| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Nafarelin targets the GnRH receptor (GnRH-R), a G protein-coupled receptor expressed on pituitary gonadotropes. As a GnRH agonist, Nafarelin binds to and activates the GnRH receptor, stimulating the release of FSH and LH from the anterior pituitary. With continuous administration, GnRH agonists cause down-regulation of GnRH receptors, leading to suppression of gonadotropin secretion and sex steroid production. This mechanism is used for therapeutic purposes.
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| ln Vitro |
In vitro, Nafarelin acts as a GnRH agonist, stimulating FSH and LH release from pituitary cells in culture. It binds to GnRH receptors with high affinity. The compound's activity is assessed by measuring gonadotropin release in cell-based assays. Detailed in vitro data are available in the primary literature. Nafarelin is a well-characterized GnRH analog used as a reference compound in reproductive endocrinology research.
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| ln Vivo |
In vivo, Nafarelin is administered intranasally or by injection for the treatment of endometriosis and central precocious puberty. It increases FSH and LH release initially, followed by down-regulation of GnRH receptors and suppression of gonadotropin secretion. This leads to reduced sex steroid production, which is the basis for its therapeutic effects. Nafarelin has been used in clinical trials and is approved for clinical use in some countries.
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| Enzyme Assay |
In vitro receptor binding assays for Nafarelin typically use membrane preparations from pituitary cells or cells expressing GnRH receptors. Radioligand binding is performed using [¹²⁵I]-GnRH or [¹²⁵I]-Nafarelin as tracer. Membranes are incubated with radioligand and varying concentrations of unlabeled Nafarelin in assay buffer at room temperature for 60-120 minutes. Nonspecific binding is determined using excess unlabeled GnRH. Bound radioactivity is measured by filtration and scintillation counting. IC₅₀ and Ki values are calculated from competition curves. Functional assays measure FSH and LH release from pituitary cells.
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| Cell Assay |
For cell-based assays, pituitary cell lines or primary pituitary cells are cultured in appropriate medium. Cells are seeded in multi-well plates and treated with Nafarelin at various concentrations (0.001-100 nM) for 2-24 hours. FSH and LH levels in culture medium are measured by ELISA or radioimmunoassay. GnRH receptor internalization and signaling are assessed by Western blotting or reporter assays. Cell viability is assessed by standard assays. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, Nafarelin is typically administered intranasally or via subcutaneous injection. For animal studies, rodents or other species are dosed at various regimens. For endometriosis models, animals are treated with Nafarelin for 2-4 weeks. Endpoints include gonadotropin and sex steroid levels in blood, ovarian and uterine weights, and histology. For precocious puberty models, pubertal onset is monitored. Blood samples are collected for hormone analysis. All procedures follow institutional guidelines.
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| ADME/Pharmacokinetics |
Nafarelin acetate hydrate (MW 1400.5, C₆₈H₈₉N₁₇O₁₆) is a synthetic GnRH analog. The compound is a peptide and is typically administered intranasally or by injection. Detailed pharmacokinetic parameters (bioavailability, half-life, clearance) are available from clinical pharmacology literature. Nafarelin is metabolized by peptidases. It is a well-characterized pharmaceutical agent.
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| Toxicity/Toxicokinetics |
Nafarelin is a clinically approved drug with an established safety profile. It is used for the treatment of endometriosis and central precocious puberty. Common side effects include hot flashes, mood changes, and vaginal dryness due to estrogen suppression. Long-term use may cause bone density loss. The compound is available as a pharmaceutical product in some countries.
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| References |
Ludwig C, Desmoulins PO, Driancourt MA, Goericke-Pesch S, Hoffmann B. Reversible downregulation of endocrine and germinative testicular function (hormonal castration) in the dog with the GnRH-agonist azagly-nafarelin as a removable implant 'Gonazon'; a preclinical trial. Theriogenology. 2009 Apr 15;71(7):1037-45. doi: 10.1016/j.theriogenology.2008.10.015. Epub 2009 Feb 23. PubMed PMID: 19233456.
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| Additional Infomation |
Nafarelin acetate may cause developmental toxicity depending on state or federal labeling requirements. Nafarelin is a potent anabolic gonadotropin-releasing hormone agonist with its 6th residue replaced by 3-(2-naphthyl)-D-alanine. Nafarelin has been used to treat central precocious puberty and endometriosis. See also: Nafarelin acetate (note moved to).
Nafarelin is a GnRH agonist used clinically for the treatment of endometriosis and central precocious puberty. Its mechanism involves GnRH receptor activation, leading to initial gonadotropin release followed by receptor down-regulation and suppression of sex steroid production. The compound is available as a pharmaceutical product in some countries. It is also available from chemical suppliers for research purposes. Its mechanism involves GnRH receptor agonism. |
| Molecular Formula |
C68H89N17O16
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|---|---|
| Molecular Weight |
1400.563
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| Exact Mass |
1399.67
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| CAS # |
86220-42-0
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| Related CAS # |
86220-42-0 (acetate);76932-56-4;
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| PubChem CID |
25079425
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
1840.1ºC at 760 mmHg
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| Flash Point |
1066.6ºC
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| Vapour Pressure |
0mmHg at 25°C
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| LogP |
3.898
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| Hydrogen Bond Donor Count |
18
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
101
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| Complexity |
2760
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(C[C@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H]1CCC(N1)=O)=O)CC2=CN=CN2)=O)CC3=CNC4=CC=CC=C34)=O)CO)=O)CC5=CC=C(O)C=C5)=O)CC6=CC7=CC=CC=C7C=C6)=O)C(N[C@H](C(N8CCC[C@H]8C(NCC(N)=O)=O)=O)CCCNC(N)=N)=O)C.CC(O)=O.O
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| InChi Key |
Pyr-His-Trp-Ser-Tyr-D-2-Nal-Leu-Arg-Pro-Gly-NH2 acetate hydrate
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| InChi Code |
FSBTYDWUUWLHBD-YSWDAIMKSA-N
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| Chemical Name |
RS-94991-298 Nafarelin acetate Nafarelin acetate hydrate Synarel
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7140 mL | 3.5700 mL | 7.1400 mL | |
| 5 mM | 0.1428 mL | 0.7140 mL | 1.4280 mL | |
| 10 mM | 0.0714 mL | 0.3570 mL | 0.7140 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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