Biological Activity
Cysteinyl leukotriene receptor 1 (CysLT1) and GPR17 antagonist. Blocks pentylenetetrazole-induced seizures, blood brain barrier (BBB) disruption and leukocyte migration in mice. Reduces neuroinflammation, improves BBB integrity, enhances learning and memory, and restores hippocampal neurogenesis and cognitive function in aged rats. Orally active and brain penetrant.
Technical Data
| M. Wt | 608.17 |
| Formula | C35H35ClNNaO3S |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 151767-02-1 |
| PubChem ID | 23663996 |
| InChI Key | LBFBRXGCXUHRJY-HKHDRNBDSA-M |
| Smiles | CC(O)(C1=C(C=CC=C1)CC[C@H](C2=CC(/C=C/C3=NC4=CC(Cl)=CC=C4C=C3)=CC=C2)SCC5(CC5)CC(O[Na])=O)C |
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 | 60.82 | 100 | |
| ethanol | 60.82 | 100 | |
| water | 30.41 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 608.17. 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 | 1.64 mL | 8.22 mL | 16.44 mL |
| 5 mM | 0.33 mL | 1.64 mL | 3.29 mL |
| 10 mM | 0.16 mL | 0.82 mL | 1.64 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.33 mL |
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References
References are publications that support the products' biological activity.
Lenz et al (2014) Cysteinyl leukotriene receptor (CysLT) antagonists decrease pentylenetetrazol-induced seizures and blood-brain barrier dysfunction. Neuroscience 277 859 PMID: 25090924
Marschallinger et al (2015) Structural and functional rejuvenation of the aged brain by an approved anti-asthmatic drug. Nat.Commun. 6 8466 PMID: 26506265
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