TCS 1102

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TCS 1102 是一种有效的双重食欲素受体拮抗剂（Ki：对于 OX2/1 受体为 0.2/3 nM）。

TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). TCS 1102 inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo and blocks orexin-A (Cat.No.1455) mediated increases in feeding behaviour.

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.

TCS 1102 (compound 18) (15, 50, 100 mg/kg; i.p; single dose) induces locomotion inhibition in rat in a dose dependent manner.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.PK of TCS 1102 in Rat (100 mg/kg; i.p.; measured at 30 min).Animal Model:Male Sprague–Dawley rats (130-160 g) Dosage:10 and 20 mg/kg Administration:Intraperitoneal injection; 30 min before received the footshocks Result:Decreased fear and anxiety in rats 14 days after exposure to footshock.

TCS 1102, TCS1102, TCS-1102

Angiogenesis

CDK

OX1| OX2

Neurological Disease

——

916141-36-1

470.59

C27H26N4O2S

>98% (HPLC)

DMSO : ≥ 100 mg/mL; 212.50 mM

Cn1c2ccccc2nc1SCC(=O)N1CCC[C@H]1C(=O)Nc1ccccc1c1ccccc1

(2S)-1-[2-(1-methylbenzimidazol-2-yl)sulfanylacetyl]-N-(2-phenylphenyl)pyrrolidine-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years