OG-L002 (OG-L-002) is a pecific inhibitor of LSD-1 [ lysine (K)-specific demethylase 1A] with potential antiviral activity. It inhibits LSD-1 with an IC50 of 20 nM in a cell-free assay, and displays 36- and 69-fold selectivity for LSD-1 over MAO-B and MAO-A, respectively. OG-L002 shows potent in vitro antiviral activity and high in vivo efficacy. It was foud to inhibit herpes simplex virus (HSV) immediate early gene expression and viral yield in vitro and suppresses HSV primary infection in vivo.
Physicochemical Properties
| Molecular Formula | C15H15NO | |
| Molecular Weight | 225.29 | |
| Exact Mass | 225.115 | |
| CAS # | 1357302-64-7 | |
| Related CAS # |
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| PubChem CID | 56639570 | |
| Appearance | White to yellow solid powder | |
| Density | 1.2±0.1 g/cm3 | |
| Boiling Point | 416.7±45.0 °C at 760 mmHg | |
| Flash Point | 205.8±28.7 °C | |
| Vapour Pressure | 0.0±1.0 mmHg at 25°C | |
| Index of Refraction | 1.644 | |
| LogP | 2.27 | |
| Hydrogen Bond Donor Count | 2 | |
| Hydrogen Bond Acceptor Count | 2 | |
| Rotatable Bond Count | 2 | |
| Heavy Atom Count | 17 | |
| Complexity | 260 | |
| Defined Atom Stereocenter Count | 2 | |
| SMILES | C1[C@@H]([C@H]1N)C2=CC=C(C=C2)C3=CC(=CC=C3)O |
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| InChi Key | DSOJSZXQRJGBCW-CABCVRRESA-N | |
| InChi Code | InChI=1S/C15H15NO/c16-15-9-14(15)11-6-4-10(5-7-11)12-2-1-3-13(17)8-12/h1-8,14-15,17H,9,16H2/t14-,15+/m1/s1 | |
| Chemical Name | 4'-((1R,2S)-2-aminocyclopropyl)biphenyl-3-ol | |
| Synonyms | OGL002; OGL 002; OG-L002 | |
| HS Tariff Code | 2934.99.9001 | |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | In comparison to the control MAOI TCP (IC50: ~1 mM), OG-L002 greatly reduces the IE gene expression of the virus in both cells (IC50: ~10 µM in HeLa cells and ~3 µM in HFF cells)[1]. |
| ln Vivo | In the ganglia, OG-L002 (ip; 6–40 mg/kg; daily; for 7 days) decreases detectable viral genome levels in a dose-dependent manner at 3 and 5 days after infection[1]. |
| Animal Protocol |
Animal/Disease Models: 4 weeks old BALB/c female mice[1] Doses: 6, 20, 40 mg/kg Route of Administration: Intraperitoneal; daily; for 7 days Experimental Results: decreased the levels of detectable viral genomes in the ganglia in a dose-dependent manner at both 3 and 5 days postinfection. |
| References |
[1]. A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. mBio. 2013 Feb 5;4(1):e00558-12. |
Solubility Data
| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (7.41 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 16.7 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: ≥ 1.67 mg/mL (7.41 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 16.7 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. Solubility in Formulation 3: ≥ 1.67 mg/mL (7.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: 1% DMSO+30% polyethylene glycol+1% Tween 80:20mg/mL  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4387 mL | 22.1936 mL | 44.3872 mL | |
| 5 mM | 0.8877 mL | 4.4387 mL | 8.8774 mL | |
| 10 mM | 0.4439 mL | 2.2194 mL | 4.4387 mL |