Delparantag
Delparantag (PMX-60056) is a salicylamide derivative and an effective unfractionated heparin (UFH) and low molecular weight heparin (LMWH) reversing agent. Delparantag shows ability to neutralize the anticoagulation and bleeding effects of UFH and LMWH.
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- CAS No.: 872454-31-4
- Formule: C56H79N13O12
- Masse moléculaire:1126.31
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Delparantag is designed to restore coagulation by specifically binding to the pentasaccharide and disrupting UFH and LMWH interaction with antithrombin[1].
In heparinized plasma, Delparantag (PMX-60056) is more potent on a gravimetric basis than protamine at neutralizing both anti-Xa and anti-IIa activities. Delparantag is able to completely neutralize heparin at an approximate 2:1 gravimetric ratio. The amount of residual anti-IIa and anti-Xa activity was significantly less with Delparantag at a concentration of 50 mg/mL. In plasma anticoagulated with enoxaparin, Delparantag produces a concentration-dependent neutralization of anti-Xa activity. The amount of anti-Xa activity remaining after supplementation of the neutralizing agent is significantly less with Delparantag at concentrations above 25 mg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Plasma half-life elimination of Delparantag is between 3 and 5 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (250-275 g) injected with UFH or LMWH (2.0 mg/kg)[2]
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Dosage:0.5 mg/kg, 1.0 mg/kg, or 2.0 mg/kg
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Administration:Intravenous injection; once
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Result:Neutralizes the antithrombotic, anticoagulant, and bleeding effects of heparins as effectively as protamine sulfate and may be slightly more efficacious against LMWHs.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 872454-31-4
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Masse moléculaire 1126.31
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Formule C56H79N13O12
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Synonyms
PMX-60056
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Sequence Shortening
K-{Oaa}-K-{Oaa}-K-{Oaa}-K
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Mahan CE. A 1-year drug utilization evaluation of protamine in hospitalized patients to identify possible future roles of heparin and low molecular weight heparin reversal agents. J Thromb Thrombolysis. 2014 Apr;37(3):271-8. [Content Brief]
[2]. Kuziej J, et al. In vivo neutralization of unfractionated heparin and low-molecular-weight heparin by a novel salicylamide derivative. Clin Appl Thromb Hemost. 2010 Aug;16(4):377-86. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Delparantag Related Classifications
HY-105240 Related Classifications
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