GnRH receptor (gonadotropin-releasing hormone receptor). Gonadorelin is a GnRH analog that binds to the GnRH receptor on pituitary gonadotrophs. This binding stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the anterior pituitary gland. The compound acts as an agonist at the GnRH receptor, triggering the downstream signaling cascade that leads to gonadotropin secretion.

Gonadorelin stimulates LH and FSH release from pituitary cells in vitro. The compound binds to the GnRH receptor and activates intracellular signaling pathways, including phospholipase C and protein kinase C, leading to gonadotropin secretion. Its potency and efficacy have been characterized in various in vitro assays using cultured pituitary cells.

In vivo, Gonadorelin is used to stimulate LH and FSH release in both humans and animals. It is indicated for the treatment of ovarian follicular cysts in dairy cattle and is used to reduce the time interval from calving to first ovulation. It is also used in cattle for synchronization of estrus and timed artificial insemination programs. In humans, it is used for diagnostic testing of pituitary function.

In vitro receptor binding assays for Gonadorelin involve competition binding experiments using radiolabeled GnRH. Membranes are prepared from pituitary cells or cells expressing the GnRH receptor. Gonadorelin is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves. Functional assays measure LH and FSH release from cultured pituitary cells.

Cellular assays for Gonadorelin involve culturing pituitary gonadotroph cells. Cells are treated with Gonadorelin at varying concentrations. LH and FSH release into the culture medium is measured by ELISA or radioimmunoassay. Intracellular signaling pathways such as calcium mobilization and MAP kinase activation can also be assessed.

In vivo animal studies for Gonadorelin are conducted in cattle and other livestock species. The compound is typically administered intramuscularly or intravenously. In dairy cattle, it is used for the treatment of ovarian follicular cysts and for synchronization of estrus. Doses vary depending on the indication, with typical doses of 200 µg used for treatment of ovarian follicular cysts.

Absorption, Distribution and Excretion
Rapidly absorbed after injection. Metabolites/Metabolites Rapidly hydrolyzed into inactive peptide components. Biological Half-Life Extremely short, initial half-life is 2 to 10 minutes; terminal half-life is 10 to 40 minutes.
Gonadorelin is a synthetic peptide hormone that is rapidly metabolized and has a short half-life. It is administered via intramuscular or intravenous injection. The compound is typically supplied as a sterile powder for reconstitution. Detailed pharmacokinetic parameters have been characterized in clinical and veterinary studies. The compound is intended for research and veterinary use.

Gonadorelin is generally well-tolerated at therapeutic doses. In veterinary use, it has been shown to be safe for the treatment of ovarian follicular cysts in cattle. The compound is classified as Repr. 2 (suspected of damaging fertility or the unborn child). It should be handled with appropriate precautions.

Gonadorelin-releasing hormone (GnRH) is a deca-peptide composed of pyroglutyl, histidine, tryptophan, serine, tyrosyl, glycyl, leucyl, arginyl, prolyl, and glycamide residues linked in sequence. It is a gonadotropin-releasing hormone agonist. It is both an oligopeptide and a peptide hormone. Gonadotropin-releasing hormone (GnRH) is another name for gonadotropin-releasing hormone. It is a synthetic deca-peptide prepared using a solid-phase peptide synthesis method. GnRH is responsible for stimulating the anterior pituitary gland to release follicle-stimulating hormone (FSH) and luteinizing hormone (LHRH). Recombinant gonadotropin-releasing hormone (GnRH) is a synthetic LHRH, identical or similar to the endogenous hormone. Gonadotropin-releasing hormone (GnRH) is synthesized and secreted by the hypothalamus. It binds to transmembrane LHRH receptors on pituitary gonadotropin cells, thereby stimulating the synthesis and secretion of gonadotropins. Sustained administration of gonadotropin-releasing hormone (GnRH) desensitizes gonadotropin-releasing cells, a negative feedback effect. This drug can be used to treat hypothalamic amenorrhea and assess hypothalamic/pituitary function. 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: GnRH acetate (active ingredient); GnRH hydrochloride (active ingredient); GnRH diacetate tetrahydrate (active ingredient)...see more...

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Drug Indications
For assessing the function and response of anterior pituitary gonadotropin-releasing cells, and also for assessing residual pituitary gonadotropin function after surgical and/or radiotherapy resection of pituitary tumors. Mechanism of Action Systemic Effects: Similar to naturally occurring gonadotropin-releasing hormone (GnRH), GnRH primarily stimulates the anterior pituitary gland to synthesize and release luteinizing hormone (LH). GnRH also increases the production and release of follicle-stimulating hormone (FSH), but to a lesser extent. In prepubertal women and some patients with gonadal dysfunction, the FSH response may be stronger than the LH response. GnRH can be used to stimulate the hypothalamus to release GnRH physiologically to treat amenorrhea, delayed puberty, and infertility. It is used to treat infertility caused by delayed puberty and hypogonadotropic hypogonadism, and to induce ovulation in women with hypothalamic amenorrhea. This leads to elevated levels of pituitary gonadotropins LH and FSH, which in turn stimulate the gonads to produce reproductive steroids. Pharmacodynamics GnRH is responsible for promoting the release of follicle-stimulating hormone and luteinizing hormone from the anterior pituitary gland. In the pituitary gland, GnRH stimulates the synthesis and release of FSH and LH, a process regulated by the frequency and amplitude of GnRH pulses and feedback regulation by androgens and estrogens. Pulsatile secretion of gonadotropin-releasing hormone (GnRH) has been found in all vertebrates and is crucial for ensuring normal reproductive function. Therefore, the single hormone GnRH controls the complex processes of female follicle growth, ovulation, corpus luteum maintenance, and male spermatogenesis. Due to its short half-life, clinical application requires the use of an infusion pump.
Gonadorelin is a synthetic GnRH analog used to stimulate LH and FSH release. It is used in veterinary medicine for the treatment of ovarian follicular cysts in cattle and for synchronization of estrus. In humans, it is used for diagnostic testing of pituitary function. The compound is also known as Fertagyl and Luforan. It is not approved for human therapeutic use in many jurisdictions and is available for research and veterinary purposes.

C55H75N17O13

1182.2901

1181.572

33515-09-2

34973-08-5 (acetate); 33515-09-2;51952-41-1 (HCl);

638793

Typically exists as solid at room temperature

1.54

1.713

-2.53

16

15

31

85

2390

8

CC(C[C@H](NC(CNC([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)=O)C(N[C@H](C(N6CCC[C@H]6C(NCC(N)=O)=O)=O)CCCNC(N)=N)=O)C

XLXSAKCOAKORKW-AQJXLSMYSA-N

InChI=1S/C55H75N17O13/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)/t36-,37-,38-,39-,40-,41-,42-,43-/m0/s1

(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

Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)