Biological Activity
Potent 5-HT4 receptor full agonist (KD = 77 nM and EC50 = 18 nM for wild type 5-HT4 receptors). Binds to receptors in a mechanism different to that of the endogenous ligand 5-HT.
Compound Libraries
BIMU 8 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 378.9 |
| Formula | C19H26N4O2.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 134296-40-5 |
| PubChem ID | 5311028 |
| InChI Key | NQYXXIUVFVOJCX-XZPOUAKSSA-N |
| Smiles | [H][C@]12CC[C@](CC(NC(N3C(C=CC=C4)=C4N(C(C)C)C3=O)=O)C2)([H])N1C.Cl |
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 | 37.89 | 100 | |
| water | 28.42 | 75 |
Preparing Stock Solutions
The following data is based on the product molecular weight 378.9. 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 | 2.64 mL | 13.2 mL | 26.39 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.28 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Pellissier et al (2009) Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors. Mol.Pharmacol. 75 982 PMID: 19168624
Schaus et al (1998) Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: Indazole and benzimidazoline derivatives. J.Med.Chem. 41 1943 PMID: 9599243
Keywords: BIMU 8, supplier, BIMU8, 5-hydroxytryptamine, 4, 5HT4, receptors, 5-HT4, receptors, agonists, serotonin, serotonergic, 4, 5-HT4, Receptors, 5-HT4, Receptors, Tocris Bioscience
