WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H510306
CAS#: 1370468-36-2
Description: Elbasvir, also known as MK-8742, is a HCV NS5A inhibitor, which is currently in phase 2b clinical trials as part of an all-oral, interferon-free regimen for the treatment of HCV infection. The NS5A protein plays a critical role in the replication of HCV and has been the focus of numerous research efforts over the past few years. NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays, making them attractive components for inclusion in all oral combination regimens.
Hodoodo Cat#: H510306
Name: Elbasvir
CAS#: 1370468-36-2
Chemical Formula: C49H55N9O7
Exact Mass: 881.42
Molecular Weight: 882.020
Elemental Analysis: C, 66.72; H, 6.29; N, 14.29; O, 12.70
Synonym: MK8742; MK-8742; MK 8742; Elbasvir; Zepatier.
IUPAC/Chemical Name: Methyl ((1S)-1-(((2S)-2-(4-((6S)-10-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)pyrrolidin-2-yl)-1H-imidazol-4-yl)-6-phenyl-6H-indolo(1,2-c)(1,3)benzoxazin-3-yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)carbonyl)-2-methylpropyl)carbamate
InChi Key: BVAZQCUMNICBAQ-PZHYSIFUSA-N
InChi Code: InChI=1S/C49H55N9O7/c1-27(2)41(54-48(61)63-5)45(59)56-20-10-14-37(56)43-50-25-34(52-43)30-17-19-36-32(22-30)23-39-33-18-16-31(24-40(33)65-47(58(36)39)29-12-8-7-9-13-29)35-26-51-44(53-35)38-15-11-21-57(38)46(60)42(28(3)4)55-49(62)64-6/h7-9,12-13,16-19,22-28,37-38,41-42,47H,10-11,14-15,20-21H2,1-6H3,(H,50,52)(H,51,53)(H,54,61)(H,55,62)/t37-,38-,41-,42-,47-/m0/s1
SMILES Code: O=C(OC)N[C@H](C(N1[C@H](C2=NC(C3=CC=C4C(N5[C@H](C6=CC=CC=C6)OC4=C3)=CC7=C5C=CC(C8=CNC([C@H]9N(C([C@@H](NC(OC)=O)C(C)C)=O)CCC9)=N8)=C7)=CN2)CCC1)=O)C(C)C
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: |
The following data is based on the product molecular weight 882.02 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: Morikawa K, Nakamura A, Shimazaki T, Sakamoto N. Safety and efficacy of elbasvir/grazoprevir for the treatment of chronic hepatitis C: current evidence. Drug Des Devel Ther. 2018 Sep 5;12:2749-2756. doi: 10.2147/DDDT.S133697. eCollection 2018. Review. PubMed PMID: 30233138; PubMed Central PMCID: PMC6132225.
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3: Sulejmani N, Jafri SM. Grazoprevir/elbasvir for the treatment of adults with chronic hepatitis C: a short review on the clinical evidence and place in therapy. Hepat Med. 2018 May 4;10:33-42. doi: 10.2147/HMER.S130103. eCollection 2018. Review. PubMed PMID: 29765256; PubMed Central PMCID: PMC5942172.
4: Ahmed H, Abushouk AI, Menshawy A, Attia A, Mohamed A, Negida A, Abdel-Daim MM. Meta-Analysis of Grazoprevir plus Elbasvir for Treatment of Hepatitis C Virus Genotype 1 Infection. Ann Hepatol. 2018 January-February;17(1):18-32. doi: 10.5604/01.3001.0010.7532. Review. PubMed PMID: 29311409.
5: Karaoui LR, Mansour H, Chahine EB. Elbasvir-grazoprevir: A new direct-acting antiviral combination for hepatitis C. Am J Health Syst Pharm. 2017 Oct 1;74(19):1533-1540. doi: 10.2146/ajhp160558. Review. PubMed PMID: 28947524.
6: Al-Salama ZT, Deeks ED. Elbasvir/Grazoprevir: A Review in Chronic HCV Genotypes 1 and 4. Drugs. 2017 May;77(8):911-921. doi: 10.1007/s40265-017-0739-8. Review. PubMed PMID: 28417245.
7: Vallet-Pichard A, Pol S. Grazoprevir/elbasvir combination therapy for HCV infection. Therap Adv Gastroenterol. 2017 Jan;10(1):155-167. doi: 10.1177/1756283X16671293. Epub 2016 Oct 17. Review. PubMed PMID: 28286567; PubMed Central PMCID: PMC5330609.
