Biological Activity
Potent and selective, competitive motilin receptor antagonist (IC50 = 4.9 nM). Selective for the motilin receptor over a range of other receptors and ion channels. Inhibits motilin-induced duodenal muscle contractions in vitro. Also inhibits motilin-induced colonic and abdominal contractions in vivo. Orally active.
Technical Data
| M. Wt | 556.71 |
| Formula | C31H45FN4O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 287206-61-5 |
| PubChem ID | 10144175 |
| InChI Key | KSDWAJPUTRBIRR-KLJDGLGGSA-N |
| Smiles | FC1=CC=C(C[C@H](NC)C(N(C)[C@@H]([C@H](C)C)C(N[C@@H](CC2=CC=C(O)C(C(C)(C)C)=C2)[C@@](NCC)=O)=O)=O)C=C1 |
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 | |||
| 1eq. HCl | 11.13 | 20 | |
| DMSO | 55.67 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 556.71. 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 | 1.8 mL | 8.98 mL | 17.96 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.59 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.8 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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References
References are publications that support the products' biological activity.
Sudo et al (2008) Oral administration of MA-2029, a novel selective and competitive motilin receptor antagonist, inhibits motilin-induced intestinal contractions and visceral pain in rabbits. Eur.J.Pharmacol. 581 296 PMID: 18164286
Keywords: MA 2029, supplier, MA2029, potent, selective, competitive, motilin, receptors, antagonists, Motilin, Receptors, Motilin, Receptors, Tocris Bioscience
