ACH-806 - CAS 870142-71-5
Catalog number: 870142-71-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H20F3N3O2S
Molecular Weight:
411.45
COA:
Inquire
Targets:
HCV
Description:
ACH-806 is a Hepatitis C virus NS3 protein inhibitor. It can inhibit viral RNA replication in HCV replicon cells and is active in genotype 1 HCV-infected patients in a proof-of-concept clinical trial. But Phase-II for Hepatitis C treatment was discontinued.
Purity:
98%
Appearance:
Powder
Synonyms:
GS-9132; N-(((4-(pentyloxy)-3-(trifluoromethyl)phenyl)amino)thioxomethyl)-3-Pyridinecarboxamide,
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
HCV
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
WJSGOXONRXFGRY-UHFFFAOYSA-N
InChI:
1S/C19H20F3N3O2S/c1-2-3-4-10-27-16-8-7-14(11-15(16)19(20,21)22)24-18(28)25-17(26)13-6-5-9-23-12-13/h5-9,11-12H,2-4,10H2,1H3,(H2,24,25,26,28)
Canonical SMILES:
CCCCCOc1ccc(cc1C(F)(F)F)NC(=S)NC(=O)c2cccnc2
Current Developer:
Originator Achillion Pharmaceuticals
1.Selection of replicon variants resistant to ACH-806, a novel hepatitis C virus inhibitor with no cross-resistance to NS3 protease and NS5B polymerase inhibitors.
Yang W;Zhao Y;Fabrycki J;Hou X;Nie X;Sanchez A;Phadke A;Deshpande M;Agarwal A;Huang M Antimicrob Agents Chemother. 2008 Jun;52(6):2043-52. doi: 10.1128/AAC.01548-07. Epub 2008 Apr 14.
We have discovered a novel class of compounds active against hepatitis C virus (HCV), using a surrogate cellular system, HCV replicon cells. The leading compound in the series, ACH-806 (GS-9132), is a potent and specific inhibitor of HCV. The selection of resistance replicon variants against ACH-806 was performed to map the mutations conferring resistance to ACH-806 and to determine cross-resistance profiles with other classes of HCV inhibitors. Several clones emerged after the addition of ACH-806 to HCV replicon cells at frequencies and durations similar to that observed with NS3 protease inhibitors and NS5B polymerase inhibitors. Phenotypic analyses of these clones revealed that they are resistant to ACH-806 but remain sensitive to other classes of HCV inhibitors. Moreover, no significant change in the susceptibility to ACH-806 was found when the replicon cellular clones resistant to NS3 protease inhibitors and NS5B polymerase inhibitors were examined. Sequencing of the entire coding region of ACH-806-resistant replicon variants yielded several consensus mutations. Reverse genetics identified two single mutations in NS3, a cysteine-to-serine mutation at amino acid 16 and an alanine-to-valine mutation at amino acid 39, that are responsible for the resistance of the replicon variants to ACH-806.
2.Naturally occurring dominant resistance mutations to hepatitis C virus protease and polymerase inhibitors in treatment-naïve patients.
Kuntzen T;Timm J;Berical A;Lennon N;Berlin AM;Young SK;Lee B;Heckerman D;Carlson J;Reyor LL;Kleyman M;McMahon CM;Birch C;Schulze Zur Wiesch J;Ledlie T;Koehrsen M;Kodira C;Roberts AD;Lauer GM;Rosen HR;Bihl F;Cerny A;Spengler U;Liu Z;Kim AY;Xing Y;Schneidewind A;Madey MA;Fleckenstein JF;Park VM;Galagan JE;Nusbaum C;Walker BD;Lake-Bakaar GV;Daar ES;Jacobson IM;Gomperts ED;Edlin BR;Donfield SM;Chung RT;Talal AH;Marion T;Birren BW;Henn MR;Allen TM Hepatology. 2008 Dec;48(6):1769-78. doi: 10.1002/hep.22549.
Resistance mutations to hepatitis C virus (HCV) nonstructural protein 3 (NS3) protease inhibitors in <1% of the viral quasispecies may still allow >1000-fold viral load reductions upon treatment, consistent with their reported reduced replicative fitness in vitro. Recently, however, an R155K protease mutation was reported as the dominant quasispecies in a treatment-naïve individual, raising concerns about possible full drug resistance. To investigate the prevalence of dominant resistance mutations against specifically targeted antiviral therapy for HCV (STAT-C) in the population, we analyzed HCV genome sequences from 507 treatment-naïve patients infected with HCV genotype 1 from the United States, Germany, and Switzerland. Phylogenetic sequence analysis and viral load data were used to identify the possible spread of replication-competent, drug-resistant viral strains in the population and to infer the consequences of these mutations upon viral replication in vivo. Mutations described to confer resistance to the protease inhibitors Telaprevir, BILN2061, ITMN-191, SCH6 and Boceprevir; the NS5B polymerase inhibitor AG-021541; and to the NS4A antagonist ACH-806 were observed mostly as sporadic, unrelated cases, at frequencies between 0.
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CAS 870142-71-5 ACH-806

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