Biological Activity
Potent, non-peptide and orally active oxytocin receptor antagonist (IC50 = 8.9 nM) that displays > 40-fold selectivity over vasopressin V1a and V2 receptors (IC50 values are 370 and 570 nM respectively). Antagonizes oxytocin-induced uterine contractions in vitro and in vivo.
Compound Libraries
L-368,899 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 591.23 |
| Formula | C26H42N4O5S2.HCl |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 160312-62-9 |
| PubChem ID | 90488775 |
| InChI Key | GIUFQWFJHXXXEQ-PHSYAEQHSA-N |
| Smiles | CC(C=CC=C2)=C2N1CCN(S(CC34CCC(C(C)4C)C[C@@H]3NC([C@@H](N)CCS(C)(=O)=O)=O)(=O)=O)CC1.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 | 59.12 | 100 | |
| water | 59.12 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 591.23. 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 | 1.69 mL | 8.46 mL | 16.91 mL |
| 5 mM | 0.34 mL | 1.69 mL | 3.38 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.69 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Williams et al (1994) 1-(((7,7-dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential util J.Med.Chem. 37 565 PMID: 8126695
Mann et al (2003) Attenuation of PGE2α release in ewes infused with the oxytocin antagonist L-368,899. Domest.Anim.Endocrinol. 25 255 PMID: 14550509
Quattropani et al (2005) Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonist. J.Med.Chem. 48 7882 PMID: 16302826
Borthwick (2010) Oral oxytocin antagonists. J.Med.Chem. 53 6525 PMID: 20550119
Keywords: L-368,899 hydrochloride, supplier, Potent, non-peptide, oxytocin, receptor, antagonists, OT, Receptors, L368899, Oxytocin, Receptors, Oxytocin, Receptors, Tocris Bioscience
