| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
It was determined that osalmid might be a ribonucleotide reductase small subunit M2 (RRM2) molecule. Osalmid strongly reduces HBV DNA and cccDNA synthesis in HepG2.2.15 cells in a time- and dose-dependent manner. It also inhibits ribonucleotide reductase (RR) activity ten times more than hydroxyurea. Following an 8-day Osalmid treatment, 16.5 μM was the EC50 for HBV DNA inhibition in cells and 11.1 μM in the culture supernatant. With a concentration-dependent effect and an IC50 of 8.23 μM, osalmid suppresses RR activity. Osalmid's strong action against HBV strains resistant to 3TC has been demonstrated [1], indicating that it may be used to treat drug-resistant HBV infections.
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| ln Vivo |
In HBV transgenic mice, osalmid can lower RR activity and HBV replication. It also exhibits a synergistic impact with 3TC without being visibly harmful. Time-dependent suppression of HBV DNA replication is observed upon oral treatment of osalmid 400 mg/kg/d. Osalmid reduced HBV DNA replication in mouse serum and liver tissue by about 40–45% after 4 weeks of treatment as compared to the control group [1].
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| References | |
| Additional Infomation |
Osalmid is an organic molecular entity.
Osalmid is under investigation in clinical trial NCT03670173 (Safety and Efficacy Assessments of Osalmid in Multiple Myeloma). |
| Exact Mass |
229.073
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|---|---|
| CAS # |
526-18-1
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| PubChem CID |
4602
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
350.8±27.0 °C at 760 mmHg
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| Melting Point |
179ºC
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| Flash Point |
165.9±23.7 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.711
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| LogP |
2.53
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
261
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC=C(O)C=C1)C2=CC=CC=C2O
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| InChi Key |
LGCMKPRGGJRYGM-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-hydroxy-N-(4-hydroxyphenyl)benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~436.24 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03670173 | UNKNOWN STATUS | Drug: Osalmid | Multiple Myeloma | Shanghai 10th People's Hospital | 2018-10-01 | Phase 1 Phase 2 |
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