Ciraparantag (PER977)
(Synonyms: (2S,2'S)-N,N'-(1,4-哌嗪二基二-3,1-丙烷二基)二[2-氨基-5-[(氨基亚胺甲基)氨基]戊酰胺]) 目录号 : GC32473
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Ciraparantag (PER977)是一种小分子合成的水溶性广谱抗凝剂逆转剂。Ciraparantag通过非共价氢键和电荷相互作用与普通肝素、低分子量肝素、磺达肝癸钠以及直接Xa因子抑制剂和直接凝血酶抑制剂结合，从而中和其抗凝活性并恢复止血功能，且不表现出明显的促凝血作用。
Cas No.:1438492-26-2
Sample solution is provided at 25 µL, 10mM.
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Ciraparantag (PER977) is a small-molecule, synthetic, water-soluble broad-spectrum anticoagulant reversal agent. Ciraparantag binds to and neutralizes the anticoagulant activity of unfractionated heparin, low molecular weight heparin, fondaparinux, as well as direct factor Xa inhibitors and direct thrombin inhibitors through non-covalent hydrogen bonding and charge-charge interactions, thereby restoring hemostatic function without exhibiting significant procoagulant effects[1-2]. Ciraparantag is suitable for the management of anticoagulant reversal in patients experiencing severe bleeding or requiring urgent surgery due to anticoagulant therapy[3-4].
In vivo, in an SD rat tail transection bleeding model, a single intravenous injection of Ciraparantag (1.25–31.25mg/kg) was administered either at the reported time of peak concentration (Tmax) of the anticoagulant (pre-injury) or after the injury. The anticoagulants used included oral edoxaban (10mg/kg), oral dabigatran (37.5mg/kg), oral apixaban (3.125mg/kg), oral rivaroxaban (5mg/kg), intravenous unfractionated heparin (1–2.5mg/kg), or intravenous enoxaparin (10mg/kg). Ciraparantag significantly reduced blood loss in the rats[5].
References:
[1] Chan NC, Weitz JI. Ciraparantag as a potential universal anticoagulant reversal agent. Eur Heart J. 2022 Mar 7;43(10):993-995.
[2] Leentjens J, Middeldorp S, Jung C. A short review of ciraparantag in perspective of the currently available anticoagulant reversal agents. Drug Discov Today. 2022 Oct;27(10):103332.
[3] Ansell J, Bakhru S, Laulicht BE, et al. Ciraparantag reverses the anticoagulant activity of apixaban and rivaroxaban in healthy elderly subjects. Eur Heart J. 2022 Mar 7;43(10):985-992.
[4] Siegal DM. Ciraparantag: the next anticoagulant airbag? Blood. 2021 Jan 7;137(1):10-11.
[5] Ansell J, Laulicht BE, Bakhru SH, et al. Ciraparantag, an anticoagulant reversal drug: mechanism of action, pharmacokinetics, and reversal of anticoagulants. Blood. 2021 Jan 7;137(1):115-125.
Ciraparantag (PER977)是一种小分子合成的水溶性广谱抗凝剂逆转剂。Ciraparantag通过非共价氢键和电荷相互作用与普通肝素、低分子量肝素、磺达肝癸钠以及直接Xa因子抑制剂和直接凝血酶抑制剂结合，从而中和其抗凝活性并恢复止血功能，且不表现出明显的促凝血作用[1-2]。Ciraparantag可用于因抗凝药物治疗而发生严重出血或需紧急手术的患者的抗凝逆转管理[3-4]。
在体内，在SD大鼠尾横断出血模型中，单次静脉注射Ciraparantag（1.25–31.25mg/kg）于抗凝剂（口服依度沙班10mg/kg、口服达比加群37.5mg/kg、口服阿哌沙班3.125mg/kg、口服利伐沙班5mg/kg、静脉注射普通肝素1–2.5mg/kg或静脉注射依诺肝素10mg/kg）达峰浓度时（损伤前）或损伤后给药，Ciraparantag能显著减少大鼠的出血量[6]。
| Animal experiment [1]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were administered an anticoagulant (e.g., edoxaban, dabigatran, apixaban, rivaroxaban, UFH, or enoxaparin) orally or intravenously. Ciraparantag (1.25 to 31.25mg/kg) was administered intravenously, either at the reported Tmax of the anticoagulant (before a bleeding injury) or after a bleeding injury (tail transection or liver laceration). Blood loss volume or bleeding time was assessed. |
Dosage form | 1.25 to 31.25mg/kg; i.v.; Single injection. |
Applications | A single dose of Ciraparantag significantly reduced blood loss induced by a variety of anticoagulants. Ciraparantag produced a dose-dependent reversal of anticoagulation, restoring blood loss to baseline (sham) levels. Ciraparantag administered after a bleeding injury also significantly reduced blood loss. |
References: | |
| Cas No. | 1438492-26-2 | SDF | |
| 别名 | (2S,2'S)-N,N'-(1,4-哌嗪二基二-3,1-丙烷二基)二[2-氨基-5-[(氨基亚胺甲基)氨基]戊酰胺] | ||
| Canonical SMILES | O=C(NCCCN1CCN(CCCNC([C@@H](N)CCCNC(N)=N)=O)CC1)[C@@H](N)CCCNC(N)=N | ||
| 分子式 | C22H48N12O2 | 分子量 | 512.7 |
| 溶解度 | Water : ≥ 31 mg/mL (60.46 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9505 mL | 9.7523 mL | 19.5046 mL |
| 5 mM | 390.1 μL | 1.9505 mL | 3.9009 mL |
| 10 mM | 195 μL | 975.2 μL | 1.9505 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A Jelly
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet