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.
For research use only. We do not sell to patients.
- CAS No.: 872454-31-4
- Formula: C56H79N13O12
- Molecular Weight:1126.31
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
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.
-
Animal Model:Male Sprague-Dawley rats (250-275 g) injected with UFH or LMWH (2.0 mg/kg)[2]
-
Dosage:0.5 mg/kg, 1.0 mg/kg, or 2.0 mg/kg
-
Administration:Intravenous injection; once
-
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
-
CAS No. 872454-31-4
-
Molecular Weight 1126.31
-
Formula C56H79N13O12
-
Synonyms
PMX-60056
-
Sequence Shortening
K-{Oaa}-K-{Oaa}-K-{Oaa}-K
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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)
Powered by Bioz