Biological Activity
Synthetic gonadotropin-releasing hormone (GnRH) agonist that stimulates secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Repeated administration causes desensitization of pituitary GnRH receptors resulting in inhibition of gonadotropin release and decreased steroid hormone synthesis. Induces atrophy and regression of experimentally induced endometriosis in rat and shrinks hypertrophic tissue in benign prostatic hyperplasia.
Technical Data
| M. Wt | 1322 |
| Formula | C66H83N17O13 |
| Sequence |
XEHWSYXLRPG (Modifications: X-1 = Glp, X-2 = 2-Nal, Gly-10 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 76932-56-4 |
| PubChem ID | 25077405 |
| InChI Key | RWHUEXWOYVBUCI-ITQXDASVSA-N |
| Smiles | [H]N1[C@@H](CCC1=O)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@H](CC1=CC2=CC=CC=C2C=C1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)NCC(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 1322. 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 | 0.76 mL | 3.78 mL | 7.56 mL |
| 5 mM | 0.15 mL | 0.76 mL | 1.51 mL |
| 10 mM | 0.08 mL | 0.38 mL | 0.76 mL |
| 50 mM | 0.02 mL | 0.08 mL | 0.15 mL |
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References
References are publications that support the products' biological activity.
Chrisp and Goa (1990) Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions. Drugs 39 523 PMID: 2140979
Letassy et al (1990) Nafarelin acetate: a gonadotrophin-releasing hormone agonist for the treatment of endometriosis. DICP 24 1204 PMID: 2151003
Mizutani et al (1995) Effect of gonadotrophin-releasing hormone agonists, nafarelin, buserelin, and leuprolide, on experimentally induced endometriosis in the rat. Int.J.Fertil.Menopausal Stud. 40 106 PMID: 7599657
Keywords: Nafarelin, supplier, GnRH, receptor, agonists, Receptors, Gonadotrophin-Releasing, Hormone, gonadotropin, Gonadotrophin-Releasing, Hormone, Receptors, Gonadotrophin-Releasing, Hormone, Receptors, Tocris Bioscience
