ホームページ Neuronal Signaling P2 Receptor antagonist Ticagrelor For research use only.

Ticagrelor

別名：AZD6140, AR-C 126532XX

Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

Ticagrelor化学構造

CAS No. 274693-27-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 70500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Ticagrelor関連製品

シグナル伝達経路

P2 Receptor Signaling Pathways

P2 Receptorシグナル伝達経路

P2 Receptor阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
H9c2 Function assay 0.1, 0,3 and 1 μM 24 h effective in reducing NCX1 reverse activity when lower concentrations 30721704
AsPC-1 Function assay 10 μM 2 h ticagrelor negated the platelet releasate effect on Akt, Erk activation and Slug upregulation 29064388
BxPC-3 Function assay 10 μM 2 h ticagrelor negated the platelet releasate effect on Akt, Erk activation and Slug upregulation 29064388
EAhy926 Apoptosis assay 40 μM and 60 μM decrease ox-LDL-induced apoptosis, particularly at a higher concentration 30592271
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生物活性

製品説明 Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.
特性 First-in-class of a new type of P2Y12 antagonist known as cyclopentyl-triazolo-pyrimidines.
Targets
P2Y12 [1]
2 nM(Ki)
In Vitro
In vitro

Ticagrelor is an active drug which, does not require metabolic activation after intestinal absorption. It does not compete directly with ADP at the ADP binding site but occupies an adjacent binding site and acts in an allosteric way, resulting in a reversible conformational change of the receptor. Ticagrelor binds reversibly to the receptor and exhibits rapid onset and offset of effect. Binding studies in rh-P2Y12 receptor-transfected CHO-K1 cells indicate that ticagrelor exhibits potent, rapid, and reversible binding, with a Kd of 10.5 nM, a kon (association constant) of 0.00011/(nM•s), a koff (dissociation constant) of 0.00087/s, and half-life values of 4 min for binding and 14 min for unbinding, indicating that the magnitude of platelet inhibition is dependent on concentrations of drug available to bind platelets. [1]

Ticagrelor moderately inhibits CYP2C9 activity in human liver microsomes, while exhibiting little or no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C19, CYP2D6, and CYP2E1. In human liver microsomes, ticagrelor inhibits midazolam 4-hydroxylation, while activating 1_-hydroxylation of midazolam. Evaluated in fresh human hepatocytes, ticagrelor is not an inducer of CYP1A2 or CYP3A4. [3]
Kinase Assay Binding assays using P2Y12-transfected CHO-K1 or humanplatelet membranes
Membranes (5 μg of protein) are added to a 96-well plate containing [125I]AZ11931285 (125 pM), [3H]ADP (10 nM), or [33P]2MeS-ADP (62.5 pM), the required concentration of competitor, and a sufficient volume of buffer (50 mM Tris, 5 mM MgCl2, 50 mM NaCl, and 0.1% nucleotide-free BSA, pH 7.4) to bring the total volume in each well to 200 μL. Binding studies using platelet membranes and [3H]ADP are performed in the presence of 100 μM (final concentration) MRS2179 to prohibit binding to P2Y1. The signal-to-noise ratios for P2Y12-transfected CHO-K1 cells are approximately 14 for [3H]ADP (specific signal: 895 c.p.m.), 24 for [33P]2MeSADP (specific signal: 3308 c.p.m.), and 24 for [125I]AZ11931285 (specific signal: 3308 c.p.m.). For the studies using platelet membranes, the signal-to-noise ratios are approximately 2 for [33P]2MeS-ADP and [3H]ADP and 1.5 for [125I]AZ11931285, with a specific signal between 100 and 400 c.p.m. In this study, an incubation time of 1 h at 30 癈 is used to allow full equilibrium to be achieved. Thereafter, free radioligand is separated from bound radioligand and counted as described above.
細胞実験 細胞株 BMDMs
濃度 20 μM
反応時間 30 minutes
実験の流れ

Cells were treated with indicated concentration of drug for 30 minutes.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot VASP-P / VASP 27694321
In Vivo
In Vivo

Absorption of ticagrelor is rapid with t max of 1.3-2 h. And the Cmax and area under the plasma concentration-time curve from time 0 to infinity increases in an apparently dose-proportional manner over the dose range studied, indicating linear pharmacokinetics. The mean terminal-phase half-life (t1/2) is approximately 7-8.5 h for ticagrelor. Inhibition of platelet aggregation (IPA) is dose related and is nearly complete at 2 h at doses of 100-400 mg. Ticagrelor is well tolerated, with no serious or doserelated adverse events or notable changes in laboratory values observed. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05774431 Recruiting
Acute Myocardial Infarction
University Hospital Heidelberg|AstraZeneca
 March 13 2023 --
NCT05283356 Recruiting
Severe Aortic Valve Stenosis|Aortic Valve Stenosis|Transcatheter Aortic Valve Replacement (TAVR)|Transcatheter Aortic Valve Implantation (TAVI)
Fundacin Biomedica Galicia Sur
 January 21 2022 Phase 4

化学情報

分子量 522.57 化学式

C23H28F2N6O4S
CAS No. 274693-27-5 SDF Download Ticagrelor SDFをダウンロードする
Smiles CCCSC1=NC(=C2C(=N1)N(N=N2)C3CC(C(C3O)O)OCCO)NC4CC4C5=CC(=C(C=C5)F)F
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (191.36 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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