For research use only. Not for therapeutic Use.
TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats[1].
TCS 1102 (10 μM) inhibits Ca2+ responses to Orexin A (human, rat, mouse) (HY-106224) and Yan 7874 (an Orexin receptor agonist) in CHO-hOX2 cells[2].
TCS 1102 (compound 18) (15, 50, 100 mg/kg; i.p; single dose) induces locomotion inhibition in rat in a dose dependent manner[1].
TCS-1102 (10 and 20 mg/kg; i.p.; single dose) decreases fear and anxiety in rats after exposure to footshock. Furthermore, TCS-1102 (10 mg/kg; i.p.; single dose) also shows anxiolytic effects for high responders (HR) rat when tested in the elevated T-maze[3].
PK of TCS 1102 in Rat (100 mg/kg; i.p.; measured at 30 min)[1]
CL (mL/min/kg)
T1/2 (h)
F (%)
Brain/plasma/CSF (nM)
3.7
0.3
11
2370/3500/43
| Catalog Number | I005463 |
| CAS Number | 916141-36-1 |
| Synonyms | (2S)-1-[2-(1-methylbenzimidazol-2-yl)sulfanylacetyl]-N-(2-phenylphenyl)pyrrolidine-2-carboxamide |
| Molecular Formula | C27H26N4O2S |
| Purity | ≥95% |
| 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 |
| SMILES | CN1C2=CC=CC=C2N=C1SCC(=O)N3CCCC3C(=O)NC4=CC=CC=C4C5=CC=CC=C5 |
| Reference | [1]. Bergman JM, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. [2]. Turku A, et al. Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity. PLoS One. 2017 Jun 2;12(6):e0178526. [3]. Chen X, et al. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks. Brain Struct Funct. 2013 Aug 18. |
