Biological Activity
Tachykinin NK1 receptor antagonist.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Technical Data
| M. Wt | 1386.57 |
| Formula | C69H91N15O16 |
| Sequence |
XADPNKFYPLW (Modifications: X-1 = Glp, Leu-10 = spiro-g-lactam-Leu, Trp-11 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 129623-01-4 |
| PubChem ID | 16130972 |
| InChI Key | KWECNVXXONDEKG-JTCMYMKESA-N |
| Smiles | CC(C)C[C@H](N1CC[C@@]2(CCCN2C(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H]2CCC(=O)N2)C1=O)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)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.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1386.57. 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 | 0.72 mL | 3.61 mL | 7.21 mL |
| 5 mM | 0.14 mL | 0.72 mL | 1.44 mL |
| 10 mM | 0.07 mL | 0.36 mL | 0.72 mL |
| 50 mM | 0.01 mL | 0.07 mL | 0.14 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Guo et al (1995) Pharmacological characterisation of GR82334, a tachykinin NK1 receptor antagonist, in the isolated spinal cord of the neonatal rat. Eur.J.Pharmacol. 281 49 PMID: 8566116
Lecci et al (1992) Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci. 51 PL277 PMID: 1335533
Hagan et al (1991) A spirolactam conformationally-constrained analogue of physalaemin which is a peptidase-resistant, selective neurokinin NK-1 receptor antagonist. Br.J.Pharmacol. 102 168P PMID:
Keywords: GR 82334, supplier, Tachykinin, NK1, receptor, antagonists, Receptors, Neurokinin, GR82334, GlaxoSmithKline, GSK, NK1, Receptor, NK1, Receptor, Tocris Bioscience
