Ticagrelor (Synonyms: 替卡格雷; AZD6140; AR-C 126532XX)

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Data Sheet SDS COA 产品使用指南技术支持

Ticagrelor (AZD6140) 是可逆的，具有口服活性的 P2Y12 受体拮抗剂，可用来研究血小板聚集。

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Ticagrelor Chemical Structure

CAS No. : 274693-27-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥550	In-stock
1 mg	￥156	In-stock
5 mg	￥312	In-stock
10 mg	￥500	In-stock
50 mg	￥714	In-stock
100 mg	￥1116	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

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Customer Review

Other Forms of Ticagrelor:

Ticagrelor-d₇ 询价
Ticagrelor (Standard) 询价

MCE 顾客使用本产品发表的 6 篇科研文献

Ticagrelor 相关产品

•相关化合物库:

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查看 P2Y Receptor 亚型特异性产品:

查看所有亚型

P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Ticagrelor (AZD6140) is a reversible oral P2Y12 receptor antagonist for the treatment of platelet aggregation.

IC₅₀ & Target

P2Y12 Receptor

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Platelet	IC₅₀	0.74 μM Compound: Ticagrelor	Antiplatelet activity against ADP-induced human platelet in platelet rich plasma assessed as inhibition of platelet aggregation preincubated for 2 mins followed by ADP stimulation and measured for 5 mins by aggregometry Antiplatelet activity against ADP-induced human platelet in platelet rich plasma assessed as inhibition of platelet aggregation preincubated for 2 mins followed by ADP stimulation and measured for 5 mins by aggregometry	[PMID: 34458743]
Platelet	IC₅₀	1.83 μM Compound: 1, AZD-6140	Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by 96-well format based turbidimetric method Inhibition of ADP-stimulated platelet aggregation in human platelet rich plasma by 96-well format based turbidimetric method	[PMID: 22984835]
Platelet	IC₅₀	2 μM Compound: Ticagrelor	Inhibition of collagen-induced platelet aggregation in human platelet preincubated for 5 mins followed by collagen-stimulation and measured after 6 mins by lumi-aggregometric method Inhibition of collagen-induced platelet aggregation in human platelet preincubated for 5 mins followed by collagen-stimulation and measured after 6 mins by lumi-aggregometric method	[PMID: 32155530]
Platelet	IC₅₀	4 μM Compound: Ticagrelor	Inhibition of TRAP6-induced platelet aggregation in human platelet preincubated for 5 mins followed by TRAP6-stimulation and measured after 6 mins by lumi-aggregometric method Inhibition of TRAP6-induced platelet aggregation in human platelet preincubated for 5 mins followed by TRAP6-stimulation and measured after 6 mins by lumi-aggregometric method	[PMID: 32155530]

体外研究
(In Vitro)

Ticagrelor 在血小板中比其他 P2Y12R 拮抗剂更有效地抑制腺苷 5′-二磷酸 (ADP) 诱导的 Ca²⁺ 释放。这种作用超越 P2Y12R 拮抗效应，部分是因为 Ticagrelor 抑制了血小板的核苷转运蛋白 1 (ENT1) ，导致细胞外腺苷积累并激活 Gs 耦合的腺苷 A2A 受体^[1]。与生理盐水处理的小鼠相比，Ticagrelor 处理的小鼠血小板与 B16-F10 细胞的相互作用减少^[2]。

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

体内研究
(In Vivo)

在 B16-F10 黑色素瘤静脉内和脾内转移模型中，用临床剂量Ticagrelor (10 mg/kg) 治疗的小鼠肺转移 (84%) 和肝转移 (86%) 明显减少。此外，与接受盐水治疗的动物相比，Ticagrelor 治疗可提高生存率。在 4T1 乳腺癌模型中也观察到了类似的效果，Ticagrelor 治疗后肺转移 (55%) 和骨髓转移 (87%) 减少^[2]。单次口服Ticagrelor (1-10 mg/kg) 可产生剂量相关的血小板聚集抑制作用。最高剂量 (10 mg/kg) 的Ticagrelor 在给药后 1 小时显着抑制血小板聚集，并在给药后 4 小时观察到峰值抑制^[3]。

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

Clinical Trial

分子量

522.57

Formula

C₂₃H₂₈F₂N₆O₄S

CAS 号

274693-27-5

性状

固体

颜色

Off-white to yellow

中文名称

替卡格雷；替格瑞洛

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (95.68 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (3.83 mM); 澄清溶液

