TCS 1102

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Cat.No. 3818 - TCS 1102 | C27H26N4O2S | CAS No. 916141-36-1
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 (5)
Reviews
Literature

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 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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 47.06 100
DMSO 47.06 100

Preparing Stock Solutions

The following data is based on the product molecular weight 470.59. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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References

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

5 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

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

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

Khoo et al (2017) The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One PMID: 28296947


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