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Description: Potent, dual orexin receptor antagonist
Chemical Name: N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
Purity: ≥98% (HPLC)
Biological Activity for TCS 1102
TCS 1102 is a 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 and blocks orexin-A (Cat.No.1455) mediated increases in feeding behaviour. 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 for TCS 1102
| M. Wt | 470.59 |
| Formula | C27H26N4O2S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 916141-36-1 |
| PubChem ID | 11960895 |
| InChI Key | YSBGRVXJEMSEQY-DEOSSOPVSA-N |
| Smiles | O=C(CSC2=NC(C=CC=C5)=C5N2C)N1CCC[C@H]1[C@](NC3=CC=CC=C3C4=CC=CC=C4)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TCS 1102
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.06 | 100 | |
| ethanol | 47.06 | 100 |
Preparing Stock Solutions for TCS 1102
The following data is based on the product molecular weight 470.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.12 mL | 10.62 mL | 21.25 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.25 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets for TCS 1102
References for TCS 1102
References are publications that support the biological activity of the product.
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
Khoo et al (2017) The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One 12 e0173967 PMID: 28296947
If you know of a relevant reference for TCS 1102, please let us know.
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Keywords: TCS 1102, TCS 1102 supplier, TCS1102, orexin, receptors, OX1, OX2, antagonists, non-selective, dual, potent, merck, Non-selective, Orexin, 3818, Tocris Bioscience
7 Citations for TCS 1102
Citations are publications that use Tocris products. Selected citations for TCS 1102 include:
Korim et al (2014) Orexinergic activation of medullary premotor neurons modulates the adrenal sympathoexcitation to hypothalamic glucoprivation. Diabetes 63 1895 PMID: 24550189
Yu et al (2023) Circadian regulation of developmental synaptogenesis via the hypocretinergic system. Nat Commun 14 3195 PMID: 37268623
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
Mavanji et al (2015) Promotion of Wakefulness and Energy Expenditure by Orexin-A in the Ventrolateral Preoptic Area. Sleep 38 1361 PMID: 25845696
Daniel J et al (2021) Orexin Modulation of VTA Dopamine Neuron Activity: Relevance to Schizophrenia. Int J Neuropsychopharmacol 24 344-353 PMID: 33587746
Khoo et al (2017) The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One PMID: 28296947
Do you know of a great paper that uses TCS 1102 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.