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Delparantag

CAS No. : 872454-31-4

MCE 站：Delparantag

产品活性：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。

研究领域：Metabolic Enzyme/Protease

作用靶点：Factor Xa

In Vitro: Delparantag is designed to restore coagulation by specifically binding to the pentasaccharide and disrupting UFH and LMWH interaction with antithrombin.
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.

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.
Plasma half-life elimination of Delparantag is between 3 and 5 min.

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