Delparantag(Synonyms: PMX-60056)

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Delparantag;(Synonyms: PMX-60056)

Delparantag (PMX-60056) 是一种水杨酰胺衍生物，也是一种有效的普通肝素 (UFH) 和低分子量肝素 (LMWH) 逆转剂。Delparantag 具有中和 UFH 和 LMWH 的抗凝和止血作用的能力。

Delparantagamp;;(Synonyms: PMX-60056)

Delparantag Chemical Structure

CAS No. : 872454-31-4

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生物活性

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[1][2].

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Delparantag (PMX-60056; 0.5 mg/kg, 1.0 mg/kg, or 2.0 mg/kg; intravenous injection; once; male Sprague-Dawley rats) treatment neutralizes the antithrombotic, anticoagulant, and bleeding effects of heparins as effectively as protamine sulfate and may be slightly more efficacious against LMWHs[2].
Plasma half-life elimination of Delparantag is between 3 and 5 min[1].

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.

Clinical Trial

分子量

1126.31

Formula

C56H79N13O12
CAS 号

872454-31-4
Sequence Shortening

K-{Oaa}-K-{Oaa}-K-{Oaa}-K
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

    [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.