Taltirelin
Based on 1 publication(s) in Google Scholar
Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca2+ concentration (Ca2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue.
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- Pureza: 99.91%
- No. CAS: 103300-74-9
- Fòrmula: C17H23N7O5
- Peso molecular:405.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Taltirelin
More
Actividad biológica
IC50: 910 nM (Thyrotropin-releasing hormone receptor)[1]
Taltirelin (5 μM; 2 h) improves cell viability, reducess ROS production and apoptosis in MPP+ (HY-W008719) or Rotenone (HY-B1756) treated SH-SY5Y cells and primary rat midbrain neurons[2].
Taltirelin (5 μM; 2 h) exerts neuroprotective effects by inhibiting tau phosphorylation and AEP activation in SH-SY5Y cells treated with MPP+ (HY-W008719) or rotenone (HY-B1756)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y neuroblastoma cells and primary neonatal rat midbrain neurons
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Concentration:5 μM
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Incubation Time:2 h
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Result:Increased cell viability.
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Cell Line:SH-SY5Y neuroblastoma cells
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Concentration:5 μM
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Incubation Time:2 h
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Result:Prevented the elevation of the cleaved caspase-3.
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Cell Line:SH-SY5Y neuroblastoma cells and primary neonatal rat midbrain neurons
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Concentration:5 μM
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Incubation Time:2 h
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Result:Reduced the levels of p-tau and AEP cleavage products: tau N368 and a-synuclein N103 fragments.
Taltirelin (1 mg/kg Intraperitoneal injection; 10 mg/kg Oral administration; 1 day) alleviates the fatigue-like behavior caused by chemotherapy treatment, tumor burden and irradiation in mouse models [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MPTP (HY-15608) or Rotenone (HY-B1756) treated male C57/BL6 mice aged 8-9 weeks old[2]
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Dosage:0.2 mg/kg, 1 mg/kg, 5 mg/kg 14 days; 0.2 mg/kg, 1 mg/kg 56 days
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Administration:Intraperitoneal injection (i.p.)
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Result:Improved the locomotor function and preserved dopaminergic neurons in the substantia nigra.
Down-regulated the levels of p-tau (S396), p-α-synuclein (S129) tau N368 and α-synuclein N103 fragments in substantia nigra and striatum.
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Animal Model:5-FU (HY-90006) or radiation treated adult C57BL/6NCr mice aged 7-8 weeks;
Balb/cAnNCr mice aged 9 weeks old with colon 26 carcinoma[3] -
Dosage:1mg/kg;
10mg/kg -
Administration:Intraperitoneal injection (i.p.);
Oral administration (p.o.);
Twice a day before the test and once again 30 minutes prior to the test. -
Result:Reversed the fatigue-like effect, caused mice to run nearer to the top of the treadmill during the test.
Chemical Information
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No. CAS 103300-74-9
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Appearance Solid
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Peso molecular 405.41
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Fòrmula C17H23N7O5
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Color White to off-white
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SMILES
O=C(N(CCC1)[C@@H]1C(N)=O)[C@@H](NC([C@@H](NC2=O)CC(N2C)=O)=O)CC3=CN=CN3
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Synonyms
TA-0910
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Mol Neurosci
A Ketogenic Diet Affects Gut Microbiota by Regulating Gut Microbiota and Promoting Hippocampal TRHR Expression to Combat Seizures. [Abstract]2024 Nov 3;74(4):104. PMID: 39489848
Solvente y solubilidad
DMSO : 100 mg/mL (246.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (246.66 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (246.66 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Thirunarayanan N, et al. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne). 2012 Oct 9;3:120. [Content Brief]
[2]. Zheng C, et al. TRH Analog, Taltirelin Protects Dopaminergic Neurons From Neurotoxicity of MPTP and Rotenone. Front Cell Neurosci. 2018 Dec 20;12:485. [Content Brief]
[3]. Dougherty JP, et al. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue. Pharmacol Res. 2017 Oct;124:1-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.4666 mL | 12.3332 mL | 24.6664 mL | 61.6660 mL |
| 5 mM | 0.4933 mL | 2.4666 mL | 4.9333 mL | 12.3332 mL | |
| 10 mM | 0.2467 mL | 1.2333 mL | 2.4666 mL | 6.1666 mL | |
| 15 mM | 0.1644 mL | 0.8222 mL | 1.6444 mL | 4.1111 mL | |
| 20 mM | 0.1233 mL | 0.6167 mL | 1.2333 mL | 3.0833 mL | |
| 25 mM | 0.0987 mL | 0.4933 mL | 0.9867 mL | 2.4666 mL | |
| 30 mM | 0.0822 mL | 0.4111 mL | 0.8222 mL | 2.0555 mL | |
| 40 mM | 0.0617 mL | 0.3083 mL | 0.6167 mL | 1.5416 mL | |
| 50 mM | 0.0493 mL | 0.2467 mL | 0.4933 mL | 1.2333 mL | |
| 60 mM | 0.0411 mL | 0.2056 mL | 0.4111 mL | 1.0278 mL | |
| 80 mM | 0.0308 mL | 0.1542 mL | 0.3083 mL | 0.7708 mL | |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2467 mL | 0.6167 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Taltirelin Related Classifications
HY-B0596 Related Classifications
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