| Identification | Back Directory | [Name]
RO6889678 | [CAS]
1578153-27-1 | [Synonyms]
RO6889678
3-Morpholinecarboxylic acid, 4-[[(6R)-6-(2-chloro-4-fluorophenyl)-3,6-dihydro-5-(methoxycarbonyl)-2-(2-thiazolyl)-4-pyrimidinyl]methyl]-, (3S)- | [Molecular Formula]
C21H20ClFN4O5S | [MDL Number]
MFCD30802197 | [MOL File]
1578153-27-1.mol | [Molecular Weight]
494.92 |
| Hazard Information | Back Directory | [Description]
RO6889678 is an inhibitor of HBV with a complex ADME profile. RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 μl/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 μl/min per mg protein, respectively. The induction potential of RO6889678 on cytochrome P450 (P450) enzymes and transporters at steady state was assessed and cotreatment with ritonavir revealed a complex drug-drug interaction with concurrent P450 inhibition and moderate UDP-glucuronosyltransferase induction. | [Uses]
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[1]. | [in vitro]
RO6889678 is a highly potent inhibitor of HBV capsid formation, with attributes that are favorable for targeting the liver while maintaining moderate peripheral exposure._x000D_
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Reference: J Pharmacol Exp Ther. 2018 May;365(2):237-248. https://pubmed.ncbi.nlm.nih.gov/29453199/ | [target]
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. | [IC 50]
CYP3A4 | [References]
[1] Nicole A Kratochwil, et al. Simultaneous Assessment of Clearance, Metabolism, Induction, and Drug-Drug Interaction Potential Using a Long-Term In Vitro Liver Model for a Novel Hepatitis B Virus Inhibitor. J Pharmacol Exp Ther. 2018 May;365(2):237-248. DOI:10.1124/jpet.117.245712 |
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Wuhan Topule
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+86-02787215551 +86-19945035818 |
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http://www.topule.com/ |
| Company Name: |
InvivoChem
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13549236410 |
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https://www.invivochem.cn/ |
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