| Identification | Back Directory | [Name]
HEC 72702) | [CAS]
1793063-59-8 | [Synonyms]
HEC 72702) HEC72702
(HEC-72702 2-Morpholinepropanoic acid, 4-[[(6R)-6-(2-bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-3,6-dihydro-2-(2-thiazolyl)-4-pyrimidinyl]methyl]-, (2R)- | [Molecular Formula]
C24H26BrFN4O5S | [MDL Number]
MFCD32868931 | [MOL File]
1793063-59-8.mol | [Molecular Weight]
581.45 |
| Hazard Information | Back Directory | [Uses]
HEC72702 is a potent and orally active hepatitis B virus capsid inhibitor with an EC50 values of 0.039 μM. HEC72702 dose-dependently reduced HBV DNA in both the plasma and livers[1]. | [in vivo]
HEC72702 (50, 100 mg/kg; p.o.; daily for 7 days) dose-dependently reduces HBV DNA in both the plasma and livers copies[1]. Pharmacokinetic Parameters of HEC72702 in Male Sprague-Dawley rats[1].
| dose (mg/kg) | iv (2) | po (5) | | AUC(0-24 h) (h*ng/mL) | 4110 | 4900 | | CL (mL/min/kg) | 8.11 | | | VSS (L/kg) | 0.41 | | | F % | | 47.7 |
Male Sprague-Dawley rats, 2 mg/kg iv; 5 mg/kg po [1].
| Animal Model: | 6-7 weeks, 16-18 g, Female BALB/c mice(HDI mouse model)[1] | | Dosage: | 50, 100 mg/kg | | Administration: | P.o.; daily for 7 days | | Result: | Demonstrated a dose-dependent reduction of HBV DNA in the plasma of infected mice. |
| [References]
[1] Ren Q, et al. 3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4. J Med Chem. 2018 Feb 8;61(3):1355-1374. DOI:10.1021/acs.jmedchem.7b01914 |
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