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25mg | ||
50mg | ||
100mg | ||
250mg |
Purity: ≥98%
TAK-024 is a novel and potent platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively. It showed a potent inhibitory effect on platelet aggregation and good dissociation between the efficacy and the bleeding side effect. Intravenous infusion of compound TAK-024 at 1.6 microg/mL/min completely prevented arterial thrombus formation induced by endothelial injury in guinea pigs. The dose of TAK-024 that prolonged the bleeding time to three times the control value was 5.8 microg/mL/min. These results suggest that compound TAK-024 might be useful in the clinical treatment of thrombotic diseases, and TAK-024 was selected as a candidate for the clinical trials.
ln Vitro |
The platelet inhibitor TAK-024 has IC50 values of 31, 79, and 51 nM in guinea pigs, humans, and monkeys, respectively. TAK-024's IC50 value in heparinized blood samples was found to be 230 nM in preliminary investigations. This value is 4.5 times lower than the IC50 in citrated physiological blood samples. TAK-024 has an ID50 value of 0.18 μg/kg/min on isolated ADP-induced guinea pig platelet aggregation and a dissociation ratio of 32 [1].
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ln Vivo |
In guinea pigs, endothelial injury-induced arterial thrombosis was entirely avoided by administering TAK-024 (compound 12c) intravenously at a rate of 1.6 μg/mL/min. Results indicated that TAK-024, with an ID50 value of 0.73 μg/kg/min, had an inhibitory impact on carotid artery thrombosis in guinea pigs caused by balloon damage. After 240 minutes, over 40% inhibition was still evident with a single intravenous dose of TAK-024 at 100 μg/kg, which produced nearly total inhibition in 120 minutes. Platelet aggregation can be dose-dependently inhibited with a single intravenous injection of 30 to 100 μg/kg TAK-024 [1].
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References |
J Med Chem.2001 Jul 19;44(15):2438-50.
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Molecular Formula |
C27H34N10O6
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Molecular Weight |
594.62226
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CAS # |
186971-69-7
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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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Synonyms |
TAK-024; TAK 024; TAK024
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6817 mL | 8.4087 mL | 16.8175 mL | |
5 mM | 0.3363 mL | 1.6817 mL | 3.3635 mL | |
10 mM | 0.1682 mL | 0.8409 mL | 1.6817 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.