TAK-024 |
| Catalog No.GC32594 |
TAK-024 es un inhibidor de plaquetas con IC50 de 31, 79 y 51 nM en humanos, monos y cobayos, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 186971-69-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.
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].
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].
[1]. Kitamura S, et al. Potent dibasic GPIIb/IIIa antagonists with reduced prolongation of bleeding time: synthesis and pharmacological evaluation of 2-oxopiperazine derivatives. J Med Chem. 2001 Jul 19;44(15):2438-50.
Cell experiment: | 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 Blood is withdrawn into a plastic syringe containing 3.8% (human and monkey) or 3.15% (guinea pig) sodium citrate (1:10 citrate/blood, v/v).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 variousconcentrations of TAK-024 (25 μL). The change in light transmittance is measured after the addition of aggregating agents (25 μL) to the cuvette[1]. |
Animal experiment: | 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]. |
References: [1]. Kitamura S, et al. Potent dibasic GPIIb/IIIa antagonists with reduced prolongation of bleeding time: synthesis and pharmacological evaluation of 2-oxopiperazine derivatives. J Med Chem. 2001 Jul 19;44(15):2438-50. | |
| Cas No. | 186971-69-7 | SDF | |
| Canonical 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 | ||
| Formula | C27H34N10O6 | M.Wt | 594.62 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6817 mL | 8.4087 mL | 16.8175 mL |
| 5 mM | 336.3 μL | 1.6817 mL | 3.3635 mL |
| 10 mM | 168.2 μL | 840.9 μL | 1.6817 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *