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Osalmid

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Category Hepatitis B Virus (HBV)
CAS 526-18-1
Description Osalmid is a ribonucleotide reductase small subunit M2 (RRM2) targeting compound that suppresses RRM2 activity in a concentration-dependent manner.
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Product Information

Synonyms Oxaphenamide; Osalmide
IUPAC Name 2-hydroxy-N-(4-hydroxyphenyl)benzamide
Molecular Weight 229.23
Molecular Formula C13H11NO3
Canonical SMILES C1=CC=C(C(=C1)C(=O)NC2=CC=C(C=C2)O)O
InChI InChI=1S/C13H11NO3/c15-10-7-5-9(6-8-10)14-13(17)11-3-1-2-4-12(11)16/h1-8,15-16H,(H,14,17)
InChIKey LGCMKPRGGJRYGM-UHFFFAOYSA-N
Boiling Point 350.8±27.0 °C at 760 mmHg
Melting Point 179°C
Flash Point 165.9±23.7 °C
Purity 99.85%
Density 1.4±0.1 g/cm3
Solubility In vitro:
10 mM in DMSO
Appearance White to off-white (Solid)
Storage Powder:
-20°C: 3 years
4°C: 2 years
In solvent:
-80°C: 6 months
-20°C: 1 month
Complexity 261
Exact Mass 229.07389321
Index Of Refraction 1.711
In Vitro Osalmid is identified as a potential ribonucleotide reductase small subunit M2 (RRM2) compound. Osalmid is 10-fold more active in inhibiting ribonucleotide reductase (RR) activity than hydroxyurea, and significantly inhibits HBV DNA and cccDNA synthesis in HepG2.2.15 cells in a time- and dose-dependent manner. After treatment for 8 days with Osalmid, the EC50 for HBV DNA inhibition are 11.1 μM for culture supernatant and 16.5 μM for cells. Osalmid suppresses RR activity in a concentration-dependent manner, with an IC50 of 8.23 μM. Osalmid is shown to possess potent activity against a 3TC-resistant HBV strain, suggesting utility in treating drug-resistant HBV infections.
In Vivo Osalmid reduces RR activity and HBV replication in HBV-transgenic mice and shows a synergistic efficacy with 3TC without significant toxicity. Oral dosing of osalmid at 400 mg/kg/d results in a time-dependent inhibition of HBV DNA replication. After treatment for 4 weeks, osalmid suppresses HBV DNA replication by about 40-45% as compared to the control in mouse sera and liver tissues.
PSA 69.56000
Target IC50: 8.23 μM (ribonucleotide reductase)
Vapor Pressure 0.0±0.8 mmHg at 25°C
XLogP3-AA 2.9

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