此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (3.83 mM); 澄清溶液

此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (3.83 mM); 澄清溶液

此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light, stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.98% ee.: 100.00%

选择批次：

Data Sheet (652 KB) SDS (393 KB)

COA (291 KB) HNMR (209 KB) RP-HPLC (341 KB) LCMS (301 KB)

产品使用指南 (1538 KB)

参考文献

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Animal Administration ^[3]	Rats: Prasugrel (10 mg/kg, p.o.) and ticagrelor (30 mg/kg, p.o.), doses that produced similar levels of inhibition of platelet aggregation, are administered to rats 4 h before the bleeding time measurements. Fresh, washed platelets (1 × 1010 platelets/mL) are prepared from other rats and suspended in Hank's balanced salt solution. Platelets are transfused via the jugular vein to rats 1 h before the bleeding time measurements and the bleeding time is determined^[3]. ^[2]Mice: Female BALB/c mice are inoculated subcutaneously in the fourth mammary pad with 4T1 breast cancer cells. Once a tumor is palpable, mice receive daily injections of PBS or ticagrelor (10 mg/kg). One week later, mice undergo primary tumor resection. At 28 days mice are sacrificed and lungs, femurs and tibiae harvested. Dissociated cells from lung and bone marrow are plated in medium containing 60 μM 6-thioguanine. After 14 days, culture plates are fixed with methanol and stained with 0.03% methylene blue to enumerate metastatic 4T1 colonies^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Animal Administration
^[3]

Rats: Prasugrel (10 mg/kg, p.o.) and ticagrelor (30 mg/kg, p.o.), doses that produced similar levels of inhibition of platelet aggregation, are administered to rats 4 h before the bleeding time measurements. Fresh, washed platelets (1 × 1010 platelets/mL) are prepared from other rats and suspended in Hank's balanced salt solution. Platelets are transfused via the jugular vein to rats 1 h before the bleeding time measurements and the bleeding time is determined^[3].

^[2]Mice: Female BALB/c mice are inoculated subcutaneously in the fourth mammary pad with 4T1 breast cancer cells. Once a tumor is palpable, mice receive daily injections of PBS or ticagrelor (10 mg/kg). One week later, mice undergo primary tumor resection. At 28 days mice are sacrificed and lungs, femurs and tibiae harvested. Dissociated cells from lung and bone marrow are plated in medium containing 60 μM 6-thioguanine. After 14 days, culture plates are fixed with methanol and stained with 0.03% methylene blue to enumerate metastatic 4T1 colonies^[2].

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

参考文献

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Ticagrelor 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9136 mL	9.5681 mL	19.1362 mL	47.8405 mL
	5 mM	0.3827 mL	1.9136 mL	3.8272 mL	9.5681 mL
	10 mM	0.1914 mL	0.9568 mL	1.9136 mL	4.7840 mL
	15 mM	0.1276 mL	0.6379 mL	1.2757 mL	3.1894 mL
	20 mM	0.0957 mL	0.4784 mL	0.9568 mL	2.3920 mL
	25 mM	0.0765 mL	0.3827 mL	0.7654 mL	1.9136 mL
	30 mM	0.0638 mL	0.3189 mL	0.6379 mL	1.5947 mL
	40 mM	0.0478 mL	0.2392 mL	0.4784 mL	1.1960 mL
	50 mM	0.0383 mL	0.1914 mL	0.3827 mL	0.9568 mL
	60 mM	0.0319 mL	0.1595 mL	0.3189 mL	0.7973 mL
	80 mM	0.0239 mL	0.1196 mL	0.2392 mL	0.5980 mL

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Keywords:

Ticagrelor274693-27-5AZD6140 AR-C 126532XX替卡格雷替格瑞洛AZD 6140AZD-6140P2Y ReceptorInhibitorinhibitorinhibit

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Ticagrelor (Synonyms: 替卡格雷; AZD6140; AR-C 126532XX)

Customer Review

Other Forms of Ticagrelor:

Ticagrelor 相关抗体

MCE 顾客使用本产品发表的 6 篇科研文献

Ticagrelor 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 P2Y Receptor 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Ticagrelor 相关抗体:

摩尔计算器

稀释计算器

Ticagrelor 相关分类

完整储备液配制表

Keywords:

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