TCS 1102

TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats[1].

Product Specifications

CAS Number

[916141-36-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/TCS-1102.html

Purity

99.73

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C([C@H]1N(C(CSC2=NC3=CC=CC=C3N2C)=O)CCC1)NC4=CC=CC=C4C5=CC=CC=C5

Molecular Formula

C27H26N4O2S

Molecular Weight

470.59

Precautions

H302, H315, H319, H335

References & Citations

[1]Bergman JM, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18 (4) :1425-30.|[2]Chen X, et al. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks. Brain Struct Funct. 2013 Aug 18.|[3]Turku A, et al. Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity. PLoS One. 2017 Jun 2;12 (6) :e0178526.