TCS 1102

Pricing Availability   Qty
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)
Datasheet
Citations (7)
Reviews
Literature (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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


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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:

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

Mavanji et al (2015) Promotion of Wakefulness and Energy Expenditure by Orexin-A in the Ventrolateral Preoptic Area. Sleep 38 1361 PMID: 25845696

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


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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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Peptides Involved in Appetite Modulation Scientific Review

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.