A potent NS5A inhibitor
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Elbasvir

Item No. 24031

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N'-[[(6S)-6-phenyl-6H-indolo[1,2-c][1,3]benzoxazine-3,10-diyl]bis[1H-imidazole-5,2-diyl-(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-methylethyl)-2-oxo-2,1-ethanediyl]]]bis-carbamic acid, C,C'-dimethyl ester
CAS Number
1370468-36-2
Synonyms
  • MK-8742
Molecular Formula
C49H55N9O7
Formula Weight
882.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 20 mgm/lEthanol: 33 mg/mlEthanol:PBS (pH 7.2)(1:2): 0.33 mg/ml
λmax
284, 352, 369 nm
SMILES
O=C([C@H](C(C)C)NC(OC)=O)N(CCC1)[C@@H]1C(N2)=NC=C2C(C=C3)=CC4=C3N([C@H](C5=CC=CC=C5)OC6=C7C=CC(C8=CN=C([C@@H]9CCCN9C([C@@H](NC(OC)=O)C(C)C)=O)N8)=C6)C7=C4
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
InChi Key
BVAZQCUMNICBAQ-PZHYSIFUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Elbasvir is a direct-acting antiviral drug that potently inhibits hepatitis C virus (HCV) non-structural protein 5A (NS5A) with an EC50 value of 2.2 pM in Huh7 human liver cancer cells expressing pH77S.3/GLuc2A, a cell-culture adapted HCV16 genotype 1a derivative and luciferase reporter, following a 48-hour exposure in vitro.1,2 NS5A is essential for HCV RNA synthesis and viral assembly, and elbasvir inhibits the assembly of new viral replicase complexes when used at a concentration of 50 pM.2 It exhibits potent inhibitory activity against a broad range of HCV genotypes with EC50 values of 0.0002-34 nM in Huh7 cells expressing replicons of HCV genotype 4 NS5A and EC50 values of less than 0.2 nM for replicons from all other tested genotypes except 2b.3,1,4 Formulations containing elbasvir have been used alone and in combination with NS3/4A protease inhibitors in the treatment of HCV.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lahser, F.C., Bystol, K., Curry, S., et al. The combination of grazoprevir, a Hepatitis C virus (HCV) NS3/4A protease inhibitor, and elbasvir, an HCV NS5A inhibitor, demonstrates a high genetic barrier to resistance in HCV genotype 1a replicons. Antimicrob. Agents Chemother. 60(5), 2954-2964 (2016).

    2. McGivern, D.R., Masaki, T., Williford, S., et al. Kinetic analyses reveal potent and early blockade of hepatitis C virus assembly by NS5A inhibitors. Gastroenterology 147(2), 453-462 (2014).

    3. Asante-Appiah, E., Curry, S., McMonagle, P., et al. Antiviral activity and resistance analysis of NS3/4A protease inhibitor grazoprevir and NS5A inhibitor elbasvir in Hepatitis C virus GT4 replicons. Antimicrob. Agents Chemother. 61(7), e00363-e00417 (2017).

    4. Liu, R., Curry, S., McMonagle, P., et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir. Antimicrob. Agents Chemother. 59(11), 6922-6929 (2015).