Taltirelin

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[1][2][3].

Product Specifications

CAS Number

[103300-74-9]

Product Name Alternative

TA-0910

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Thyroid Hormone Receptor

Type

Reference compound

Related Pathways

Apoptosis; Vitamin D Related/Nuclear Receptor

Applications

Neuroscience-Neuromodulation

Field of Research

Endocrinology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Taltirelin.html

Concentration

10mM

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=C(N(CCC1)[C@@H]1C(N)=O)[C@@H](NC([C@@H](NC2=O)CC(N2C)=O)=O)CC3=CN=CN3

Molecular Formula

C17H23N7O5

Molecular Weight

405.41

Precautions

H302, H315, H319, H335

References & Citations

[1]Thirunarayanan N, et al. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne) . 2012 Oct 9;3:120.|[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.|[3]Dougherty JP, et al. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue. Pharmacol Res. 2017 Oct;124:1-8.