| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Thyrotropin-releasing hormone (TRH) receptor. TRH free acid is the physiological metabolite of TRH, which acts on the TRH receptor to stimulate TSH release from the pituitary gland.
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| ln Vitro |
Numerous biological processes connected to the endocrine and central nervous systems have been demonstrated to be impacted by the products of TRH breakdown. In brain tissue and plasma, TRH (pGlu-His-Pro-NH2) can be enzymatically broken down to yield TRH-OH. TRH and hGHRH increased the amount of [3H]GH released into the culture medium by 435% and 464%, respectively, in comparison to controls; TRH-OH had no impact [1]. A particular proline endopeptidase cleaves the C-terminal amide group to create TRH-OH. It is one among the most stable TRH derivatives and is found in large amounts throughout the brain. Mammalian septal neurons' Na+ channel activity is inhibited by TRH-OH. About 60% of the examined cells exhibited a dose-dependent reversible decrease of Na+ current when exposed to doses of TRH-OH ranging from 0.01 to 2.5 μM. The peak Na+ current amplitude is decreased by 20–50% when using 2 μM TRH-OH[2].
In vitro, TRH free acid is the physiological metabolite of TRH. TRH itself stimulates the anterior pituitary to release thyroid-stimulating hormone (TSH), which in turn regulates thyroid hormone production. Beyond endocrine function, TRH also acts as a neuromodulator in the central nervous system, influencing mood, arousal, and autonomic functions. |
| ln Vivo |
In vivo, TRH stimulates the anterior pituitary to release TSH, which regulates thyroid hormone production. TRH also acts as a neuromodulator in the central nervous system, influencing mood, arousal, and autonomic functions. TRH free acid is the physiological metabolite of TRH and may have similar biological activities.
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| Enzyme Assay |
Non-cell receptor binding assays are performed using membrane preparations from cells expressing the TRH receptor (e.g., pituitary cells). Radioligand binding studies are conducted using [³H]TRH or [³H]MeTRH as tracers. Membranes are incubated with the radioligand and varying concentrations of TRH free acid (0.001-100 μM). Nonspecific binding is determined with excess unlabeled TRH. After incubation at 4°C for 60-120 minutes, filtration and scintillation counting are performed. Ki values are calculated from competition curves.
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| Cell Assay |
Cellular assays are performed using pituitary cell lines (e.g., GH3 or AtT-20 cells) that express the TRH receptor. Cells are treated with TRH free acid at concentrations ranging from 0.01 nM to 10 μM. TSH release is measured by ELISA or RIA. Intracellular calcium mobilization is assessed using fluorescent calcium indicators (e.g., Fura-2) as a measure of TRH receptor activation. EC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies are conducted in rodent models. TRH or TRH free acid is administered via intravenous, intraperitoneal, or intracerebroventricular routes at doses ranging from 0.01-10 mg/kg. TSH and thyroid hormone levels are measured in serum at various time points. Behavioral and autonomic effects are assessed to evaluate central nervous system activity.
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| ADME/Pharmacokinetics |
TRH free acid (molecular weight: 363.37, CAS: 24769-58-2) is a physiological metabolite of TRH. It is soluble in water and PBS. The compound should be stored as a powder at -20°C or in solvent at -80°C for long-term preservation. TRH free acid is used as a research tool for studying the HPT axis and TRH receptor signaling.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for TRH free acid are limited. As a physiological metabolite of the endogenous hormone TRH, it is expected to have a favorable safety profile. No significant toxicity has been reported at physiological concentrations. High doses of TRH may cause endocrine and autonomic effects. The compound is for research use only.
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| References |
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| Additional Infomation |
TRH free acid (TRH-OH) is the physiological metabolite of thyrotropin-releasing hormone. TRH is a tripeptide hormone (pGlu-His-Pro-NH2) that regulates the hypothalamic-pituitary-thyroid axis. TRH also acts as a neuromodulator in the central nervous system. TRH free acid is used as a research tool for studying TRH receptor signaling and thyroid function. It is not approved for clinical use and is available for research purposes only.
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| Molecular Formula |
C16H21N5O5
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|---|---|
| Molecular Weight |
363.374
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| Exact Mass |
363.154
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| CAS # |
24769-58-2
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| Related CAS # |
Protirelin;24305-27-9;Protirelin acetate;120876-23-5
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| PubChem CID |
10428784
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.64g/cm3
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| Index of Refraction |
1.741
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| LogP |
2.767
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
598
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| Defined Atom Stereocenter Count |
3
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| SMILES |
O=C(O)[C@@H]1CCCN1C([C@@H](NC([C@@H]2CCC(N2)=O)=O)CC3=CN=CN3)=O
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| InChi Key |
ITYONPBTNRIEBA-SRVKXCTJSA-N
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| InChi Code |
InChI=1S/C16H21N5O5/c22-13-4-3-10(19-13)14(23)20-11(6-9-7-17-8-18-9)15(24)21-5-1-2-12(21)16(25)26/h7-8,10-12H,1-6H2,(H,17,18)(H,19,22)(H,20,23)(H,25,26)/t10-,11-,12-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carboxylic acid
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| Synonyms |
Pglu-his-pro; Deamido-TRH; TRH free acid
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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) |
H2O : ~100 mg/mL (~275.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (275.20 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Solubility in Formulation 2: 10 mg/mL (27.52 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7520 mL | 13.7601 mL | 27.5202 mL | |
| 5 mM | 0.5504 mL | 2.7520 mL | 5.5040 mL | |
| 10 mM | 0.2752 mL | 1.3760 mL | 2.7520 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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