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| 25mg |
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Purity: ≥98%
Ticagrelor (formerly AZD-6140; AR-C 126532XX; AZD6140; AR-C126532XX; Trade name: Brilinta; Brilique; Possia) is the first reversibly binding, potent and orally bioactive P2Y12 receptor antagonist used as an antiplatelet and anticoagulant. It inhibits P2Y12 receptor with a Ki of 2 NM. Ticagrelor was approved in 2011 by FDA as an antiplatelet drug for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries. Like the thienopyridines prasugrel, clopidogrel and ticlopidine, ticagrelor blocks adenosine diphosphate (ADP) receptors of subtype P2Y12. In contrast to the other antiplatelet drugs, ticagrelor has a binding site different from ADP, making it an allosteric antagonist, and the blockage is reversible.
| ln Vitro |
Compared to other P2Y12R antagonists, ticagrelor encourages a higher suppression of adenosine 5′-diphosphate (ADP)-induced Ca2+ release in ischemic platelets. Beyond its antagonistic effects on P2Y12R, ticagrelor also inhibits the equilibrative nucleoside transporter 1 (ENT1) on platelets, which causes extracellular adenosine to accumulate and Gs-coupled adenosine A2A receptors to become activated[1]. When compared to mice treated with saline, B16-F10 cells show less interaction with platelets from mice treated with ticagrelor[2].
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| ln Vivo |
Mice given a therapeutic dose of ticagrelor (10 mg/kg) in B16-F10 melanoma intravenous and intrasplenic metastatic models show significant decreases in lung (84%) and liver (86%) metastases. In addition, animals treated with ticagrelor have higher survival rates than those treated with saline. Similar results are seen in a 4T1 breast cancer model, where ticagrelor therapy reduces lung (55%) and bone marrow (87%) metastases[2]. Titicagrelor (1–10 mg/kg) administered orally once has a dose-related inhibitory impact on platelet aggregation. When ticagrelor is administered at its maximum dosage of 10 mg/kg, platelet aggregation is significantly inhibited beginning one hour after medication and reaches its peak four hours later[3].
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| References |
[1]. Aungraheeta R, et al. Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood. 2016 Dec 8;128(23):2717-2728.
[2]. Gebremeskel S, et al. The reversible P2Y12 inhibitor ticagrelor inhibits metastasis and improves survival in mouse models of cancer. Int J Cancer. 2015 Jan 1;136(1):234-40. [3]. Sugidachi A, et al. A comparison of the pharmacological profiles of prasugrel and ticagrelor assessed by platelet aggregation, thrombus formation and haemostasis in rats. Br J Pharmacol. 2013 May;169(1):82-9 |
| Molecular Formula |
C23H28F2N6O4S
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| Molecular Weight |
522.57
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| CAS # |
274693-27-5
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| Related CAS # |
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| SMILES |
O[C@H]1[C@@H](O)[C@H](N2N=NC3=C(N[C@H]4[C@H](C5=CC=C(F)C(F)=C5)C4)N=C(SCCC)N=C32)C[C@@H]1OCCO
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| InChi Key |
OEKWJQXRCDYSHL-FNOIDJSQSA-N
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| InChi Code |
InChI=1S/C23H28F2N6O4S/c1-2-7-36-23-27-21(26-15-9-12(15)11-3-4-13(24)14(25)8-11)18-22(28-23)31(30-29-18)16-10-17(35-6-5-32)20(34)19(16)33/h3-4,8,12,15-17,19-20,32-34H,2,5-7,9-10H2,1H3,(H,26,27,28)/t12-,15+,16+,17-,19-,20+/m0/s1
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| Chemical Name |
(1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamino]-5-(propylthio)- 3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
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| Synonyms |
AZD 6140; AZD 6140; AR-C 126532XX; AR-C-126532XX; AZD-6140; AZD6140; AR-C126532XX; Ticagrelor; brand name: Brilinta; Brilique; Possia
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9136 mL | 9.5681 mL | 19.1362 mL | |
| 5 mM | 0.3827 mL | 1.9136 mL | 3.8272 mL | |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9136 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.
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