872454-31-4
872454-31-4 structure
- Name: Delparantag
- Chemical Name: N-[(2S)-6-amino-1-[3-[[(2S)-6-amino-1-[3-[[(2S)-6-amino-1-(3-carbamoyl-4-methoxyanilino)-1-oxohexan-2-yl]carbamoyl]-4-methoxyanilino]-1-oxohexan-2-yl]carbamoyl]-4-methoxyanilino]-1-oxohexan-2-yl]-5-[[(2S)-2,6-diaminohexanoyl]amino]-2-methoxybenzamide
- CAS Number: 872454-31-4
- Molecular Formula: C56H79N13O12
- Molecular Weight: 1126.31000
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Factor Xa
- Create Date: 2017-07-20 13:18:12
- Modify Date: 2024-03-03 14:08:25
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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].
| Name | N-[(2S)-6-amino-1-[3-[[(2S)-6-amino-1-[3-[[(2S)-6-amino-1-(3-carbamoyl-4-methoxyanilino)-1-oxohexan-2-yl]carbamoyl]-4-methoxyanilino]-1-oxohexan-2-yl]carbamoyl]-4-methoxyanilino]-1-oxohexan-2-yl]-5-[[(2S)-2,6-diaminohexanoyl]amino]-2-methoxybenzamide |
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| Synonyms | delparantag |
| Description | 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]. |
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| Related Catalog | |
| 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]. |
| 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]. 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. |
| References |
| Molecular Formula | C56H79N13O12 |
|---|---|
| Molecular Weight | 1126.31000 |
| Exact Mass | 1125.60000 |
| PSA | 439.23000 |
| LogP | 11.52110 |