TCS 1102

Cat. No. 3818

TCS 1102 C27H26N4O2S [916141-36-1]

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Chemical Name: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide

Biological Activity

Potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). Inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo. Brain penetrant.

Licensing Information

Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)

Technical Data

M.Wt:
470.59
Formula:
C27H26N4O2S
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at RT
CAS No:
916141-36-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Winrow et al (2010) Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure. Neuropharmacology 58 185. PMID: 19596018.

Bergman et al (2008) Proline bis-amides as potent dual orexin receptor antagonists. Bioorg.Med.Chem.Letts 18 1425.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for TCS 1102 include:

Dong et al (2015) Blocking of orexin receptors in the paraventricular nucleus of the thalamus has no effect on the expression of conditioned fear in rats. Front Behav Neurosci 9 161. PMID: 26136671.

Putula et al (2014) Calcium affects OX1 orexin (hypocretin) receptor responses by modifying both orexin binding and the signal transduction machinery. Br J Pharmacol 171 5816. PMID: 25132134.

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Keywords: TCS 1102, supplier, TCS1102, orexin, receptors, OX1, OX2, antagonists, non-selective, dual, potent, merck, Tocris Bioscience, Non-selective Orexin Antagonist products

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