A superagonist of TRH1 and TRH2 receptors
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Taltirelin (trifluoroacetate salt)

Item No. 46438

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
hexahydro-1-methyl-2,6-dioxo-4S-pyrimidinecarbonyl-L-histidyl-L-prolinamide, methyl ester, monotrifluoroacetate salt
CAS Number
1549593-18-1
Synonyms
  • TA-0910
Molecular Formula
C17H23N7O5 • CF3COOH
Formula Weight
519.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
O=C([C@@H]1CCCN1C([C@H](CC2=CN=CN2)NC([C@H]3NC(N(C(C3)=O)C)=O)=O)=O)N.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C17H23N7O5.C2HF3O2/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;3-2(4,5)1(6)7/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29);(H,6,7)/t10-,11-,12-;/m0./s1
InChi Key
MPHHNZYPQHGMFE-LFELFHSZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $89

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    Taltirelin is a superagonist of thyrotropin-releasing hormone (TRH) receptors and a derivative of TRH.1 It increases intracellular calcium levels in HEK293 cells expressing the mouse TRH1 or TRH2 receptors (EC50s = 2 and 0.12 nM, respectively).2 Taltirelin (5 µM) reduces rotenone-induced production of reactive oxygen species (ROS) and MPP+-induced increases in the levels of phosphorylated tau and α-synuclein fragments in SH-SY5Y cells.3 It also prevents MPP+-induced decreases in the viability of SH-SY5Y cells. Taltirelin (1 mg/kg) improves motor function in a mouse model of Parkinson’s disease induced by rotenone (Item No. 13995). It also reduces mechanical allodynia in a mouse model of inflammatory pain, an effect that can be prevented by yohimbine (Item No. 19869) or WAY-100635 (Item No. 14599).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Thirunarayanan, N., Raaka, B.M., and Gershengorn, M.C. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Front. Endocrinol. (Lausanne) 3, 120 (2012).

    2. Thirunarayanan, N., Nir, E.A., Raaka, B.M., et al. Thyrotropin-releasing hormone receptor type 1 (TRH-R1), not TRH-R2, primarily mediates taltirelin actions in the CNS of mice. Neuropsychopharmacology 38(6), 950-956 (2013).

    3. Zheng, C., Chen, G., Tan, Y., et al. TRH analog, taltirelin protects dopaminergic neurons from neurotoxicity of MPTP and rotenone. Front. Cell. Neurosci. 12, 485 (2018).

    4. Eto, K., Kim, S.K., Nabekura, J., et al. Taltirelin, a thyrotropin-releasing hormone analog, alleviates mechanical allodynia through activation of descending monoaminergic neurons in persistent inflammatory pain. Brain Res. 1414, 50-57 (2011).