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TCS1102
Axon 2744
CAS:
916141-36-1
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C27H26N4O2S
- MW: 470.59
Description
TCS1102 is a potent and selective dual orexin receptor antagonist (Ki values of 3 and 0.2 nM for hOX1R and hOX2R, respectively). Moreover, TCS1102 demonstrated in vivo central activity when dosed peripherally in a pharmacodynamic model of orexin activity.
More Information
| Parent CAS No. | 916141-36-1 |
|---|---|
| Chemical Name | (S)-N-(Biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide |
| SMILES | C1(NC(=O)[C@@H]2CCCN2C(CSC2=NC3C=CC=CC=3N2C)=O)C(C2C=CC=CC=2)=CC=CC=1 |&1:4,r| |
| MFCD | N.A. |
| 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 |
| InChiKey | YSBGRVXJEMSEQY-DEOSSOPVSA-N |
| CID | 11960895 |
| Short Description | OX1/2 antagonist |
References
- JM Bergman et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30.
- CJ Winrow et al. Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure. Neuropharmacology. 2010 Jan;58(1):185-94.
- SY Khoo et al. The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One. 2017 Mar 15;12(3):e0173967.
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