RO6889678
RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation.
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- CAS No.: 1578153-27-1
- Formule: C21H20ClFN4O5S
- Masse moléculaire:494.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
CYP3A4 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>30 μM
Compound: (R)-52
|
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay
|
[PMID: 29381358] |
| HepG2 2.2.15 | EC50 |
0.003 μM
Compound: HAP_R10
|
Antiviral activity against HBV stably transfected in human HepG2.2.15 cells assessed as reduction of HBV DNA replication incubated for 5 days by q-PCR analysis
Antiviral activity against HBV stably transfected in human HepG2.2.15 cells assessed as reduction of HBV DNA replication incubated for 5 days by q-PCR analysis
|
[PMID: 36896968] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1578153-27-1
-
Masse moléculaire 494.92
-
Formule C21H20ClFN4O5S
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SMILES
O=C([C@H]1N(CC2=C(C(OC)=O)[C@H](C3=CC=C(F)C=C3Cl)N=C(C4=NC=CS4)N2)CCOC1)O
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)