| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Protirelin Acetate primarily targets the thyrotropin-releasing hormone receptor (TRHR), a G protein-coupled receptor expressed on the surface of pituitary thyrotrophs and lactotrophs. By binding to and activating this receptor, it stimulates the release of thyroid-stimulating hormone (TSH) and prolactin from the anterior pituitary. TSH subsequently stimulates the thyroid gland to produce and release thyroid hormones (T4 and T3). Protirelin also has neuromodulatory functions in the central nervous system, where it acts as a neurotransmitter or neuromodulator. Its effects are mediated through the TRHR, which is widely distributed in the brain.
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| ln Vitro |
In vitro, Protirelin Acetate stimulates the release of thyrotropin (TSH) and prolactin from anterior pituitary cells in culture. Its activity is assessed by measuring the secretion of these hormones into the culture medium. The compound binds specifically to the TRHR with high affinity, activating the receptor and downstream signaling pathways. Protirelin has been shown to have neuroprotective effects in some in vitro models, potentially through the modulation of neurotransmitter release and reduction of excitotoxicity.
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| ln Vivo |
Protirelin (TRH), a neuropeptide with a long evolutionary history that precedes the split between protostomes and deuterostomes, may have played an ancestral role in regulating postembryonic development and reproduction [1]. Rats' body temperature was examined in relation to thyrotropin-releasing hormone (Protirelin, TRH), one of the hypothalamic-releasing hormones. Male Wistar rats weighing 200–250 g were intraperitoneally given dosages of 1, 5, 10, and 20 mg/kg of protetin. The temporary, dose-dependent elevation of body temperature is brought on by protelin. When 20 mg/kg Protirelin was injected into rats after thyroidectomies, the animals' body temperature rose significantly while they were not actually surgically operated on. According to the current findings, protirelin's tendency to cause hyperthermia may be influenced by thyroid hormone secretion [2].
In vivo, Protirelin Acetate is used as a diagnostic agent to assess thyroid function and pituitary responsiveness. The TRH Test involves the administration of Protirelin and the subsequent measurement of TSH levels in the blood to evaluate the function of the hypothalamic-pituitary-thyroid axis. The compound has also been studied for its potential therapeutic effects in neurological and psychiatric disorders due to its neurostimulatory and antidepressant-like activities. In animal models, Protirelin has been shown to have antidepressant-like effects and to improve cognitive function. |
| Enzyme Assay |
The in vitro activity of Protirelin Acetate is assessed using primary anterior pituitary cell cultures or cell lines expressing the TRHR (e.g., GH3 cells). Cells are cultured in appropriate media and treated with various concentrations of Protirelin Acetate (typically 0.1 nM to 10 µM) for 1-24 hours. TSH and prolactin levels in the culture medium are measured by radioimmunoassay or ELISA. The activation of downstream signaling pathways (e.g., PLC, MAPK) is assessed by measuring intracellular calcium levels using fluorescent dyes (e.g., Fura-2) or by Western blotting using phospho-specific antibodies.
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| Cell Assay |
For cellular assays, GH3 rat pituitary cells or primary anterior pituitary cells are used. Cells are cultured in appropriate media and treated with various concentrations of Protirelin Acetate (typically 0.1 nM to 10 µM) for defined periods. TSH and prolactin secretion is measured by ELISA or radioimmunoassay. Intracellular calcium levels are measured using fluorescence microscopy or plate readers with calcium-sensitive dyes. Cell proliferation is assessed using MTT or CellTiter-Glo assays. The expression of TSH and prolactin genes is analyzed by qPCR.
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| Animal Protocol |
In vivo, Protirelin Acetate is typically administered intravenously or intramuscularly as a diagnostic agent. In the TRH Test, a dose of 200-500 µg of Protirelin is administered to patients, and blood samples are collected at various time points (0, 20, 30, and 60 minutes) for TSH measurement. In animal studies, Protirelin is administered intraperitoneally or intracerebroventricularly at doses ranging from 0.1 to 10 mg/kg. The effects on behavior, cognitive function, and hormone levels are assessed. In toxicological studies, the compound is administered at various doses, and clinical chemistry, hematology, and histopathology are evaluated.
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| ADME/Pharmacokinetics |
Protirelin Acetate has a short half-life in the circulation (approximately 2-6 minutes) due to rapid degradation by peptidases. It is administered as a bolus injection for diagnostic purposes. The compound is metabolized by pyroglutamyl peptidase and prolyl endopeptidase, producing inactive metabolites that are excreted in urine. Its rapid degradation limits its therapeutic utility but makes it suitable for diagnostic testing. The compound is soluble in water and DMSO.
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| Toxicity/Toxicokinetics |
Protirelin Acetate is generally well-tolerated at diagnostic doses. Common side effects include nausea, flushing, dizziness, headache, and a transient increase in blood pressure. These effects are typically mild and self-limiting. At higher doses, the compound may cause more pronounced effects, including gastrointestinal disturbances and changes in heart rate. The compound is contraindicated in patients with hypersensitivity to Protirelin or its components. It should be used with caution in patients with cardiovascular disease or epilepsy.
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| References | |
| Additional Infomation |
Protirelin Acetate is a diagnostic agent used in the TRH Test to evaluate hypothalamic-pituitary-thyroid axis function. It is not currently available in any FDA-approved product but remains an important diagnostic tool in some countries. The compound has also been studied for its potential therapeutic applications in neurological and psychiatric disorders, including depression, Alzheimer's disease, and spinal cord injury, due to its neurostimulatory and neuromodulatory effects. Its role as a highly conserved neuropeptide that emerged before the divergence of protostomes and deuterostomes makes it a compound of evolutionary and physiological interest. Protirelin Acetate is available from chemical suppliers for research purposes.
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| Molecular Formula |
C38H56N12O14
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| Molecular Weight |
904.923248291016
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| Exact Mass |
904.403
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| CAS # |
120876-23-5
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| Related CAS # |
Protirelin;24305-27-9;Thyrotropin-Releasing Hormone (TRH), Free Acid;24769-58-2
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| PubChem CID |
138376494
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
64
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| Complexity |
628
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C([C@H](CC1=CN=CN1)NC([C@@H]1CCC(N1)=O)=O)N1CCC[C@H]1C(N)=O.O=C([C@H](CC1=CN=CN1)NC([C@@H]1CCC(N1)=O)=O)N1CCC[C@H]1C(N)=O.OC(C)=O.OC(C)=O.OC(C)=O
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| InChi Key |
FCUSEANSBYKTPA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/2C16H22N6O4.3C2H4O2/c2*17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10;3*1-2(3)4/h2*7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25);3*1H3,(H,3,4)
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| Chemical Name |
acetic acid;N-[1-(2-carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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| Synonyms |
TRF Acetate; Thyrotropin-releasing hormone; Protirelin Acetate
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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 : ~250 mg/mL (~552.54 mM)
H2O : ~50 mg/mL (~110.51 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (221.01 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1051 mL | 5.5254 mL | 11.0507 mL | |
| 5 mM | 0.2210 mL | 1.1051 mL | 2.2101 mL | |
| 10 mM | 0.1105 mL | 0.5525 mL | 1.1051 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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