![[D-Arg6,Pro9-NEt]Salmon gonadotropin-releasing hormone](/upload/0201/637348523095467850571695764.png)
| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
sGnRH-A functions as a potent agonist of the GnRH receptor (gonadotropin-releasing hormone receptor). It binds to GnRH receptors on pituitary gonadotrophs, stimulating the synthesis and release of pituitary gonadotropins and growth hormone in teleost fish. The compound shows very high affinity to GnRH receptors and is typically applied in combination with dopamine antagonists such as domperidone or pimozide to induce ovulation and spawning in a large number of fish species.
|
|---|---|
| ln Vitro |
sGnRH-A (0.1 nM-1 μM, 24 h) lethally increases GH mRNA levels and stimulates GH death [1]. sGnRH-A (10 nM, 6 h) induces an increase in growth hormone levels that is nearly 5 times higher than death [1].
sGnRH-A at concentrations ranging from 0.1 nM to 1 μM for 24 hours increases GH mRNA levels and stimulates growth hormone secretion. At 10 nM for 6 hours, sGnRH-A induces an increase in growth hormone levels that is nearly 5 times higher than baseline. These in vitro studies demonstrate the compound's potent ability to stimulate GH production at the transcriptional and secretory levels in pituitary cell models. |
| ln Vivo |
In vivo, sGnRH-A is used as an effective ovulation inducer for artificial insemination in aquaculture. When administered in combination with a dopamine antagonist, sGnRH-A induces ovulation and spawning in a large number of fish species. The compound has been successfully applied in reproductive management programs for various commercially important fish species to enhance spawning success and egg production.
|
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for sGnRH-A typically involves competitive binding studies using radiolabeled GnRH analogs and membrane preparations from pituitary tissues or cells expressing GnRH receptors. The assay measures the displacement of labeled ligand by increasing concentrations of sGnRH-A to determine binding affinity (Ki or IC50). Receptor binding is performed in suitable buffer systems at optimized temperature and incubation times, followed by filtration or centrifugation to separate bound from free radioligand, with radioactivity counted via scintillation spectroscopy.
|
| Cell Assay |
In vitro cellular studies are conducted using primary pituitary cell cultures or immortalized gonadotrope cell lines. Cells are treated with sGnRH-A at various concentrations (typically 0.1 nM to 1 μM) for defined time periods (e.g., 6-24 hours). GH mRNA levels are quantified by RT-PCR or Northern blot analysis, and GH protein secretion is measured by ELISA or radioimmunoassay in culture media. Cell viability and proliferation are also assessed to evaluate potential cytotoxic effects of the compound.
|
| Animal Protocol |
In vivo animal experiments are performed in fish species for aquaculture research. Fish are administered sGnRH-A via injection (typically intraperitoneal or intramuscular) at doses ranging from micrograms to milligrams per kilogram body weight, often in combination with dopamine antagonists such as domperidone or pimozide. Endpoints include ovulation rate, spawning success, egg quality, and plasma gonadotropin and growth hormone levels measured at various time points post-administration.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of sGnRH-A in fish include rapid absorption following injection, distribution to pituitary and peripheral tissues, and metabolic clearance primarily via enzymatic degradation. The D-arginine substitution and ethylamide-modified C-terminus confer enhanced resistance to enzymatic degradation, resulting in improved metabolic stability and prolonged biological activity compared to native sGnRH. The compound has a molecular weight of 1282.45 g/mol and exhibits LogP of 4.034.
|
| Toxicity/Toxicokinetics |
Toxicological data for sGnRH-A are primarily derived from aquaculture safety studies. The compound is generally well-tolerated in fish at effective doses. No significant acute toxicity has been reported at doses used for induced ovulation and spawning. Standard safety assessments include evaluation of injection site reactions, behavioral changes, and histopathological examination of target organs. The compound is for research use only and not intended for human therapeutic applications.
|
| References |
|
| Additional Infomation |
sGnRH-A is also known as [D-Arg6,Pro9-NEt]Salmon gonadotropin-releasing hormone, sGnRH-A, and (Des-Gly10,D-Arg6,Pro-NHEt9)-LHRH (salmon) acetate salt. It is supplied as a powder with ≥98% purity and should be stored at -20°C for long-term stability. The compound is primarily used in aquaculture research for reproductive management and growth enhancement. Not intended for individual clinical or medical purposes.
|
| Molecular Formula |
C64H83N17O12
|
|---|---|
| Molecular Weight |
1282.45052
|
| Exact Mass |
1281.64
|
| CAS # |
96497-82-4
|
| Related CAS # |
sGnRH-A acetate
|
| PubChem CID |
121493629
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.48±0.1 g/cm3 (20 °C, 760 mmHg)
|
| LogP |
4.034
|
| Hydrogen Bond Donor Count |
16
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
32
|
| Heavy Atom Count |
93
|
| Complexity |
2610
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
C(C1=CNC2C=CC=CC1=2)[C@H](NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](NC([C@@H]1CCC(=O)N1)=O)CC1NC=NC=1)CC1=CNC2C=CC=CC1=2)CC1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(N1CCC[C@H]1C(=O)NCC)=O
|
| InChi Key |
PYXUQVSYYFRRBD-OIAWHVPDSA-N
|
| InChi Code |
InChI=1S/C64H83N17O12/c1-4-68-62(92)53-16-10-24-81(53)63(93)51(25-35(2)3)79-58(88)48(27-37-30-70-43-13-7-5-11-41(37)43)76-55(85)45(15-9-23-69-64(65)66)74-57(87)47(26-36-17-19-40(83)20-18-36)75-61(91)52(33-82)80-59(89)49(28-38-31-71-44-14-8-6-12-42(38)44)77-60(90)50(29-39-32-67-34-72-39)78-56(86)46-21-22-54(84)73-46/h5-8,11-14,17-20,30-32,34-35,45-53,70-71,82-83H,4,9-10,15-16,21-29,33H2,1-3H3,(H,67,72)(H,68,92)(H,73,84)(H,74,87)(H,75,91)(H,76,85)(H,77,90)(H,78,86)(H,79,88)(H,80,89)(H4,65,66,69)/t45-,46+,47+,48+,49+,50+,51+,52+,53+/m1/s1
|
| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-5-(diaminomethylideneamino)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
|
| Synonyms |
[D-Arg6,Pro9-NEt]Salmon gonadotropin-releasing hormone
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.7798 mL | 3.8988 mL | 7.7976 mL | |
| 5 mM | 0.1560 mL | 0.7798 mL | 1.5595 mL | |
| 10 mM | 0.0780 mL | 0.3899 mL | 0.7798 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
