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| Targets |
(Glu2)-TRH targets the TRH receptor, a G-protein coupled receptor expressed in the central nervous system and pituitary. It acts as a functional antagonist of TRH by binding to its receptors without activating them, thereby negatively modulating the cholinergic effects of TRH in the mouse brain.
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| ln Vitro |
In vitro, (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. It acts as a negative modulator of the cholinergic effect of TRH. The compound is resistant to degradation by thyroliberinase, making it more stable than native TRH in cell-based assays.
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| ln Vivo |
(Glu2)-TRH (1-100 μmol/kg; intravenously) alleviates TRH-induced excitatory effects in a dose-dependent manner [1]. When compared to the vehicle-treated group, (Glu2)-TRH (10 μmol/kg; i.v.) given 10 minutes prior to pentobarbital (60 mg/kg; i.p.) decreased sleep duration by around 20% [1].
In vivo, (Glu2)-TRH displays neuroprotective, antidepressant, and anticonvulsant properties in the central nervous system. It is studied for its potential in modulating thyroid function and its use in research on neuroendocrine signaling. The compound may have therapeutic applications in conditions like hypothyroidism and metabolic disorders. |
| Enzyme Assay |
Receptor binding assays for (Glu2)-TRH use membrane preparations from cells expressing the TRH receptor. Radiolabeled TRH is incubated with varying concentrations of the test compound, and binding affinity is determined by competition binding curves.
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| Cell Assay |
Cellular assays for (Glu2)-TRH typically use neuronal cell cultures or cells expressing the TRH receptor. Acetylcholine release is measured in hippocampal slices or cultures to assess the compound's modulatory effects on cholinergic transmission. Calcium mobilization and signaling pathways can also be evaluated.
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| Animal Protocol |
Animal/Disease Models: Male Swiss-Webster mouse (30 g) [1]
Doses: 1, 2, 5, 10, 15, 25, 50, 100 μmol/kg Route of Administration: IV; Pentobarbital (60 mg/kg , intraperitoneal (ip) injection) Results for the first 10 minutes: TRH-induced (10 μmol/kg; intravenous (iv) (iv)injection) stimulant effects were attenuated in a dose-dependent manner. In vivo studies with (Glu2)-TRH are conducted in rodent models. The compound is typically administered via intravenous, intraperitoneal, or intracerebroventricular injection. Behavioral assays for antidepressant and anticonvulsant activity are performed, and neuroprotective effects are assessed in models of neurodegeneration. |
| ADME/Pharmacokinetics |
(Glu2)-TRH is resistant to metabolism by thyroliberinase, giving it greater metabolic stability than native TRH. The compound is expected to have a longer half-life in circulation and tissues compared to TRH. Standard peptide storage conditions apply.
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| Toxicity/Toxicokinetics |
Toxicity data for (Glu2)-TRH are limited. The compound is generally considered to be well-tolerated. Standard safety precautions for laboratory handling of research compounds should be followed.
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| References | |
| Additional Infomation |
Pglu-glu-pro-amide is an oligopeptide.
(Glu2)-TRH is a research-use compound and is not approved for therapeutic applications. It is also known as a thyrotropin-releasing hormone analogue. The compound is used to study TRH receptor pharmacology, neuroendocrine signaling, and the cholinergic system. It is available from multiple research suppliers. |
| Molecular Formula |
C15H22N4O6
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|---|---|
| Molecular Weight |
354.36
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| Exact Mass |
354.154
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| CAS # |
85541-78-2
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| PubChem CID |
122148
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| Appearance |
White to off-white solid powder
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| Density |
1.416g/cm3
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| Boiling Point |
899.9ºC at 760 mmHg
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| Flash Point |
498ºC
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| Index of Refraction |
1.575
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| LogP |
-2.7
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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 |
7
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| Heavy Atom Count |
25
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| Complexity |
593
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N
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| InChi Key |
HYZBGWLLSXSYLX-GUBZILKMSA-N
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| InChi Code |
InChI=1S/C15H22N4O6/c16-13(23)10-2-1-7-19(10)15(25)9(4-6-12(21)22)18-14(24)8-3-5-11(20)17-8/h8-10H,1-7H2,(H2,16,23)(H,17,20)(H,18,24)(H,21,22)/t8-,9-,10-/m0/s1
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| Chemical Name |
(4S)-5-[(2S)-2-carbamoylpyrrolidin-1-yl]-5-oxo-4-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoic 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 (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 : ~100 mg/mL (~282.20 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 | 2.8220 mL | 14.1099 mL | 28.2199 mL | |
| 5 mM | 0.5644 mL | 2.8220 mL | 5.6440 mL | |
| 10 mM | 0.2822 mL | 1.4110 mL | 2.8220 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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