8: Elbasvir/grazoprevir. Aust Prescr. 2017 Feb;40(1):32-34. doi: 10.18773/austprescr.2017.010. Epub 2017 Feb 1. Review. PubMed PMID: 28246435; PubMed Central PMCID: PMC5313242.
9: Papudesu C, Kottilil S, Bagchi S. Elbasvir/grazoprevir for treatment of chronic hepatitis C virus infection. Hepatol Int. 2017 Mar;11(2):152-160. doi: 10.1007/s12072-016-9761-2. Epub 2016 Sep 13. Review. Erratum in: Hepatol Int. 2017 May;11(3):315-316. PubMed PMID: 27624503.
10: El Kassas M, Elbaz T, Abd El Latif Y, Esmat G. Elbasvir and grazoprevir for chronic hepatitis C genotypes 1 and 4. Expert Rev Clin Pharmacol. 2016 Nov;9(11):1413-1421. doi: 10.1080/17512433.2016.1233813. Epub 2016 Sep 26. Review. PubMed PMID: 27603877.
11: Gamal N, Andreone P. Grazoprevir/elbasvir fixed-dose combination for hepatitis C. Drugs Today (Barc). 2016 Jul;52(7):377-85. doi: 10.1358/dot.2016.52.7.2510258. Review. PubMed PMID: 27540596.
12: Suraweera D, Weeratunga AN, Saab S. Spotlight on grazoprevir-elbasvir once-daily combination and its potential in the treatment of hepatitis C. Drug Des Devel Ther. 2016 Jun 29;10:2119-27. doi: 10.2147/DDDT.S90537. eCollection 2016. Review. PubMed PMID: 27418810; PubMed Central PMCID: PMC4933565.
13: Bell AM, Wagner JL, Barber KE, Stover KR. Elbasvir/Grazoprevir: A Review of the Latest Agent in the Fight against Hepatitis C. Int J Hepatol. 2016;2016:3852126. doi: 10.1155/2016/3852126. Epub 2016 Jun 15. Review. PubMed PMID: 27403342; PubMed Central PMCID: PMC4925941.
14: Pedraza F, Ladino M, Roth D. Impact of grazoprevir and elbasvir in the treatment of hepatitis C virus-infected patients with chronic kidney disease and end-stage renal disease. Clin Liver Dis (Hoboken). 2016 May 27;7(5):112-115. doi: 10.1002/cld.549. eCollection 2016 May. Review. PubMed PMID: 31041043; PubMed Central PMCID: PMC6490272.
15: Carrion AF, Martin P. Safety and efficacy of elbasvir and grazoprevir for treatment of hepatitis C. Expert Opin Drug Saf. 2016 Jun;15(6):883-90. doi: 10.1080/14740338.2016.1179278. Epub 2016 May 3. Review. PubMed PMID: 27091555.
16: Keating GM. Elbasvir/Grazoprevir: First Global Approval. Drugs. 2016 Apr;76(5):617-24. doi: 10.1007/s40265-016-0558-3. Review. PubMed PMID: 26943930.
17: Elbasvir/grazoprevir (Zepatier) for hepatitis C. Med Lett Drugs Ther. 2016 Feb 29;58(1489):25-7. Review. PubMed PMID: 26938699.
18: Alric L, Bonnet D. Grazoprevir + elbasvir for the treatment of hepatitis C virus infection. Expert Opin Pharmacother. 2016;17(5):735-42. doi: 10.1517/14656566.2016.1161028. Epub 2016 Mar 21. Review. PubMed PMID: 26933896.
19: Sulejmani N, Jafri SM, Gordon SC. Pharmacodynamics and pharmacokinetics of elbasvir and grazoprevir in the treatment of hepatitis C. Expert Opin Drug Metab Toxicol. 2016;12(3):353-61. doi: 10.1517/17425255.2016.1148685. Review. PubMed PMID: 26849059.
20: Landaverde C, Wells J, Hamner R, Goldstein JL. Dual therapy of grazoprevir and elbasvir for the treatment of hepatitis C infection. Expert Rev Gastroenterol Hepatol. 2016;10(4):419-29. doi: 10.1586/17474124.2016.1147346. Epub 2016 Feb 24. Review. PubMed PMID: 26818134.