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Taltirelin (TA-0910) is at thyrotropin-releasing hormone receptor (TRH-R) superagonist (IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release))[1].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $59 | 5 days | 5 days |
| Description | Taltirelin (TA-0910) is at thyrotropin-releasing hormone receptor (TRH-R) superagonist (IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release))[1]. |
| Targets&IC50 | TRHR:910 nM (IC50) |
| In vivo | Taltirelin (TAL), in mouse models of CRF.?To model fatigue, we used a mouse model of chemotherapy, a mouse model of radiation therapy, and mice bearing colon 26 carcinoma tumors.?We used the treadmill fatigue test to assess fatigue-like behavior after treatment with TAL.?Additionally, we used wild-type and TRH receptor knockout mice to determine which TRH receptor was necessary for the actions of TAL.?Tumor-bearing mice displayed muscle wasting and all models caused fatigue-like behavior, with mice running a shorter distance in the treadmill fatigue test than controls.?TAL reversed fatigue-like behavior in all three models and the mouse TRH1 receptor was necessary for the effects of TAL.?These data suggest that TAL may be useful in alleviating fatigue in all cancer patients and provide further support for evaluating TAL as a potential therapy for CRF in humans[1]. |
| Synonyms | TA-0910 |
| Molecular Weight | 405.41 |
| Formula | C17H23N7O5 |
| Cas No. | 103300-74-9 |
| Smiles | CN1C(=O)C[C@H](NC1=O)C(=O)N[C@@H](CC1=CN=CN1)C(=O)N1CCC[C@H]1C(N)=O |
| Relative Density. | 1.447 g/cm3 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (74 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.93 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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