| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Taltirelin targets the thyrotropin-releasing hormone receptor (TRH-R). It acts as a superagonist at this receptor, binding with lower affinity (IC50 = 910 nM) compared to TRH (IC50 = 36 nM) in cells stably expressing TRH-R. It stimulates an increase in cytosolic Ca²⁺ concentration (Ca²⁺ release) with an EC50 of 36 nM. By activating TRH-R, it modulates neurotransmitter systems, including dopamine release and turnover.
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| ln Vitro |
In vitro, Taltirelin is a potent superagonist at the TRH receptor, with an IC50 of 910 nM and an EC50 of 36 nM for stimulating Ca²⁺ release. It binds to the human TRH receptor with lower affinity than TRH. In HEK-EM 293 cells stably expressing TRH-R, it stimulates an increase in cytosolic Ca²⁺ concentration. Its Ki values in the anterior pituitary, hypothalamus, and brain stem range from 145.5 to 170.4 nM.
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| ln Vivo |
Taltirelin demonstrates significant in vivo activity. It increases the extracellular levels of dopamine (DA) and its metabolites, DOPAC and homovanillic acid, in the rat brain at doses of 1-10 mg/kg. In mouse models of cancer-related fatigue, it reverses fatigue-like behavior, an effect dependent on the mouse TRH1 receptor. It also reduces mechanical allodynia by activating descending monoaminergic neurons in persistent inflammatory pain models. It has neuroprotective effects in cellular and animal models of Parkinson's disease.
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| Enzyme Assay |
In vitro receptor binding assays for Taltirelin involve measuring its affinity for the TRH receptor. Membrane preparations from cells expressing human TRH-R are incubated with radiolabeled ligands, such as [³H]MeTRH, and varying concentrations of Taltirelin. Non-specific binding is determined in the presence of excess unlabeled ligand. Bound radioactivity is collected by filtration and quantified by scintillation counting. Ki values are calculated from competition curves.
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| Cell Assay |
In vitro cell-based functional assays use cells, such as HEK-EM 293 cells, stably expressing the human TRH receptor. Cells are loaded with a calcium-sensitive fluorescent indicator and treated with varying concentrations of Taltirelin (typically 0.1-1000 nM). Receptor activation is measured as changes in fluorescence intensity due to Ca²⁺ release. EC50 values are calculated from concentration-response curves.
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| Animal Protocol |
In vivo animal studies are typically conducted in rodent models. For assessing dopamine release, rats are administered Taltirelin (1-10 mg/kg) and microdialysis is used to measure extracellular levels of DA and its metabolites in the brain. For cancer-related fatigue, mouse models of chemotherapy, radiation therapy, or tumor-bearing mice are used. Fatigue-like behavior is assessed using a treadmill fatigue test. For neuroprotection, cellular and animal models of Parkinson's disease are employed.
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| ADME/Pharmacokinetics |
Taltirelin is orally active and can cross the blood-brain barrier. It is a metabolically stable TRH analog. It has a substantially longer half-life and longer duration of action than TRH. For in vivo formulation, it can be prepared in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline at 2 mg/mL. Powder can be stored at -20°C for 3 years and in solvent at -80°C for 1 year. Its tetrahydrate form is approved in Japan.
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| Toxicity/Toxicokinetics |
In 13-week toxicology studies, animals receiving 5 or 50 mg/kg showed a decrease in body weight or suppression of body weight gain, and a decrease in food intake. Toxicokinetic data suggested no alterations in metabolism with repeated treatment. The acute oral LD50 in mice and rats is >4000 mg/kg.
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| References | |
| Additional Infomation |
Talirelin is an oligopeptide composed of (4S)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxylic acid, L-histidine, and L-proline linked sequentially by peptide bonds. It is a thyrotropin-releasing hormone (TRH) analog. Its tetrahydrate form has been approved in Japan for the treatment of spinal muscular atrophy. It possesses nootropic, neuroprotective, and analgesic effects.
Taltirelin (TA-0910), marketed as Ceredist, is the only TRH analog with proven clinical efficacy in a multi-center, double-blind, placebo-controlled trial for spinocerebellar degeneration. It has nootropic, neuroprotective, and analgesic effects. It has been evaluated for its potential to alleviate fatigue in cancer patients and for neuroprotective effects in Parkinson's disease models. Its tetrahydrate form has been approved in Japan for the treatment of spinal muscular atrophy. |
| Molecular Formula |
C17H23N7O5
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|---|---|
| Molecular Weight |
405.41
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| Exact Mass |
405.176
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| Elemental Analysis |
C, 50.36; H, 5.72; N, 24.18; O, 19.73
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| CAS # |
103300-74-9
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| Related CAS # |
Taltirelin acetate;1549593-23-8;Taltirelin-13C,d3
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| PubChem CID |
114750
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Melting Point |
72-75°
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| Index of Refraction |
1.612
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| LogP |
-4.09
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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 |
29
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| Complexity |
714
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| Defined Atom Stereocenter Count |
3
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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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| InChi Key |
LQZAIAZUDWIVPM-SRVKXCTJSA-N
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| InChi Code |
InChI=1S/C17H23N7O5/c1-23-13(25)6-10(22-17(23)29)15(27)21-11(5-9-7-19-8-20-9)16(28)24-4-2-3-12(24)14(18)26/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29)/t10-,11-,12-/m0/s1
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| Chemical Name |
(4S)-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide
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| Synonyms |
Taltirelin; CCRIS 8513; TA 0910; TA0910; TA-0910
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 (~246.66 mM)
H2O : ~100 mg/mL (~246.66 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (246.66 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4666 mL | 12.3332 mL | 24.6664 mL | |
| 5 mM | 0.4933 mL | 2.4666 mL | 4.9333 mL | |
| 10 mM | 0.2467 mL | 1.2333 mL | 2.4666 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04107740 | Completed | Drug: C-Trelin OD Tab (5mg Taltirelin Hydrate) |
Spinocerebellar Degeneration | HLB Pharmaceutical Co., Ltd. | March 4, 2019 | Phase 4 |
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