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Glecaprevir

SKU: orb1302067

Description

Glecaprevir

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

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Glecaprevir

Key Properties

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CAS Number1365970-03-1
MW838.87
Purity99.69%
FormulaC38H46F4N6O9S
SMILES[H][C@@]12C[C@H](N(C1)C(=O)[C@@H](NC(=O)O[C@]1([H])CCC[C@@]1([H])OC\C=C\C(F)(F)c1nc3ccccc3nc1O2)C(C)(C)C)C(=O)N[C@@]1(C[C@H]1C(F)F)C(=O)NS(=O)(=O)C1(C)CC1
TargetHCV Protease,SARS-CoV
SolubilityDMSO:130 mg/mL (154.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (4.77 mM)

Bioactivity

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Target IC50
3CLpro (SARS CoV):4.09 μM|the replication of stable HCV subgenomic replicons containing proteases from genotypes 1 to 6:0.21-4.6 nM (EC50)|HCV NS3/4A protease:3.5-11.3 nM|Huh7 cells:0.2 nM (EC50)
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In Vivo
The mean maximal decreases in HCV RNA levels from baseline were approximately 4 log10 IU/ml for all ABT-493 doses ranging from 100 mg to 700 mg and for ABT-530 doses of ≥ 40 mg. There were no meaningful differences in viral load declines for patients with versus without compensated cirrhosis. Twenty-four (50%) of the baseline samples from patients treated with ABT-493 had RAVs to NS3/4A protease inhibitors. Among 40 patients treated with ABT-530, 6 (15%) carried baseline RAVs to NS5A inhibitors .
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In Vitro
Glecaprevir (ABT-493) inhibited the enzymatic activity of purified NS3/4A proteases from HCV genotypes 1 to 6 in vitro (IC50: 3.5-11.3 nM) and the replication of stable HCV subgenomic replicons containing proteases from genotypes 1 to 6 (EC50: 0.21-4.6 nM). Glecaprevir had a median EC50 of 0.30 nM (range, 0.05 to 3.8 nM) for HCV replicons containing proteases from 40 samples from patients infected with HCV genotypes 1 to 5 .
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Cell Research
The activity of glecaprevir, paritaprevir, or grazoprevir against cells of nine cell lines each stably transfected with an HCV subgenomic replicon containing NS3 protease from a different HCV genotype was determined using a luciferase reporter assay as described previously. Five of these nine cell lines have been described previously, including those transfected with genotypes 1a H77, 1b Con1, 3a, 4a, and 6a. The other four cell lines were established by transfecting cells with a nonchimeric genotype 2a JFH-1 replicon, two genotype 2a JFH-1 chimeric replicons containing either a genotype 2b NS3 protease domain (N-terminal 251 amino acids) or a sequence encoding full-length NS3 through the first 39 amino acids of NS5B from genotype 5a (strain SA13), and one chimeric replicon with a genotype 1b Con1 backbone containing full-length NS3 and NS4A sequences from genotype 6e. The genotype 2b and 6e NS3 sequences were each synthetically constructed based on a consensus sequence derived from the alignment of 15 genotype 2b and 4 genotype 6e sequences, respectively. All replicon constructs were bicistronic subgenomic replicons similar to those described by Bartenschlager and coworkers, and the replicon cell lines were generated by introducing these constructs into cells of an Huh-7 human hepatoma-derived cell line. The inhibitory effect of the PIs on HCV replication in replicon cells was determined in Dulbecco's modified Eagle medium containing 5% fetal bovine serum with or without 40% human plasma. The EC50s were determined using nonlinear regression curve fitting as described previously .
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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ABT 493, ABT493, ABT-493, Glecaprevir, Hepatitis C virus, HCV, HCVProtease, HCV Protease, HCV NS3/4A protease, inhibit, Inhibitor, SARS-CoV, SARSCoV, SARS coronavirus

Similar Products

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  • Glecaprevir

    Glecaprevir [orb1226435]

    >98% (HPLC)

    1365970-03-1

    838.9

    C38H46F4N6O9S

    5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 2 mg, 1 g, 500 mg, 200 mg
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Compound Identifiers

PubChem CID
66828839 ↗

Key Properties

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No computed properties available.

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 80.00
5 mg
$ 100.00
1 ml x 10 mM (in DMSO)
$ 120.00
10 mg
$ 120.00
25 mg
$ 200.00
50 mg
$ 330.00
100 mg
$ 490.00
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