Biological Activity
Selective M3 muscarinic receptor antagonist (pKi values are 8.52, 7.93, 7.90 and 7.78 for M3, M2, M1 and M4 receptors respectively). Displays higher affinity at ileal M3 receptors (pKi = 9.3) compared to oesophageal and tracheal M3 receptors (pKi values are 8.8 and 8.2 respectively). Inhibits gastrointestinal motility in vivo in the absence of cardiovascular effects.
Compound Libraries
Zamifenacin fumarate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 531.6 |
| Formula | C27H29NO3.C4H4O4 |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 127308-98-9 |
| PubChem ID | 20056967 |
| InChI Key | PMHKTAIGYOVZEZ-ZHWJIHCSSA-N |
| Smiles | C1(CCN3C[C@H](OC(C5=CC=CC=C5)C4=CC=CC=C4)CCC3)=CC=C(OCO2)C2=C1.C(C=CC(O[H])=O)(O[H])=O |
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 | 53.16 | 100 | |
| ethanol | 13.29 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 531.6. 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 | 1.88 mL | 9.41 mL | 18.81 mL |
| 5 mM | 0.38 mL | 1.88 mL | 3.76 mL |
| 10 mM | 0.19 mL | 0.94 mL | 1.88 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wallis (1995) Pre-clinical and clinical pharmacology of selective muscarinic M3 receptor antagonists. Life Sci. 56 861 PMID: 10188786
Watson et al (1995) Characterization of the interaction of zamifenacin at muscarinic receptors in vitro. Eur.J.Pharmacol. 285 135 PMID: 8566131
Choppin (2002) Muscarinic receptors in isolated urinary bladder smooth muscle from different mouse strains. Br.J.Pharmacol. 137 522 PMID: 12359634
Keywords: Zamifenacin fumarate, supplier, Selective, M3, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, UK76654, UK, 76654, M3, Receptors, M3, Receptors, Tocris Bioscience
