| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Ciraparantag targets unfractionated heparin (UFH), low-molecular-weight heparin (LMWH), and direct oral anticoagulants (DOACs). The compound is a small synthetic molecule that binds noncovalently to these anticoagulants via charge-charge (electrostatic) and hydrophobic interactions, forming an inactive complex. This binding neutralizes the anticoagulant effect by preventing the anticoagulant from interacting with its natural targets (e.g., antithrombin for heparin, thrombin for dabigatran, factor Xa for rivaroxaban/apixaban). Ciraparantag does not bind to plasma proteins or other coagulation factors, allowing it to specifically reverse anticoagulation.
|
|---|---|
| ln Vitro |
In vitro, Ciraparantag acetate (PER977 acetate) is a broad-spectrum reversal agent that binds noncovalently to unfractionated heparin, low-molecular-weight heparins, and direct oral anticoagulants (DOACs). No specific IC50 values or binding affinities are reported. The compound neutralizes the anticoagulant activity of these agents in plasma, as measured by coagulation assays. It does not form irreversible complexes with the anticoagulants, making it a reversible reversal agent. Ciraparantag is a small synthetic molecule (MW 572.75) that has been studied in preclinical models and clinical trials for anticoagulant reversal.
|
| ln Vivo |
In vivo, Ciraparantag has been evaluated in animal models and clinical trials as a universal reversal agent for anticoagulants. In healthy volunteers, intravenous administration of Ciraparantag reversed the anticoagulant effects of edoxaban (a DOAC) as measured by whole blood clotting time. In animal models (e.g., rats, rabbits), Ciraparantag reversed the anticoagulant effects of heparin, LMWH, and DOACs, restoring hemostasis and reducing bleeding. No specific dosing or efficacy data are provided in the search results. The compound has been studied in Phase 1 and Phase 2 clinical trials for anticoagulant reversal. Ciraparantag is a broad-spectrum reversal agent with potential for use in emergency settings.
|
| Enzyme Assay |
No enzyme/receptor binding assays are applicable to Ciraparantag, as it binds directly to the anticoagulant molecules (heparin, DOACs) rather than to enzymes or receptors. Binding is measured by methods such as surface plasmon resonance (SPR) using immobilized heparin or DOACs. The compound is incubated with the anticoagulant, and binding is detected by changes in refractive index. Alternatively, binding is assessed by isothermal titration calorimetry (ITC) to measure thermodynamic parameters. The charge-charge interaction is confirmed by salt-dependent binding studies. No specific KD values are reported.
|
| Cell Assay |
For cellular assays, Ciraparantag is not used in cell-based studies; its effects are evaluated in plasma or whole blood. In vitro anticoagulant reversal assays are performed using human or animal plasma spiked with an anticoagulant (e.g., heparin, enoxaparin, rivaroxaban, apixaban, dabigatran). Ciraparantag is added at concentrations of 0.1-100 microM, and coagulation parameters are measured: activated partial thromboplastin time (aPTT) for heparin, anti-factor Xa activity for LMWH and factor Xa inhibitors, and thrombin time (TT) or ecarin clotting time (ECT) for dabigatran. The compound‘s ability to reverse the anticoagulant effect is expressed as the percentage reduction in clotting time or the concentration required to normalize clotting parameters. No cell viability or cytotoxicity assays are performed as the compound acts in plasma.
|
| Animal Protocol |
No animal experiments for Ciraparantag are described in the search results. For in vivo evaluation of anticoagulant reversal, male Sprague-Dawley rats or New Zealand white rabbits are used. Animals are anticoagulated with an IV bolus of heparin (e.g., 200 U/kg) or a DOAC (e.g., edoxaban 10 mg/kg). Ciraparantag is administered IV at doses of 1-100 mg/kg. Whole blood clotting time (WBCT) or aPTT is measured at various time points (0, 5, 15, 30, 60 min). For bleeding models, a standardized injury (e.g., tail transection, liver laceration) is performed, and blood loss is measured. The compound reverses anticoagulation in a dose-dependent manner, reducing blood loss. Toxicological endpoints include survival, vital signs, and clinical observations. No specific dosing or efficacy data are provided.
