Biological Activity
Very potent ligand for α1 sites (Ki for displacement of prazosin = 0.2 nM). Displays different binding properties for each α1 subtype (pKi values are 8.74, 9.44 and 9.57 for α1B, α1D and α1A adrenoceptors respectively). Also binds to 5-HT1A sites (Ki = 50 nM).
Technical Data
| M. Wt | 419.48 |
| Formula | C23H25N5O3 |
| Storage | Store at RT |
| CAS Number | 133399-65-2 |
| PubChem ID | 4013695 |
| InChI Key | AQASGOHUMGAWJJ-UHFFFAOYSA-N |
| Smiles | COC1=C(C=CC=C1)N1CCN(CCN2C(=O)NC3=C(NC4=CC=CC=C34)C2=O)CC1 |
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 | 4.19 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 419.48. 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 | 2.38 mL | 11.92 mL | 23.84 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
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References
References are publications that support the products' biological activity.
Russo et al (1991) Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective α1 adrenoceptor ligands. J.Med.Chem. 34 1850 PMID: 1648138
Romeo et al (2003) New pyrimido[5,4-b]indoles as ligands for α1-adrenoceptor subtypes. J.Med.Chem. 46 2877 PMID: 12825930
Keywords: 3-MPPI, supplier, 5-HT1A, ligand, α1-adrenoceptor, alpha1-adrenoceptor, a1-adrenoceptor, Serotonin, Receptors, 5-HT1, α1-adrenergic, alpha1-adrenergic, a1-adrenergic, Adrenergic, Alpha-1, Receptors, Tocris Bioscience
