to the control animals. Ninety minutes after starting the infusion, citrated blood is collected from the abdominal aorta under anesthesia, and Platelet rich plasma (PRP) is prepared. As the aggregation inducer, ADP (20 μL, submaximal concentration) is used. The bleeding time (BT) is also examined 90 min after starting the infusion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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