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-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 Gonadorelin-releasing hormone agonist. It is both an oligopeptide and a peptide hormone. Gonadorelin-releasing hormone (GnRH) is another name for Gonadorelin-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 Gonadorelin-releasing hormone (GnRH) is a synthetic LHRH, identical or similar to the endogenous hormone. Gonadorelin-releasing hormone (GnRH) is synthesized and secreted by the hypothalamus. It binds to transmembrane LHRH receptors on pituitary Gonadorelin cells, thereby stimulating the synthesis and secretion of Gonadorelins. Sustained administration of Gonadorelin-releasing hormone (GnRH) desensitizes Gonadorelin-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 Gonadorelins (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 Gonadorelin-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 Gonadorelin-releasing cells, and also for assessing residual pituitary Gonadorelin function after surgical and/or radiotherapy resection of pituitary tumors. Mechanism of Action Systemic Effects: Similar to naturally occurring Gonadorelin-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 Gonadorelins 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 Gonadorelin-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.

C55H75N17O13

1182.2901

1181.573

71447-49-9

34973-08-5 (acetate); 33515-09-2;51952-41-1 (HCl);499785-55-6(monoacetate); 78308-49-3 (diacetate hydrate); 71447-49-9 (diacetate);

638793

Typically exists as solid at room temperature

1.289

16

15

31

85

2390

8

O=C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])N([H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C(C([H])([H])N([H])C([C@]([H])(C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])O[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)N([H])C([C@]([H])(C([H])([H])C1=C([H])N=C([H])N1[H])N([H])C([C@]1([H])C([H])([H])C([H])([H])C(N1[H])=O)=O)=O)=O)=O)=O)=O)=O)N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])C([H])([H])C(N([H])[H])=O)=O

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

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.)