TCS 1102

Pricing Availability Delivery Time Qty
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 (3)
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
DMSO 47.06 100
ethanol 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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:

Khoo et al (2017) The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One 12 PMID: 28296947


If you know of a relevant reference for TCS 1102, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Non-selective Orexin Antagonists

Keywords: TCS1102 orexin receptors OX1 OX2 antagonists non-selective dual potent merck Non-selective Orexin

3 Citations for TCS 1102

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

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

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


Do you know of a great paper that uses TCS 1102 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Peptide Hormone Receptors

Peptide Hormone Receptors Product Listing

A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:

  • Anterior Pituitary Regulation
  • Blood Pressure Regulation
  • Feeding and Appetite Regulation
  • Glucose Regulation
  • Peptide Hormone Processing
Peptides Involved in Appetite Modulation

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.

Pathways for TCS 1102

Protocols

TODO: Add Protocols