WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H461183
CAS#: 959716-28-0 (free base)
Description: Pegnivacogin is an RNA aptamer inhibitor of coagulation factor IXa. Pegnivacogin is a polymer mixture.
Hodoodo Cat#: H461183
Name: Pegnivacogin
CAS#: 959716-28-0 (free base)
Chemical Formula:
Exact Mass: 0.00
Molecular Weight: 0.000
Elemental Analysis:
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Related CAS #: 959716-28-0 (free base); 959716-32-6 (Na)
Synonym: Pegnivacogin; RB 006; RB-006; RB006;
IUPAC/Chemical Name: bis(2-methoxyethyl) (6-oxo-6-((6-(phosphonooxy)hexyl)amino)hexane-1,5-diyl)dicarbamate
InChi Key: QGVYYLZOAMMKAH-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H40N3O11P/c1-30-13-15-32-19(25)22-11-7-5-9-17(23-20(26)33-16-14-31-2)18(24)21-10-6-3-4-8-12-34-35(27,28)29/h17H,3-16H2,1-2H3,(H,21,24)(H,22,25)(H,23,26)(H2,27,28,29)
SMILES Code: COCCOC(NCCCCC(C(NCCCCCCOP(O)(O)=O)=O)NC(OCCOC)=O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.03.00
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 0.00 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Vavalle JP, Rusconi CP, Zelenkofske S, Wargin WA, Ortel TL, Alexander JH, Povsic TJ, Becker RC. The effect of the REG2 Anticoagulation System on thrombin generation kinetics: a pharmacodynamic and pharmacokinetic first-in-human study. J Thromb Thrombolysis. 2014 Oct;38(3):275-84. doi: 10.1007/s11239-014-1081-6. PubMed PMID: 24880800.
2: Povsic TJ, Vavalle JP, Alexander JH, Aberle LH, Zelenkofske SL, Becker RC, Buller CE, Cohen MG, Cornel JH, Kasprzak JD, Montalescot G, Fail PS, Sarembock IJ, Mehran R; RADAR Investigators. Use of the REG1 anticoagulation system in patients with acute coronary syndromes undergoing percutaneous coronary intervention: results from the phase II RADAR-PCI study. EuroIntervention. 2014 Aug;10(4):431-8. doi: 10.4244/EIJY14M06_01. PubMed PMID: 24929350.
3: Povsic TJ, Wargin WA, Alexander JH, Krasnow J, Krolick M, Cohen MG, Mehran R, Buller CE, Bode C, Zelenkofske SL, Rusconi CP, Becker RC; RADAR Investigators. Pegnivacogin results in near complete FIX inhibition in acute coronary syndrome patients: RADAR pharmacokinetic and pharmacodynamic substudy. Eur Heart J. 2011 Oct;32(19):2412-9. doi: 10.1093/eurheartj/ehr179. Epub 2011 Jun 30. PubMed PMID: 21724623.
4: Ganson NJ, Povsic TJ, Sullenger BA, Alexander JH, Zelenkofske SL, Sailstad JM, Rusconi CP, Hershfield MS. Pre-existing anti-polyethylene glycol antibody linked to first-exposure allergic reactions to pegnivacogin, a PEGylated RNA aptamer. J Allergy Clin Immunol. 2016 May;137(5):1610-1613.e7. doi: 10.1016/j.jaci.2015.10.034. Epub 2015 Dec 11. PubMed PMID: 26688515; PubMed Central PMCID: PMC5819876.
5: Bel A, Borik W, Davidson S, Helies JM, Stimmer L, Fremes S, Zelenkofske S, Rusconi C, Alexander J, Alexander D, Menasché P, Pepper J. Inhibition of factor IXa by the pegnivacogin system during cardiopulmonary bypass: a potential substitute for heparin. A study in baboons. Eur J Cardiothorac Surg. 2016 Feb;49(2):682-9. doi: 10.1093/ejcts/ezv159. Epub 2015 May 7. PubMed PMID: 25953802.
6: Povsic TJ, Cohen MG, Chan MY, Zelenkofske SL, Wargin WA, Harrington RA, Alexander JH, Rusconi CP, Becker RC. Dose selection for a direct and selective factor IXa inhibitor and its complementary reversal agent: translating pharmacokinetic and pharmacodynamic properties of the REG1 system to clinical trial design. J Thromb Thrombolysis. 2011 Jul;32(1):21-31. doi: 10.1007/s11239-011-0588-3. PubMed PMID: 21503856.
7: Vavalle JP, Rusconi CP, Zelenkofske S, Wargin WA, Alexander JH, Becker RC. A phase 1 ascending dose study of a subcutaneously administered factor IXa inhibitor and its active control agent. J Thromb Haemost. 2012 Jul;10(7):1303-11. doi: 10.1111/j.1538-7836.2012.04742.x. PubMed PMID: 22500821.
8: Lincoff AM, Mehran R, Povsic TJ, Zelenkofske SL, Huang Z, Armstrong PW, Steg PG, Bode C, Cohen MG, Buller C, Laanmets P, Valgimigli M, Marandi T, Fridrich V, Cantor WJ, Merkely B, Lopez-Sendon J, Cornel JH, Kasprzak JD, Aschermann M, Guetta V, Morais J, Sinnaeve PR, Huber K, Stables R, Sellers MA, Borgman M, Glenn L, Levinson AI, Lopes RD, Hasselblad V, Becker RC, Alexander JH; REGULATE-PCI Investigators. Effect of the REG1 anticoagulation system versus bivalirudin on outcomes after percutaneous coronary intervention (REGULATE-PCI): a randomised clinical trial. Lancet. 2016 Jan 23;387(10016):349-356. doi: 10.1016/S0140-6736(15)00515-2. Epub 2015 Nov 5. Erratum in: Lancet. 2016 Mar 19;387(10024):1162. Boudoulas, Dean [corrected to Boudoulas, Konstantinos D.]. PubMed PMID: 26547100.
