| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
Purity: = 99.06%
| Targets |
Gonadorelin Acetate targets the gonadotropin-releasing hormone receptor (GNRHR), a G protein-coupled receptor expressed on the surface of pituitary gonadotrophs. It acts as an agonist at this receptor, with a Ki of 13 nM in CHO cells expressing the human receptor. Upon binding, it stimulates the release of LH and FSH.
|
|---|---|
| ln Vitro |
In vitro, Gonadorelin Acetate is used to study the regulation of gonadotropin secretion. It stimulates LH and FSH release from rat anterior pituitary cultures. Its activity is measured by quantifying the amount of these hormones released into the culture medium.
|
| ln Vivo |
In vivo, Gonadorelin Acetate is used to treat reproductive disorders. It is recommended for the treatment of ovarian cysts and for improving fertility in cows, and for the induction of ovulation in rabbits. It is also used in diagnostic tests to evaluate pituitary function.
|
| Enzyme Assay |
The binding affinity of Gonadorelin Acetate to its receptor is determined using a radioligand binding assay. In this cell-free system, membrane preparations from cells expressing the GNRHR are incubated with a radiolabeled GnRH analog in the presence of varying concentrations of Gonadorelin Acetate. The displacement of the radiolabeled ligand is measured to calculate the Ki.
|
| Cell Assay |
For cellular assays, primary cultures of rat anterior pituitary cells are used. These cells are treated with Gonadorelin Acetate, and the amount of LH and FSH released into the culture medium is measured by radioimmunoassay or ELISA.
|
| Animal Protocol |
In vivo, Gonadorelin Acetate is administered via injection. In veterinary medicine, it is used to induce ovulation in cattle and other livestock. Its efficacy is assessed by monitoring reproductive outcomes.
|
| ADME/Pharmacokinetics |
Gonadorelin Acetate is a synthetic peptide. As a peptide, it has a short half-life in the circulation and is typically administered via injection.
|
| Toxicity/Toxicokinetics |
As a peptide hormone, Gonadorelin Acetate is generally well-tolerated. Its effects are related to its mechanism of action, which can lead to temporary changes in reproductive hormone levels.
|
| Additional Infomation |
Gonadotropin-releasing hormone (GnRH) is a decapeptide that stimulates the synthesis and secretion of pituitary gonadotropins (luteinizing hormone and follicle-stimulating hormone). GnRH is produced by neurons in the preoptic septum of the hypothalamus and released into the pituitary portal bloodstream, thereby stimulating gonadotropin-releasing cells in the anterior pituitary.
See also: Gonadotropin-releasing hormone acetate (note moved to). Gonadorelin Acetate is a veterinary drug and a diagnostic agent. It is used to treat reproductive disorders in livestock and to assess pituitary function in both veterinary and human medicine. Its role as a synthetic GnRH has made it a valuable tool in reproductive biology. |
| Molecular Formula |
C55H75N17O13.C2H4O2
|
|---|---|
| Molecular Weight |
1242.34206
|
| Exact Mass |
1241.594
|
| CAS # |
34973-08-5
|
| Related CAS # |
34973-08-5 (acetate); 33515-09-2;51952-41-1 (HCl);499785-55-6(monoacetate); 78308-49-3 (diacetate hydrate); 71447-49-9 (diacetate);
|
| PubChem CID |
11980076
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.198
|
| Hydrogen Bond Donor Count |
17
|
| Hydrogen Bond Acceptor Count |
17
|
| Rotatable Bond Count |
31
|
| Heavy Atom Count |
89
|
| Complexity |
2420
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
O=C(N[C@@H](CO)C(N[C@H](C(NCC(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N(CCC1)[C@@H]1C(NCC(N)=O)=O)=O)=O)=O)=O)CC2=CC=C(O)C=C2)=O)[C@@H](NC([C@@H](NC([C@H](CC3)NC3=O)=O)CC4=CNC=N4)=O)CC5=CNC6=C5C=CC=C6.OC(C)=O
|
| InChi Key |
NGCGMRBZPXEPOZ-HBBGHHHDSA-N
|
| InChi Code |
InChI=1S/C55H75N17O13.C2H4O2/c1-29(2)19-38(49(80)67-37(9-5-17-60-55(57)58)54(85)72-18-6-10-43(72)53(84)62-25-44(56)75)66-46(77)26-63-47(78)39(20-30-11-13-33(74)14-12-30)68-52(83)42(27-73)71-50(81)40(21-31-23-61-35-8-4-3-7-34(31)35)69-51(82)41(22-32-24-59-28-64-32)70-48(79)36-15-16-45(76)65-36;1-2(3)4/h3-4,7-8,11-14,23-24,28-29,36-43,61,73-74H,5-6,9-10,15-22,25-27H2,1-2H3,(H2,56,75)(H,59,64)(H,62,84)(H,63,78)(H,65,76)(H,66,77)(H,67,80)(H,68,83)(H,69,82)(H,70,79)(H,71,81)(H4,57,58,60);1H3,(H,3,4)/t36-,37-,38-,39-,40-,41-,42-,43-;/m0./s1
|
| Chemical Name |
acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]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
|
| 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 | 0.8049 mL | 4.0247 mL | 8.0493 mL | |
| 5 mM | 0.1610 mL | 0.8049 mL | 1.6099 mL | |
| 10 mM | 0.0805 mL | 0.4025 mL | 0.8049 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
COA