Biological Activity
Potent and selective NK2 receptor antagonist (pA2 = 8.08, rabbit pulmonary artery). Displays > 250-fold selectivity over NK1 (pA2 = 5.66, guinea pig ileum) and NK3 (Ki > 10 mM, guinea pig brain). Active in vivo.
Technical Data
| M. Wt | 1081.24 |
| Formula | C57H68N12O10 |
| Sequence |
DYWVWWK (Modifications: Trp-3, Trp-5, Trp-6 = D-Trp, Lys-7 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 135306-85-3 |
| PubChem ID | 90479818 |
| InChI Key | QQHOFZNACVKNHK-JRPYWGABSA-N |
| Smiles | [H]N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CCCCN)C(N)=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.
Preparing Stock Solutions
The following data is based on the product molecular weight 1081.24. 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 | 0.92 mL | 4.62 mL | 9.25 mL |
| 5 mM | 0.18 mL | 0.92 mL | 1.85 mL |
| 10 mM | 0.09 mL | 0.46 mL | 0.92 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.18 mL |
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References
References are publications that support the products' biological activity.
Bartho et al (1992) Tachykininergic transmission to the circular muscle of the guinea-pig ileum: evidence for the involvement of NK2 receptors. Br.J.Pharmacol. 105 805 PMID: 1380373
Maggi et al (1991) In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J.Pharmacol.Exp.Ther. 257 1172 PMID: 1710662
Subramanian et al (1994) Pharmacological evidence of tachykinin-induced intracellular calcium rise in a human NK2 receptor transfected cell line. Biochem.Biophys.Res.Commun. 200 1512 PMID: 8185607
Keywords: MEN 10376, supplier, Potent, selective, NK2, antagonists, Tachykinin, Receptors, Neurokinin, MEN10376, NK2, Receptor, NK2, Receptor, Tocris Bioscience
