Biological Activity
Potent and selective tachykinin NK2 receptor agonist (EC50 = 3.7 nM in rat colon). Displays > 1000- and > 300-fold selectivity over NK1 and NK3 receptors respectively. Active in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
| M. Wt | 921.12 |
| Formula | C42H68N10O11S |
| Sequence |
KDSFVGLM (Modifications: Leu-7 = R-γ-lactam-Leu, Met-8 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 137593-52-3 |
| PubChem ID | 5311135 |
| InChI Key | HVUNRXRFMQDMBO-BPZYSUIOSA-N |
| Smiles | [H]N[C@@H](CCCCN)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)NC1CCN([C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C1=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
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 921.12. 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 | 1.09 mL | 5.43 mL | 10.86 mL |
| 5 mM | 0.22 mL | 1.09 mL | 2.17 mL |
| 10 mM | 0.11 mL | 0.54 mL | 1.09 mL |
| 50 mM | 0.02 mL | 0.11 mL | 0.22 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Chang et al (2000) Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. J.Pharmacol.Exp.Ther. 294 147 PMID: 10871306
Chizh et al (1995) Endogenous modulation of excitatory amino acid responsiveness by tachykinin NK1 and NK2 receptors in the rat spinal cord. Br.J.Pharmacol. 115 1013 PMID: 7582497
Deal et al (1992) Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. J.Med.Chem. 35 4195 PMID: 1331460
Keywords: GR 64349, supplier, Potent, selective, NK2, agonists, Tachykinin, Receptors, Neurokinin, GR64349, GlaxoSmithKline, GSK, NK2, Receptor, NK2, Receptor, Tocris Bioscience
