1. GPCR/G Protein
  2. P2Y Receptor

TAK-024 

Cat. No.: HY-100254
Handling Instructions

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.

TAK-024 Chemical Structure

TAK-024 Chemical Structure

CAS No. : 186971-69-7

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.

IC50 & Target

IC50: 31 nM (human platelet), 79 nM (monkey platelet), 51 nM (pig platelet)[1]

In Vitro

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].

In Vivo

Intravenous infusion of TAK-024 (compound 12c) at 1.6 μg/mL/min completely prevents arterial thrombus formation induced by endothelial injury in guinea pigs. Results demonstrate the inhibitory effects of TAK-024 on the carotid thrombosis induced by balloon injury in guinea pigs and the ID50 value is 0.73 μg/kg/min. A single dose of TAK-024 at 100 μg/kg iv produces almost complete inhibition for 120 min, and about 40% inhibition is observed after 240 min. Dose-dependent inhibition of platelet aggregation is achieved with a single iv dose of 30 to 100 μg/kg of TAK-024[1].

References
Cell Assay
[1]

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 Blood is withdrawn into a plastic syringe containing 3.8% (human and monkey) or 3.15% (guinea pig) sodium citrate (1:10 citrate/blood, v/v).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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

594.62

Formula

C₂₇H₃₄N₁₀O₆

CAS No.

186971-69-7

SMILES

O=C(O)CN1C([[email protected]](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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TAK-024
Cat. No.:
HY-100254
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TAK-024

Cat. No.: HY-100254