Biological Activity
Specific, non-competitve 15-lipoxygenase (15-LOX) inhibitor (Ki = 197nM) that has no demonstrable effect on 5-LOX, 12-LOX, COX-1 or COX-2 (IC50 = 0.54 μM for 15-LOX in rabbit reticulocytes). Lacks non-specific antioxidant properties and prevents atherogenesis via regulation of monocyte-macrophage enrichment in vivo.
Technical Data
| M. Wt | 237.32 |
| Formula | C15H11NS |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 4079-26-9 |
| PubChem ID | 297589 |
| InChI Key | ZGOOPZVQMLHPFM-UHFFFAOYSA-N |
| Smiles | C12=CC=CC=C1C3=C(C(C=CC=C4)=C4SC3)N2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.73 | 100 | |
| ethanol | 11.87 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 237.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.21 mL | 21.07 mL | 42.14 mL |
| 5 mM | 0.84 mL | 4.21 mL | 8.43 mL |
| 10 mM | 0.42 mL | 2.11 mL | 4.21 mL |
| 50 mM | 0.08 mL | 0.42 mL | 0.84 mL |
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References
References are publications that support the products' biological activity.
Sendobry et al (1997) Attenuation of diet-induced atherosclerosis in rabbits with a highly selective 15-lipoxygenase inhibitor lacking significant antioxidant properties. Br.J.Pharmacol. 120 1199 PMID: 9105693
Bocan et al (1998) A specific 15-lipoxygenase inhibitor limits the progression and monocyte-macrophage enrichment of hypercholesterolemia-induced atherosclerosis in the rabbit. Atherosclerosis 136 203 PMID: 9543090
Sordillo et al (2005) Enhanced 15-HPETE production during oxidant stress induces apoptosis of endothelial cells. Prostaglandins Other Lipid Mediat. 76 19 PMID: 15967159
Keywords: PD 146176, supplier, Selective, 15-lipoxygenase, inhibitors, inhibits, Oxygenases, Oxidases, PD146176, 15-LOX, ferroptosis, inhibitors, inhibits, Lipoxygenase, Ferroptosis, Lipoxygenase, Tocris Bioscience
