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.

Product information

CAS Number: 872454-31-4

Molecular Weight: 1126.31

Formula: C56H79N13O12

Chemical Name: 5-[(2S)-6-amino-2-({5-[(2S)-6-amino-2-({5-[(2S)-6-amino-2-({5-[(2S)-2,6-diaminohexanamido]-2-methoxyphenyl}formamido)hexanamido]-2-methoxyphenyl}formamido)hexanamido]-2-methoxyphenyl}formamido)hexanamido]-2-methoxybenzamide

Smiles: COC1=CC=C(C=C1C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)C1=CC(=CC=C1OC)NC(=O)[C@H](CCCCN)NC(=O)C1=CC(=CC=C1OC)NC(=O)[C@H](CCCCN)NC(=O)C1=CC(=CC=C1OC)NC(=O)[C@@H](N)CCCCN

InChiKey: PWFIFNGOPQUNIT-ITMZJIMRSA-N

InChi: InChI=1S/C56H79N13O12/c1-78-45-21-17-33(29-37(45)49(62)70)64-54(75)42(14-6-10-26-58)67-51(72)39-31-35(19-23-47(39)80-3)66-56(77)44(16-8-12-28-60)69-52(73)40-32-36(20-24-48(40)81-4)65-55(76)43(15-7-11-27-59)68-50(71)38-30-34(18-22-46(38)79-2)63-53(74)41(61)13-5-9-25-57/h17-24,29-32,41-44H,5-16,25-28,57-61H2,1-4H3,(H2,62,70)(H,63,74)(H,64,75)(H,65,76)(H,66,77)(H,67,72)(H,68,71)(H,69,73)/t41-,42-,43-,44-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.