Elinogrel
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MedKoo CAT#: 319823

CAS#: 936500-94-6 (free base)

Description: Elinogrel, also known as PRT 060128, is P2Y12 inhibitor. Similarly to ticagrelor and in contrast to clopidogrel, elinogrel was a reversible inhibitor that acted fast and short (for about 12 hours), and it was not a prodrug but pharmacologically active itself. The substance was used in form of its potassium salt, intravenously for acute treatment and orally for long-term treatment. Development was terminated in 2012.

Chemical Structure

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Elinogrel
CAS# 936500-94-6 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 319823
Name: Elinogrel
CAS#: 936500-94-6 (free base)
Chemical Formula: C20H15ClFN5O5S2
Exact Mass: 523.02
Molecular Weight: 523.938
Elemental Analysis: C, 45.85; H, 2.89; Cl, 6.77; F, 3.63; N, 13.37; O, 15.27; S, 12.24

Price and Availability

Size Price Availability Quantity
50mg USD 750 2 Weeks
100mg USD 1250 2 Weeks
200mg USD 1950 2 Weeks
500mg USD 3450 2 Weeks
1g USD 5850 2 Weeks
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Related CAS #: 936501-01-8 (potassium)   936500-94-6 (free base)    

Synonym: PRT 060128; PRT-060128; PRT060128; Elinogrel

IUPAC/Chemical Name: 5-chloro-N-((4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)phenyl)carbamoyl)thiophene-2-sulfonamide

InChi Key: LGSDFTPAICUONK-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H15ClFN5O5S2/c1-23-15-9-14-12(8-13(15)22)18(28)27(20(30)25-14)11-4-2-10(3-5-11)24-19(29)26-34(31,32)17-7-6-16(21)33-17/h2-9,23H,1H3,(H,25,30)(H2,24,26,29)

SMILES Code: O=C(NC1=CC=C(N2C(NC3=C(C=C(F)C(NC)=C3)C2=O)=O)C=C1)NS(=O)(C4=CC=C(Cl)S4)=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, not in water

Shelf Life: >2 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: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 523.94 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.

Recalculate based on batch purity %
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:

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1: Oestreich JH. Elinogrel, a reversible P2Y12 receptor antagonist for the treatment of acute coronary syndrome and prevention of secondary thrombotic events. Curr Opin Investig Drugs. 2010 Mar;11(3):340-8. PMID: 20178048.


2: Serebruany VL, Sibbing D, DiNicolantonio JJ. Dyspnea and reversibility of antiplatelet agents: ticagrelor, elinogrel, cangrelor, and beyond. Cardiology. 2014;127(1):20-4. doi: 10.1159/000354876. Epub 2013 Oct 26. PMID: 24192670.


3: Müller KAL, Geisler T, Gawaz M. Elinogrel, an orally and intravenously available ADP-receptor antagonist. Hamostaseologie. 2012;32(3):191-194. English. doi: 10.5482/ha-1192. Epub 2017 Dec 28. PMID: 29589361.


4: Bonadei I, Sciatti E, Vizzardi E, D'Aloia A, Raddino R, Metra M. New frontiers in the management of acute coronary syndromes: cangrelor and elinogrel. Recent Pat Cardiovasc Drug Discov. 2014;9(1):22-7. doi: 10.2174/1574890109666140610153605. PMID: 24915974.


5: Ueno M, Rao SV, Angiolillo DJ. Elinogrel: pharmacological principles, preclinical and early phase clinical testing. Future Cardiol. 2010 Jul;6(4):445-53. doi: 10.2217/fca.10.67. PMID: 20608816.


6: André P, DeGuzman F, Haberstock-Debic H, Mills S, Pak Y, Inagaki M, Pandey A, Hollenbach S, Phillips DR, Conley PB. Thienopyridines, but not elinogrel, result in off-target effects at the vessel wall that contribute to bleeding. J Pharmacol Exp Ther. 2011 Jul;338(1):22-30. doi: 10.1124/jpet.110.178574. Epub 2011 Mar 29. PMID: 21447613.


7: Müller KA, Geisler T, Gawaz M. Elinogrel, an orally and intravenously available ADP-receptor antagonist. How does elinogrel affect a personalized antiplatelet therapy? Hamostaseologie. 2012;32(3):191-4. doi: 10.5482/ha-1192. Epub 2012 Jul 5. PMID: 22772894.


8: Angiolillo DJ, Welsh RC, Trenk D, Neumann FJ, Conley PB, McClure MW, Stephens G, Kochman J, Jennings LK, Gurbel PA, Wójcik J, Dabrowski M, Saucedo JF, Stumpf J, Buerke M, Broderick S, Harrington RA, Rao SV. Pharmacokinetic and pharmacodynamic effects of elinogrel: results of the platelet function substudy from the intravenous and oral administration of elinogrel to evaluate tolerability and efficacy in nonurgent percutaneous coronary intervention patients (INNOVATE-PCI) trial. Circ Cardiovasc Interv. 2012 Jun;5(3):347-56. doi: 10.1161/CIRCINTERVENTIONS.111.965608. Epub 2012 May 22. PMID: 22619259.


