产品
编 号：F517193
分子式：C29H32ClF3N2O3
分子量：549.02
分子式：C29H32ClF3N2O3
分子量：549.02
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 913358-93-7
产品详情
生物活性：
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
体内研究：
Almorexant hydrochloride (1.8 μMol/kg，100 μL；IP，每日) 减少肿瘤体积。 Almorexant hydrochloride (300 mg/kg，PO，一次) 可以帮助大鼠完全能够进行空间和回避学习。 Almorexant hydrochloride (30-300 mg/kg) 剂量依赖性地增加快速眼动 (REM) 和非 REM (NREM)) 睡眠并明显减少觉醒，而不会引起猝倒或第二天表现缺陷。Animal Model:Mice xenografted with AsPC-1 cells
Dosage:1.8 μmol/kg, 100 μL
Administration:IP, daily, starting at day 0 or day 38
Result:Resulted in a significant decrease in tumor volume when treatment starting at day 0. Started after AsPC-1 tumors were developed (day 38), rapidly and strongly reduced the volume of established tumors.
Animal Model:Long-Evans rats (24, male, 16-18 weeks of age)
Dosage:300 mg/kg
Administration:PO, once
Result:Successfully learned the spatial task, established spatial memory.
Animal Model:Male C57BL/6 mice (Orexin/ataxin-3 transgenic (TG) mice and WT mice, 32 ± 0.9 g, age 15 ± 0.5 week)
Dosage:30, 100, 300 mg/kg (3, 10, and 30 mg/mL; 10 mL/kg)
Administration:IP, once every 3 days
Result:Exacerbated cataplexy in TG mice and increased nonrapid eye movement (NREM) sleep with heightened sleep/wake fragmentation in both genotypes during the 12-h dark period after dosing. Showed greater hypnotic potency in WT mice than in TG mice.
体外研究：
Almorexant hydrochloride (1 μM) 促进 SHP2/OX1R 复合物的酪氨酸磷酸化。 Almorexant hydrochloride (1 μM) 抑制 AsPC-1 细胞的生长。
Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
体内研究：
Almorexant hydrochloride (1.8 μMol/kg，100 μL；IP，每日) 减少肿瘤体积。 Almorexant hydrochloride (300 mg/kg，PO，一次) 可以帮助大鼠完全能够进行空间和回避学习。 Almorexant hydrochloride (30-300 mg/kg) 剂量依赖性地增加快速眼动 (REM) 和非 REM (NREM)) 睡眠并明显减少觉醒，而不会引起猝倒或第二天表现缺陷。Animal Model:Mice xenografted with AsPC-1 cells
Dosage:1.8 μmol/kg, 100 μL
Administration:IP, daily, starting at day 0 or day 38
Result:Resulted in a significant decrease in tumor volume when treatment starting at day 0. Started after AsPC-1 tumors were developed (day 38), rapidly and strongly reduced the volume of established tumors.
Animal Model:Long-Evans rats (24, male, 16-18 weeks of age)
Dosage:300 mg/kg
Administration:PO, once
Result:Successfully learned the spatial task, established spatial memory.
Animal Model:Male C57BL/6 mice (Orexin/ataxin-3 transgenic (TG) mice and WT mice, 32 ± 0.9 g, age 15 ± 0.5 week)
Dosage:30, 100, 300 mg/kg (3, 10, and 30 mg/mL; 10 mL/kg)
Administration:IP, once every 3 days
Result:Exacerbated cataplexy in TG mice and increased nonrapid eye movement (NREM) sleep with heightened sleep/wake fragmentation in both genotypes during the 12-h dark period after dosing. Showed greater hypnotic potency in WT mice than in TG mice.
体外研究：
Almorexant hydrochloride (1 μM) 促进 SHP2/OX1R 复合物的酪氨酸磷酸化。 Almorexant hydrochloride (1 μM) 抑制 AsPC-1 细胞的生长。
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