Taltirelin acetate
Based on 1 publication(s) in Google Scholar
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). 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.
For research use only. We do not sell to patients.
- Purity : 99.75%
- CAS No.: 1549593-23-8
- Formula: C19H27N7O7
- Molecular Weight:465.46
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-B0596
TaltirelinThyroid Hormone Receptor Agonist -
HY-A0070
Liothyronine sodiumTRα/TRβ Agonist -
HY-14823
SobetiromeTRβ Agonist -
HY-A0070R
Liothyronine sodium (Standard)TRα/TRβ Agonist -
HY-18341A
L-Thyroxine sodium salt pentahydrateThyroid Hormone -
HY-B1201
TiratricolThyroid Hormone Receptor Inhibitor -
HY-12216
ResmetiromTHR-β Agonist -
HY-108742
AbaloparatidePTHR1 Activator -
HY-B0208
MethimazoleAnti-thyroid Agent -
HY-W010696
Reverse T3Thyroid Hormone -
HY-111288
MB-07811
Publications Citing Use of MedChemExpress (MCE) Taltirelin acetate
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Biological Activity
Description
IC50 & Target
IC50: 910 nM (Thyrotropin-releasing hormone receptor)[1]
In Vitro
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. Further protocols information, click here.
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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
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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.
In Vivo
Taltirelin (0.2-5 mg/kg; Intraperitoneal injection; 14-56 days) has a neuroprotective effect in mouse models of MPTP (HY-15608) and chronic rotenone (HY-B1756) -induced PD, and improves locomotor function in mice [2].
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1549593-23-8
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Appearance Solid
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Molecular Weight 465.46
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Formula C19H27N7O7
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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.CC(O)=O
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Synonyms
TA-0910 acetate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (268.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (4.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1484 mL | 10.7421 mL | 21.4841 mL | 53.7103 mL |
| 5 mM | 0.4297 mL | 2.1484 mL | 4.2968 mL | 10.7421 mL | |
| 10 mM | 0.2148 mL | 1.0742 mL | 2.1484 mL | 5.3710 mL | |
| 15 mM | 0.1432 mL | 0.7161 mL | 1.4323 mL | 3.5807 mL | |
| 20 mM | 0.1074 mL | 0.5371 mL | 1.0742 mL | 2.6855 mL | |
| 25 mM | 0.0859 mL | 0.4297 mL | 0.8594 mL | 2.1484 mL | |
| 30 mM | 0.0716 mL | 0.3581 mL | 0.7161 mL | 1.7903 mL | |
| 40 mM | 0.0537 mL | 0.2686 mL | 0.5371 mL | 1.3428 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4297 mL | 1.0742 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3581 mL | 0.8952 mL | |
| 80 mM | 0.0269 mL | 0.1343 mL | 0.2686 mL | 0.6714 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5371 mL |
Taltirelin acetate Related Classifications
HY-B0596A Related Classifications
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