LY 517717

• CAT Number: R052727
• CAS Number: 313489-71-3
• Molecular Formula: C27H33N5O2
• Molecular Weight: 459.594
• Purity: ≥95%
• Target: coagulation factor Xa inhibitor
• Storage: -20°C
• IUPAC Name: N-[(1R)-2-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-2-oxo-1-phenylethyl]-1H-indole-6-carboxamide
• InChI: InChI=1S/C27H33N5O2/c1-30-13-10-23(11-14-30)31-15-17-32(18-16-31)27(34)25(21-5-3-2-4-6-21)29-26(33)22-8-7-20-9-12-28-24(20)19-22/h2-9,12,19,23,25,28H,10-11,13-18H2,1H3,(H,29,33)/t25-/m1/s1
• InChIKey: VYNKVNDKAOGAAQ-RUZDIDTESA-N
• SMILES: CN1CCC(CC1)N2CCN(CC2)C(=O)C(C3=CC=CC=C3)NC(=O)C4=CC5=C(C=C4)C=CN5

LY 517717 is a coagulation factor Xa inhibitor potentially for the treatment of venous thromboembolism (VTE).

Reference

1: Agnelli G, Haas S, Ginsberg JS, Krueger KA, Dmitrienko A, Brandt JT. A phase II study of the oral factor Xa inhibitor LY517717 for the prevention of venous thromboembolism after hip or knee replacement. J Thromb Haemost. 2007 Apr;5(4):746-53. PubMed PMID: 17408408.2: Perzborn E. Factor Xa inhibitors–new anticoagulants for secondary haemostasis. Hamostaseologie. 2009 Aug;29(3):260-7. PubMed PMID: 19644596.3: Turpie AG. Oral, direct factor Xa inhibitors in development for the prevention and treatment of thromboembolic diseases. Arterioscler Thromb Vasc Biol. 2007 Jun;27(6):1238-47. Review. PubMed PMID: 17379841.4: Denas G, Pengo V. Investigational anticoagulants for hematological conditions: a new generation of therapies. Expert Opin Investig Drugs. 2013 Oct;22(10):1281-94. doi: 10.1517/13543784.2013.821463. Review. PubMed PMID: 23876036.5: Ahrens I, Peter K, Lip GY, Bode C. Development and clinical applications of novel oral anticoagulants. Part II. Drugs under clinical investigation. Discov Med. 2012 Jun;13(73):445-50. Review. PubMed PMID: 22742650.6: Bondarenko M, Curti C, Montana M, Rathelot P, Vanelle P. Efficacy and toxicity of factor Xa inhibitors. J Pharm Pharm Sci. 2013;16(1):74-88. Review. PubMed PMID: 23683607.7: Romualdi E, Ageno W. Investigational factor Xa inhibitors for thrombosis and acute coronary syndromes. Expert Opin Investig Drugs. 2011 Apr;20(4):495-505. doi: 10.1517/13543784.2011.562190. Review. PubMed PMID: 21385107.8: Norman P. Fragments 2007–what has fragment-based drug discovery delivered for medicinal chemistry? 7 March 2007, Cambridge, UK. IDrugs. 2007 May;10(5):313-6. PubMed PMID: 17487781.9: Harenberg J, Wehling M. Current and future prospects for anticoagulant therapy: inhibitors of factor Xa and factor IIa. Semin Thromb Hemost. 2008 Feb;34(1):39-57. doi: 10.1055/s-2008-1066023. Review. PubMed PMID: 18393142.10: Imberti D, Dall/’Asta C, Pierfranceschi MG. Oral factor Xa inhibitors for thromboprophylaxis in major orthopedic surgery: a review. Intern Emerg Med. 2009 Dec;4(6):471-7. doi: 10.1007/s11739-009-0293-9. Review. PubMed PMID: 19696978.11: Hampton T. New oral anticoagulants show promise. JAMA. 2006 Feb 15;295(7):743-4. PubMed PMID: 16478891.12: Imberti D, Prisco D. Oral factor Xa inhibitors for venous thromboembolism prevention in major orthopedic surgery: a review. Pathophysiol Haemost Thromb. 2008;36(5):217-26. doi: 10.1159/000252816. Review. PubMed PMID: 19996630.13: Turpie AG. New oral anticoagulants in atrial fibrillation. Eur Heart J. 2008 Jan;29(2):155-65. Review. PubMed PMID: 18096568.14: Kubitza D, Haas S. Novel factor Xa inhibitors for prevention and treatment of thromboembolic diseases. Expert Opin Investig Drugs. 2006 Aug;15(8):843-55. Review. PubMed PMID: 16859389.