TCS 1102_product_DataBase

Bioactivity

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 brain peneration and moderate bioavailability in rats[1].

Invitro

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].

In Vivo

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)

Name

TCS 1102

CAS

916141-36-1

Formula

C27H26N4O2S

Molar Mass

470.59

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

TCS 1102

CAS: 916141-36-1 F: C27H26N4O2S W: 470.59