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| Targets |
The primary target of GHRF is the growth hormone-releasing hormone receptor (GHRHR), also known as the GHRH receptor, which is a G protein-coupled receptor (GPCR) located on the surface of somatotroph cells in the anterior pituitary gland. Upon binding to GHRHR, the receptor stimulates the production of cAMP, which triggers the release of growth hormone from secretory vesicles.
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| ln Vitro |
The in vitro activity of mouse GHRF is classically evaluated using primary anterior pituitary cell cultures. In these assays, the peptide stimulates the synthesis and secretion of growth hormone (GH). The EC₅0 for GH release in rat pituitary cells is typically in the low nanomolar range (approximately 2-3 nM). The compound's activity can be measured by quantifying GH levels in the culture medium using ELISA or radioimmunoassay (RIA) after a defined incubation period (e.g., 30 minutes to 4 hours). The response is dose-dependent and can be suppressed by somatostatin.
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| ln Vivo |
In vivo, the activity of mouse GHRF is studied primarily to model the effects of growth hormone stimulation. In rodent models, intravenous or subcutaneous administration leads to a rapid, dose-dependent increase in serum growth hormone levels. This effect is widely used in research to investigate the physiology of the growth hormone axis. The in vivo formulation is often prepared using a vehicle such as 5% DMSO + 30% PEG300 + 5% Tween 80 + 60% saline.
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| Enzyme Assay |
Non-cell-based (cell-free) receptor binding assays for GHRF involve the use of membrane preparations from cells expressing the human or rodent GHRH receptor. A standard protocol uses ¹2⁵I-labeled GHRF or a GHRF analog in competition binding assays. Membranes (typically 10-50 microg) are incubated with a fixed concentration of radiolabeled tracer (e.g., 0.1-0.5 nM) and increasing concentrations of unlabeled GHRF (0.01-1000 nM). After incubation (e.g., 60 minutes at 25degC), bound and free radioligands are separated by rapid filtration through GF/B filters, and the radioactivity on the filters is measured using a scintillation counter. Non-specific binding is determined in the presence of a high concentration of unlabeled peptide (e.g., 1 microM). The binding affinity (Kd) and competitive inhibition (IC₅0) are calculated using curve-fitting software.
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| Cell Assay |
Cell-based assays for GHRF are typically conducted using primary cultures of rat pituitary cells or clonal cell lines such as GH3 or GH4C1. These cells are plated in multi-well plates and allowed to recover for 2-4 days. They are then treated with various concentrations of GHRF (e.g., 10 pM to 1 microM) for a defined period (e.g., 30 min for rapid release, or 4-24 h for synthesis studies). GH concentrations in the supernatant are quantified using a specific ELISA or RIA. For mechanistic studies, cells can be pre-treated with inhibitors of protein kinase A (PKA), phospholipase C (PLC), or calcium chelators to identify the signaling pathways involved.
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| Animal Protocol |
In vivo animal experiments for GHRF are often conducted in normal Sprague-Dawley rats. The peptide is administered via intravenous (IV) or subcutaneous (SC) injection at doses ranging from 1 to 100 microg/kg. Blood samples are collected from the tail vein at various time points (e.g., 0, 5, 10, 15, 30, 60 minutes) and serum GH levels are measured by ELISA. Pharmacokinetic (PK) and pharmacodynamic (PD) profiles are constructed to correlate plasma concentration with GH release. This model is also used to test the effects of GHRF receptor agonists and antagonists.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GHRF, mouse TFA are typical for a peptide hormone. After IV administration, the peptide is rapidly cleared from the circulation, with a short terminal half-life (typically 2-10 minutes). After SC administration, absorption is slower and a more sustained elevation of plasma GH levels is observed. The TFA salt provides improved stability and solubility in aqueous buffers. For storage, the peptide is kept as a powder at -20degC (stable for up to 3 years) or in a solvent at -80degC (stable for up to 1 year).
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| Toxicity/Toxicokinetics |
As a peptide hormone, the toxicity of GHRF is generally low at standard research doses. No significant toxic effects have been reported in animal studies at doses used for GH release (1-100 microg/kg). The peptide is species-specific; mouse GHRF is less active in humans. There are no significant safety concerns with proper handling. Standard laboratory safety precautions should be observed to avoid exposure through inhalation or injection.
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| References | |
| Additional Infomation |
Additional information: The compound has a molecular formula of C202H33₆N₆0O₆₉S, with a molecular weight of approximately 5030 g/mol (free base). It is supplied as a TFA salt to enhance solubility. It is used exclusively for research purposes and not for human consumption. Synonyms include Mouse growth hormone-releasing factor TFA and somatocrinin.
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| Molecular Formula |
C220H365N69O64S.XC2HF3O2
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| Molecular Weight |
5032.74 (free base)
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| Related CAS # |
GHRF, mouse
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| Sequence |
His-Val-Asp-Ala-Ile-Phe-Thr-Thr-Asn-Tyr-Arg-Lys-Leu-Leu-Ser-Gln-Leu-Tyr-Ala-Arg-Lys-Val-Ile-Gln-Asp-Ile-Met-Asn-Lys-Gln-Gly-Glu-Arg-Ile-Gln-Glu-Gln-Arg-Ala-Arg-Leu-SerHVDAIFTTNYRKLLSQLYARKVIQDIMNKQGERIQEQRARLS
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| Appearance |
White to off-white solid powder
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| Synonyms |
Mouse growth hormone-releasing factor TFA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (with sonication)
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| 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.) |
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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