9: Gurbel PA, Bliden KP, Antonino MJ, Stephens G, Gretler DD, Jurek MM, Pakyz RE, Shuldiner AR, Conley PB, Tantry US. The effect of elinogrel on high platelet reactivity during dual antiplatelet therapy and the relation to CYP2C19*2 genotype: first experience in patients. J Thromb Haemost. 2010 Jan;8(1):43-53. doi: 10.1111/j.1538-7836.2009.03648.x. Epub 2009 Oct 11. PMID: 19817997.


10: Welsh RC, Rao SV, Zeymer U, Thompson VP, Huber K, Kochman J, McClure MW, Gretler DD, Bhatt DL, Gibson CM, Angiolillo DJ, Gurbel PA, Berdan LG, Paynter G, Leonardi S, Madan M, French WJ, Harrington RA; INNOVATE-PCI Investigators. A randomized, double-blind, active-controlled phase 2 trial to evaluate a novel selective and reversible intravenous and oral P2Y12 inhibitor elinogrel versus clopidogrel in patients undergoing nonurgent percutaneous coronary intervention: the INNOVATE-PCI trial. Circ Cardiovasc Interv. 2012 Jun;5(3):336-46. doi: 10.1161/CIRCINTERVENTIONS.111.964197. Epub 2012 May 29. PMID: 22647518.


11: Berger JS, Roe MT, Gibson CM, Kilaru R, Green CL, Melton L, Blankenship JD, Metzger DC, Granger CB, Gretler DD, Grines CL, Huber K, Zeymer U, Buszman P, Harrington RA, Armstrong PW. Safety and feasibility of adjunctive antiplatelet therapy with intravenous elinogrel, a direct-acting and reversible P2Y12 ADP- receptor antagonist, before primary percutaneous intervention in patients with ST-elevation myocardial infarction: the Early Rapid ReversAl of platelet thromboSis with intravenous Elinogrel before PCI to optimize reperfusion in acute Myocardial Infarction (ERASE MI) pilot trial. Am Heart J. 2009 Dec;158(6):998-1004.e1. doi: 10.1016/j.ahj.2009.10.010. PMID: 19958867.


12: Schrör K. 'Reversible nature of platelet binding causing transfusion-related acute lung injury (TRALI) syndrome may explain dyspnea after ticagrelor and elinogrel' - a hypothesis that remains unproven. Thromb Haemost. 2012 Dec;108(6):1028-30. doi: 10.1160/TH12-07-0513. Epub 2012 Oct 16. PMID: 23070063.


13: Serebruany VL. Viewpoint: reversible nature of platelet binding causing transfusion-related acute lung injury (TRALI) syndrome may explain dyspnea after ticagrelor and elinogrel. Thromb Haemost. 2012 Dec;108(6):1024-7. doi: 10.1160/TH12-03-0180. Epub 2012 Oct 16. PMID: 23070029.


14: Michelson AD. New P2Y12 antagonists. Curr Opin Hematol. 2009 Sep;16(5):371-7. doi: 10.1097/MOH.0b013e32832ea2f2. PMID: 19550317.


15: Haberstock-Debic H, Andre P, Mills S, Phillips DR, Conley PB. A clopidogrel- insensitive inducible pool of P2Y12 receptors contributes to thrombus formation: inhibition by elinogrel, a direct-acting, reversible P2Y12 antagonist. J Pharmacol Exp Ther. 2011 Oct;339(1):54-61. doi: 10.1124/jpet.111.184143. Epub 2011 Jul 5. PMID: 21730013.


16: Caldeira D, Pinto FJ, Ferreira JJ. Dyspnea and reversibility profile of P2Y₁₂ antagonists: systematic review of new antiplatelet drugs. Am J Cardiovasc Drugs. 2014 Aug;14(4):303-11. doi: 10.1007/s40256-014-0071-6. PMID: 24659260.


17: Packard KA, Campbell JA, Knezevich JT, Davis EM. Emerging antiplatelet therapy for coronary artery disease and acute coronary syndrome. Pharmacotherapy. 2012 Mar;32(3):244-73. doi: 10.1002/j.1875-9114.2012.01021.x. PMID: 22392457.


18: Patel PA, Lane B, Augoustides JG. Progress in platelet blockers: the target is the P2Y12 receptor. J Cardiothorac Vasc Anesth. 2013 Jun;27(3):620-4. doi: 10.1053/j.jvca.2013.01.008. PMID: 23672863.


19: Michelson AD. Advances in antiplatelet therapy. Hematology Am Soc Hematol Educ Program. 2011;2011:62-9. doi: 10.1182/asheducation-2011.1.62. PMID: 22160013.


20: Klonaris C, Patelis N, Drebes A, Matheiken S, Liakakos T. Antiplatelet Treatment in Peripheral Arterial Disease: The Role of Novel Antiplatelet Agents. Curr Pharm Des. 2016;22(29):4610-4616. doi: 10.2174/1381612822666160607065109. PMID: 27281329.