产品
编 号：F519186
分子式：C27H26N4O2S
分子量：470.59
分子式：C27H26N4O2S
分子量：470.59
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
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询价
结构图
CAS No: 916141-36-1
产品详情
生物活性：
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.
体内研究：
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)CL (mL/min/kg)T1/2 (h)F (%)Brain/plasma/CSF (nM)
3.70.3112370/3500/43
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.
体外研究：
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 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.
体内研究：
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)CL (mL/min/kg)T1/2 (h)F (%)Brain/plasma/CSF (nM)
3.70.3112370/3500/43
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.
体外研究：
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.
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