CAS 526-18-1|osalmid
Introduction:Basic information about CAS 526-18-1|osalmid, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | osalmid | ||
|---|---|---|---|
| CAS Number | 526-18-1 | Molecular Weight | 229.231 |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 350.8±27.0 °C at 760 mmHg |
| Molecular Formula | C13H11NO3 | Melting Point | 179ºC |
| MSDS | / | Flash Point | 165.9±23.7 °C |
Names
| Name | 2-Hydroxy-N-(4-hydroxyphenyl)-benzamide |
|---|---|
| Synonym | More Synonyms |
osalmid BiologicalActivity
| Description | Osalmid is a ribonucleotide reductase small subunit M2 (RRM2) targeting compound; suppresses ribonucleotide reductase activity with an IC50 of 8.23 μM. |
|---|---|
| Related Catalog | Signaling Pathways >>Anti-infection >>HBVResearch Areas >>Infection |
| Target | IC50: 8.23 μM (ribonucleotide reductase)[1] |
| 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[1]. |
| 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[1]. |
| Cell Assay | HepG2.2.15 cells are cultured in the presence of 200 μg/mL G418. Cell viability is determined using a Cell Counting Kit-8 in 96-well plates treated with Osalmid for designated times. For long term assays, the culture supernatants are replaced with fresh media containing Osalmid every two days. The control wells contained equivalent amounts of DMSO. The CC50 is calculated as the concentration of a compound that reduced the cell viability to 50% compared to the control[1]. |
| Animal Admin | Mice: The HBV-transgenic mouse lineage is initially produced on a BALB/c background. Osalmid or 3TC is suspended in 0.05% CMC-Na and administered once a day by gavage at 400 and 100 mg/kg, respectively, for 28 days. For the combination group, mice are intragastrically administered with a mixture of osalmid and 3TC. 0.05% CMC-Na solution is used as control. The mouse sera are collected and assayed for HBV DNA levels and AST/ALT activity. Mice are then sacrificed after the 28-day drug treatment and the livers are excised for analysis[1]. |
| References | [1]. Liu X, et al. Inhibition of hepatitis B virus replication by targeting ribonucleotide reductase M2 protein. Biochem Pharmacol. 2016 Mar 1;103:118-28. |
Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 350.8±27.0 °C at 760 mmHg |
| Melting Point | 179ºC |
| Molecular Formula | C13H11NO3 |
| Molecular Weight | 229.231 |
| Flash Point | 165.9±23.7 °C |
| Exact Mass | 229.073898 |
| PSA | 69.56000 |
| LogP | 2.53 |
| Vapour Pressure | 0.0±0.8 mmHg at 25°C |
| Index of Refraction | 1.711 |
| InChIKey | LGCMKPRGGJRYGM-UHFFFAOYSA-N |
| SMILES | O=C(Nc1ccc(O)cc1)c1ccccc1O |
Toxicological Information
CHEMICAL IDENTIFICATION |
ACUTE TOXICITY DATA - TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 6702 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,159,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 1484 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,290,1995
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >5 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,159,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1050 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - lacrimation Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- JJPAAZ Japanese Journal of Pharmacology. (Japanese Pharmacological Soc., c/o Dept. of Pharmacology, Faculty of Medicine, Kyoto Univ., Sakyo-ku, Kyoto 606, Japan) V.1- 1951- Volume(issue)/page/year: 22,235,1972
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 517 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,159,1982
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1900 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 116,154,1958
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 180 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- CSLNX* U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals. (Aberdeen Proving Ground, MD 21010) Volume(issue)/page/year: NX#03234
Safety Information
| Hazard Codes | Xn |
|---|---|
| Risk Phrases | R22 |
| Safety Phrases | 26-36/37 |
| HS Code | 2924299090 |
Customs
| HS Code | 2924299090 |
|---|---|
| Summary | 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0% |
Synonyms
| MFCD00020026 |
| bilene |
| osalmid |
| bilocol |
| 2-Hydroxy-N-(4-hydroxyphenyl)benzamide |
| Qsalmid |
| auxobil |
| EINECS 208-385-9 |
| LOIRD |
| 2-Hydroxy-N-(4-Hydroxy Phenyl)Benzamide |
| driol |
| phps |
| l1718 |
| Benzamide, 2-hydroxy-N-(4-hydroxyphenyl)- |
| 4'-HYDROXYSALICYLANILIDE |
| Oksafenamide |
| enidran |
| N-Salicoylaminophenol |