9: Povsic TJ, Lawrence MG, Lincoff AM, Mehran R, Rusconi CP, Zelenkofske SL, Huang Z, Sailstad J, Armstrong PW, Steg PG, Bode C, Becker RC, Alexander JH, Adkinson NF, Levinson AI; REGULATE-PCI Investigators. Pre-existing anti-PEG antibodies are associated with severe immediate allergic reactions to pegnivacogin, a PEGylated aptamer. J Allergy Clin Immunol. 2016 Dec;138(6):1712-1715. doi: 10.1016/j.jaci.2016.04.058. Epub 2016 Jul 14. PubMed PMID: 27522158.
10: Povsic TJ, Vavalle JP, Aberle LH, Kasprzak JD, Cohen MG, Mehran R, Bode C, Buller CE, Montalescot G, Cornel JH, Rynkiewicz A, Ring ME, Zeymer U, Natarajan M, Delarche N, Zelenkofske SL, Becker RC, Alexander JH; RADAR Investigators. A Phase 2, randomized, partially blinded, active-controlled study assessing the efficacy and safety of variable anticoagulation reversal using the REG1 system in patients with acute coronary syndromes: results of the RADAR trial. Eur Heart J. 2013 Aug;34(31):2481-9. doi: 10.1093/eurheartj/ehs232. Epub 2012 Aug 2. PubMed PMID: 22859796; PubMed Central PMCID: PMC3895957.
11: Povsic TJ, Cohen MG, Mehran R, Buller CE, Bode C, Cornel JH, Kasprzak JD, Montalescot G, Joseph D, Wargin WA, Rusconi CP, Zelenkofske SL, Becker RC, Alexander JH. A randomized, partially blinded, multicenter, active-controlled, dose-ranging study assessing the safety, efficacy, and pharmacodynamics of the REG1 anticoagulation system in patients with acute coronary syndromes: design and rationale of the RADAR Phase IIb trial. Am Heart J. 2011 Feb;161(2):261-268.e1-2. doi: 10.1016/j.ahj.2010.10.022. PubMed PMID: 21315207.
12: Rice NT, Szlam F, Varner JD, Bernstein PS, Szlam AD, Tanaka KA. Differential Contributions of Intrinsic and Extrinsic Pathways to Thrombin Generation in Adult, Maternal and Cord Plasma Samples. PLoS One. 2016 May 19;11(5):e0154127. doi: 10.1371/journal.pone.0154127. eCollection 2016. PubMed PMID: 27196067; PubMed Central PMCID: PMC4873248.
13: Capodanno D. Emerging strategies for rapid reversal of anticoagulation in patients undergoing catheter-based interventions: aptamers enter the RADAR. EuroIntervention. 2014 Aug;10(4):425-7. doi: DOI: 10.4244/EIJV10I4A74. PubMed PMID: 25138180.
14: Staudacher DL, Putz V, Heger L, Reinöhl J, Hortmann M, Zelenkofske SL, Becker RC, Rusconi CP, Bode C, Ahrens I. Direct factor IXa inhibition with the RNA-aptamer pegnivacogin reduces platelet reactivity in vitro and residual platelet aggregation in patients with acute coronary syndromes. Eur Heart J Acute Cardiovasc Care. 2017 Apr 1:2048872617703065. doi: 10.1177/2048872617703065. [Epub ahead of print] PubMed PMID: 28403626.
15: Ganetsky VS, Hadley DE, Thomas TF. Role of novel and emerging oral anticoagulants for secondary prevention of acute coronary syndromes. Pharmacotherapy. 2014 Jun;34(6):590-604. doi: 10.1002/phar.1375. Epub 2013 Dec 13. Review. PubMed PMID: 24338703.
16: Gomez-Outes A, Suarez-Gea ML, Lecumberri R, Terleira-Fernandez AI, Vargas-Castrillon E. Specific antidotes in development for reversal of novel anticoagulants: a review. Recent Pat Cardiovasc Drug Discov. 2014;9(1):2-10. Review. PubMed PMID: 25494843.
17: Ahrens I, Bode C, Zirlik A. Anticoagulation during and after acute coronary syndrome. Hamostaseologie. 2014;34(1):72-7. doi: 10.5482/HAMO-13-09-0048. Epub 2013 Dec 13. Review. PubMed PMID: 24337310.
18: Vavalle JP, Cohen MG. The REG1 anticoagulation system: a novel actively controlled factor IX inhibitor using RNA aptamer technology for treatment of acute coronary syndrome. Future Cardiol. 2012 May;8(3):371-82. doi: 10.2217/fca.12.5. Epub 2012 Mar 15. Review. PubMed PMID: 22420328; PubMed Central PMCID: PMC3739693.
19: Eikelboom JW, Zelenkofske SL, Rusconi CP. Coagulation factor IXa as a target for treatment and prophylaxis of venous thromboembolism. Arterioscler Thromb Vasc Biol. 2010 Mar;30(3):382-7. doi: 10.1161/ATVBAHA.110.203117. Epub 2010 Feb 5. Review. PubMed PMID: 20139356.
20: Szlam F, Luan D, Bolliger D, Szlam AD, Levy JH, Varner JD, Tanaka KA. Anti-factor IXa Aptamer reduces propagation of thrombin generation in plasma anticoagulated with warfarin. Thromb Res. 2010 May;125(5):432-7. doi: 10.1016/j.thromres.2009.11.018. Epub 2009 Dec 11. PubMed PMID: 20004955.
