Ciraparantag (PER977) |
رقم الكتالوجGC32473
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Canonical SMILES | O=C(NCCCN1CCN(CCCNC([C@@H](N)CCCNC(N)=N)=O)CC1)[C@@H](N)CCCNC(N)=N | ||
| Formula | C22H48N12O2 | M.Wt | 512.7 |
| الذوبان | Water : ≥ 31 mg/mL (60.46 mM) | 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 | 1.9505 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 |
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 saline, 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% Appearance: A Jelly
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)