TCS 1102 - ≥98%(HPLC), high purity , CAS No.916141-36-1, Antagonist of OX 1 receptor;Antagonist of OX 2 receptor

Item Number
T287352
Grouped product items
SKUSizeAvailabilityPrice Qty
T287352-10mg
10mg
In stock
$109.90
T287352-25mg
25mg
In stock
$247.90
T287352-50mg
50mg
In stock
$391.90
T287352-100mg
100mg
In stock
$705.90

Potent, dual orexin receptor antagonist

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent, dual orexin receptor antagonist (Kivalues are 0.2 and 3 nM for OX2and OX1receptors respectively). Inhibits ADL-orexin B-mediated locomotion following i.p. administrationin vivoand blocksorexin-A mediated increases in feeding behaviour. Brain penet
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of OX 1 receptor;Antagonist of OX 2 receptor
Product Description

Product Describtion:
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). IC50 value: 0.2 nM (Ki, OX2 receptor); 3 nM (Ki, OX1 receptor) ;Target: OX2 and OX1 receptor TCS-1102 (10 and 20 mg/kg, i.p.) were found to decrease fear and anxiety in rats 14 days after exposure to footshock.Furthermore, TCS-1102 (10 mg/kg, i.p.) was found to have anxiolytic effects that were specific for HR when tested in the elevated T-maze.

Associated Targets(Human)

HCRTR1 Tclin Orexin receptor type 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HCRTR2 Tclin Orexin receptor type 2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SLC18A2 Tclin Synaptic vesicular amine transporter (118 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCRTR1 Tclin Orexin receptor 1 (5435 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCRTR2 Tclin Orexin receptor 2 (5902 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Brain (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasma (328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cerebrospinal fluid (288 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (2S)-1-[2-(1-methylbenzimidazol-2-yl)sulfanylacetyl]-N-(2-phenylphenyl)pyrrolidine-2-carboxamide
INCHI InChI=1S/C27H26N4O2S/c1-30-23-15-8-7-14-22(23)29-27(30)34-18-25(32)31-17-9-16-24(31)26(33)28-21-13-6-5-12-20(21)19-10-3-2-4-11-19/h2-8,10-15,24H,9,16-18H2,1H3,(H,28,33)/t24-/m0/s1
InChi Key YSBGRVXJEMSEQY-DEOSSOPVSA-N
Canonical SMILES CN1C2=CC=CC=C2N=C1SCC(=O)N3CCCC3C(=O)NC4=CC=CC=C4C5=CC=CC=C5
Isomeric SMILES CN1C2=CC=CC=C2N=C1SCC(=O)N3CCC[C@H]3C(=O)NC4=CC=CC=C4C5=CC=CC=C5
PubChem CID 11960895
MeSH Entry Terms N-(1,1'-biphenyl)-2-yl-1-(2-((1-methyl-1H-benzimidazol-2-yl)thio)acetyl-2-pyrrolidinedicarboxamide;TCS 1102;TCS1102
Molecular Weight 470.59

Certificates

Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
A2205625Certificate of AnalysisOct 11, 2024 T287352
A2205627Certificate of AnalysisOct 11, 2024 T287352
A2205628Certificate of AnalysisOct 11, 2024 T287352
A2205629Certificate of AnalysisOct 11, 2024 T287352

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 47.06, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 47.06, Max Conc. mM: 100

Related Documents

References

1. Bergman JM, Roecker AJ, Mercer SP, Bednar RA, Reiss DR, Ransom RW, Meacham Harrell C, Pettibone DJ, Lemaire W, Murphy KL et al..  (2008)  Proline bis-amides as potent dual orexin receptor antagonists..  Bioorg Med Chem Lett,  18  (4): (1425-30).  [PMID:18207395] [10.1021/op500134e]

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