| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
Purity: ≥98%
Protirelin (Thyrel TRH) is a novel, potent and highly conserved neuropeptide that exerts the hormonal control of thyroid-stimulating hormone (TSH) levels as well as neuromodulatory functions. Protirelin is used to treat hypothyroidism by stimulating the release of a hormone called thyroid-stimulating hormone, or TSH, from the anterior pituitary gland.
| Targets |
Protirelin (synthetic pQHP-NH₂) activates the human thyrotropin-releasing hormone receptor (TRHR) and the Caenorhabditis elegans TRHR ortholog TRHR-1. [1]
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| ln Vitro |
Protirelin (pQHP-NH₂) activated the C. elegans TRHR-1 expressed in CHO cells at a concentration of 10 µM in a calcium mobilization assay. [1]
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| ln Vivo |
The effect of thyrotropin-releasing hormone (Protirelin, TRH), one of the hypothalamic-releasing hormones, on body temperature in rats was studied. Protirelin was injected intraperitoneally at doses of 1, 5, 10 and 20 mg/kg into male Wistar rats weighing 200-250 g. Protirelin causes a dose-dependent transient increase in body temperature. Injection of 20 mg/kg Protirelin into thyroidectomized rats caused a significant increase in body temperature in sham-operated animals, but did not show an increase in body temperature. The current results indicate that thyroid hormones may have been involved in the control of postembryonic growth and reproduction in the past [1].
Intraperitoneal (i.p.) injection of Protirelin (TRH tartrate) at doses of 10 and 20 mg/kg induced a dose-dependent, transient hyperthermia in male Wistar rats (200-250 g). The hyperthermia appeared early, with a peak rise in rectal temperature (mean increase of 0.5°C to 1.5°C) observed at 40 minutes post-injection, and lasted for approximately 80 minutes. Doses of 1 and 5 mg/kg did not cause a significant temperature increase. [2] Thyroidectomized rats, which underwent surgery 10 days prior, failed to exhibit the hyperthermic response to a 20 mg/kg i.p. dose of Protirelin. In contrast, sham-operated animals showed a significant temperature rise with the same dose. This result suggests that the hyperthermic action of Protirelin in rats is mediated through the release of thyroid hormone. [2] |
| Enzyme Assay |
A luminescence-based calcium mobilization assay was used to measure GPCR activation. CHO cells expressing the receptor of interest, along with aequorin and a promiscuous human Gα subunit, were loaded with coelenterazine H. After peptide addition, luminescence was measured at 469 nm for 30 seconds. In this assay, Protirelin activated the C. elegans TRHR-1 at 10 µM. [1]
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| Animal Protocol |
Ninety male Wistar rats weighing 200-250 g were used. Protirelin tartrate was dissolved in physiological saline. In the first experiment, different groups of rats received a single intraperitoneal injection of the drug at doses of 1, 5, 10, or 20 mg/kg; a control group received saline only. Rectal temperature was measured using an electronic thermometer inserted 5 cm into the rectum, before and at various time points after injection. The experiment was conducted from 1 p.m. to 4 p.m. in a room maintained at 24 ± 1°C. [2]
In the second experiment, rats were subjected to thyroidectomy or sham surgery under thiopental sodium anesthesia. Ten days post-operation, thyroidectomized and sham-operated rats received a single intraperitoneal injection of either Protirelin (20 mg/kg) or saline. Rectal temperature was measured using the same method as in the first experiment. [2] |
| References | |
| Additional Infomation |
Thyrotropin-releasing hormone (TRH) is a tripeptide composed of L-pyroglutyl, L-histyl, and L-prolyl residues linked in sequence. It is a human metabolite, belonging to the peptide hormone and tripeptide class. TRH is a synthetic analog of endogenous peptide-based TRH and is currently used in pharmaceutical applications. It is a tripeptide troponin released by the hypothalamus, stimulating the anterior pituitary gland to release thyroid-stimulating hormone (TSH) and prolactin. Although no FDA-approved products currently contain TRH, it is a component of TRH testing, used to detect the anterior pituitary response in diseases such as secondary hypothyroidism and acromegaly. There are reports and data regarding the presence of TRH in humans. TRH is a tripeptide that stimulates the release of TSH and prolactin. It is synthesized by neurons in the paraventricular nucleus of the hypothalamus. After TRH (formerly known as TRF) is released into the pituitary portal circulation, it stimulates the anterior pituitary to release TSH and PRL.
See also: transferrin (note moved to). Thyrotropin-releasing hormone (pQHP-NH₂) is the synthetic form of thyrotropin-releasing hormone (TRH), a highly conserved tripeptide in vertebrates. It has been used as a reference ligand in comparative studies of cross-species TRH-like neuropeptide systems. In this study, it was used as a positive control to demonstrate cross-species activation of the TRH receptor. [1] |
| Molecular Formula |
C16H22N6O4
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|---|---|
| Molecular Weight |
362.3837
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| Exact Mass |
362.17
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| CAS # |
24305-27-9
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| Related CAS # |
Protirelin acetate;120876-23-5;Thyrotropin-Releasing Hormone (TRH), Free Acid;24769-58-2
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| PubChem CID |
638678
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
942.1±65.0 °C at 760 mmHg
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| Flash Point |
523.6±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.617
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| LogP |
-2.43
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
597
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CC2=CN=CN2)NC(=O)[C@@H]3CCC(=O)N3)C(=O)N
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| InChi Key |
XNSAINXGIQZQOO-SRVKXCTJSA-N
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| InChi Code |
InChI=1S/C16H22N6O4/c17-14(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/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25)/t10-,11-,12-/m0/s1
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| Chemical Name |
(S)-N-((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl)-5-oxopyrrolidine-2-carboxamide
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| Synonyms |
Synthetic thyrotropin-releasing hormone; TRF; TRH; TSH-RF; pGlu-His-Pro-NH2; {pGLU}HP-NH2; Protirelin; Antepan; Hirtonin; A-38579; A 38579; A38579; Thyrel TRH
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~689.88 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7595 mL | 13.7977 mL | 27.5953 mL | |
| 5 mM | 0.5519 mL | 2.7595 mL | 5.5191 mL | |
| 10 mM | 0.2760 mL | 1.3798 mL | 2.7595 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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