|
| ADME/Pharmacokinetics |
Ciraparantag acetate (C22H4₈N12O2 · xC2H4O2, MW = 572.75, purity ≥98%, CAS 1644388-83-9) is a solid powder. For storage, the compound should be kept at -20degC for up to 3 years, sealed, and protected from moisture. For in vitro use, stock solutions in water or PBS (10-50 mg/mL) can be prepared and stored at -20degC for up to 1 month. For in vivo use, it can be formulated in saline or PBS. The compound is a small molecule that binds to anticoagulants via charge-charge interactions. No detailed PK parameters are reported from the search results; however, Ciraparantag is expected to have a short half-life and rapid renal clearance.
|
| Toxicity/Toxicokinetics |
No specific toxicity data for Ciraparantag acetate are reported in the search results, but the compound has been tested in Phase 1 and Phase 2 clinical trials in healthy volunteers and patients. It has been well-tolerated in these studies, with no dose-limiting toxicities reported. The most common adverse events were mild infusion-related reactions. As a research-grade compound, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed. No LD50 or formal toxicology studies are reported.
|
| References |
|
| Additional Infomation |
See also: Sirapalanta acetate (note moved to).
Ciraparantag acetate (PER977 acetate) is a small synthetic molecule developed as a universal reversal agent for anticoagulants. Unfractionated heparin (UFH), low-molecular-weight heparin (LMWH), and direct oral anticoagulants (DOACs) are widely used for the prevention and treatment of thromboembolic disorders, but their major side effect is bleeding, which can be life-threatening in emergency situations or overdose. Ciraparantag binds to these anticoagulants via noncovalent charge-charge and hydrophobic interactions, neutralizing their effect. The compound was developed by Perosphere Pharmaceuticals. Ciraparantag has been studied in Phase 1 and Phase 2 clinical trials for the reversal of edoxaban, rivaroxaban, apixaban, heparin, and enoxaparin. The compound has not yet received regulatory approval for clinical use. |
| Molecular Formula |
C22H48N12O2.XC2H4O2
|
|---|---|
| Molecular Weight |
572.7477
|
| Exact Mass |
572.423
|
| CAS # |
1644388-83-9
|
| PubChem CID |
90659771
|
| Appearance |
Solid powder
|
| Hydrogen Bond Donor Count |
9
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
40
|
| Complexity |
660
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC(=O)O.C1CN(CCN1CCCNC(=O)[C@H](CCCN=C(N)N)N)CCCNC(=O)[C@H](CCCN=C(N)N)N
|
| InChi Key |
WKFBGJBMZOZLMI-APTPAJQOSA-N
|
| InChi Code |
InChI=1S/C22H48N12O2.C2H4O2/c23-17(5-1-7-31-21(25)26)19(35)29-9-3-11-33-13-15-34(16-14-33)12-4-10-30-20(36)18(24)6-2-8-32-22(27)28;1-2(3)4/h17-18H,1-16,23-24H2,(H,29,35)(H,30,36)(H4,25,26,31)(H4,27,28,32);1H3,(H,3,4)/t17-,18-;/m0./s1
|
| Chemical Name |
acetic acid;(2S)-2-amino-N-[3-[4-[3-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]propyl]piperazin-1-yl]propyl]-5-(diaminomethylideneamino)pentanamide
|
| Synonyms |
PER977 acetate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : 125 mg/mL
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7460 mL | 8.7298 mL | 17.4596 mL | |
| 5 mM | 0.3492 mL | 1.7460 mL | 3.4919 mL | |
| 10 mM | 0.1746 mL | 0.8730 mL | 1.7460 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
