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Submit ReviewGR 64349
Description: Potent, selective NK2 agonist
Purity: ≥95% (HPLC)
Biological Activity for GR 64349
GR 64349 is a 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 for GR 64349
| M. Wt | 921.12 |
| Formula | C42H68N10O11S |
| Sequence |
KDSFVGLM (Modifications: Leu-7 = R-γ-lactam-Leu, Met-8 = C-terminal amide) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GR 64349
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for GR 64349
References for GR 64349
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for GR 64349, please let us know.
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Keywords: GR 64349, GR 64349 supplier, Potent, selective, NK2, agonists, Tachykinin, Receptors, Neurokinin, GR64349, GlaxoSmithKline, GSK, Receptor, 1668, Tocris Bioscience
3 Citations for GR 64349
Citations are publications that use Tocris products. Selected citations for GR 64349 include:
León et al (2016) Direct actions of kisspeptins on GnRH neurons permit attainment of fertility but are insufficient to fully preserve gonadotropic axis activity. Sci.Rep. 6 19206 PMID: 26755241
Ruiz-Pino et al (2015) Effects and interactions of tachykinins and dynorphin on FSH and LH secretion in developing and adult rats. Endocrinology 156 576 PMID: 25490143
Navarro et al (2015) The integrated hypothalamic tachykinin-kisspeptin system as a central coordinator for reproduction. Sci Rep 156 627 PMID: 25422875
Do you know of a great paper that uses GR 64349 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.