| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
GnRH receptor (GNRHR, agonist). Gonadorelin binds to GnRH receptors on anterior pituitary gonadotroph cells, stimulating the synthesis and secretion of both LH and FSH.
|
|---|---|
| ln Vitro |
In vitro, gonadorelin stimulates the release of LH and FSH from cultured pituitary cells. It binds to the GnRH receptor with high affinity and activates downstream signaling pathways leading to gonadotropin secretion.
|
| ln Vivo |
In vivo, gonadorelin is used to induce ovulation and treat infertility. It is also used diagnostically to assess pituitary function. Chronic administration can lead to downregulation of GnRH receptors and suppression of gonadotropin secretion, which is exploited therapeutically.
|
| Enzyme Assay |
GnRH receptor binding assay: membrane preparations from cells expressing human GnRH receptors are incubated with a radiolabeled GnRH analog (e.g., [¹²⁵I]-or [³H]-buserelin) and varying concentrations of gonadorelin. Bound radioactivity is measured by scintillation counting to determine binding affinity (Ki or IC₅₀).
|
| Cell Assay |
Pituitary cell cultures (e.g., primary rat pituitary cells or the LβT2 gonadotroph cell line) are treated with gonadorelin. LH and FSH secretion into the culture medium is measured by radioimmunoassay (RIA) or ELISA. Downstream signaling, such as calcium flux or MAPK activation, can also be assessed.
|
| Animal Protocol |
Animal models of reproductive disorders (e.g., female rats with induced ovulation) or pituitary function are used to evaluate the in vivo effects of gonadorelin. The compound is administered intravenously or subcutaneously, and serum LH and FSH levels are measured by RIA or ELISA.
|
| Additional Infomation |
Gonadorelin hydrochloride (GnRH) is a polypeptide. It 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: Gonadorelin hydrochloride (note moved to).
|
| Molecular Formula |
C55H76CLN17O13
|
|---|---|
| Molecular Weight |
1218.76
|
| Exact Mass |
1217.549
|
| CAS # |
51952-41-1
|
| 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 |
23624131
|
| Appearance |
Typically exists as solid at room temperature
|
| tPSA |
475
|
| Hydrogen Bond Donor Count |
17
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
31
|
| Heavy Atom Count |
86
|
| Complexity |
2390
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
CC(C)CC(C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)NCC(=O)N)NC(=O)CNC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C(CO)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CC5=CN=CN5)NC(=O)C6CCC(=O)N6.Cl
|
| InChi Key |
UPRWQSQENCASAD-HBBGHHHDSA-N
|
| InChi Code |
InChI=1S/C55H75N17O13.ClH/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;/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);1H/t36-,37-,38-,39-,40-,41-,42-,43-;/m0./s1
|
| Chemical Name |
(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;hydrochloride
|
| Synonyms |
Gonadorelin HCl Factrel LH-RH hydrochloride AY-24,031Gonadorelin hydrochloride AY 24,031 AY24,031
|
| 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 | 0.8205 mL | 4.1025 mL | 8.2051 mL | |
| 5 mM | 0.1641 mL | 0.8205 mL | 1.6410 mL | |
| 10 mM | 0.0821 mL | 0.4103 mL | 0.8205 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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