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148687-76-7

中文名称 3-([3,5-BIS(TRIFLUOROMETHYL)PHENYL]METHOXY)-2-PHENYL-PIPERIDINE HYDROCHLORIDE
英文名称 3-([3,5-BIS(TRIFLUOROMETHYL)PHENYL]METHOXY)-2-PHENYL-PIPERIDINE HYDROCHLORIDE
CAS 148687-76-7
分子式 C20H20ClF6NO
分子量 439.82
MOL 文件 148687-76-7.mol
148687-76-7 结构式 148687-76-7 结构式

基本信息

中文别名
化合物 T22902
英文别名
L-733,061 HYDROCHLORIDE
L-733,060 HYDROCHLORIDE
3-([3,5-BIS(TRIFLUOROMETHYL)PHENYL]METHOXY)-2-PHENYL-PIPERIDINE HYDROCHLORIDE

物理化学性质

储存条件2-8°C
储存条件2-8°C
溶解度DMSO: >10 mg/mL
溶解度二甲基亚砜:>10 mg/mL
形态solid
颜色white
水溶解性Soluble to 50 mM in water with gentle warming

安全数据

安全说明22-24/25
WGK Germany3
WGK Germany3
3-([3,5-BIS(TRIFLUOROMETHYL)PHENYL]METHOXY)-2-PHENYL-PIPERIDINE HYDROCHLORIDE价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/08/19HY-14406A3-([3,5-BIS(TRIFLUOROMETHYL)PHENYL]METHOXY)-2-PHENYL-PIPERIDINE HYDROCHLORIDE
L-733060 hydrochloride
148687-76-71 mg2600元

常见问题列表

生物活性
L-733060 hydrochloride 是一种有效的速激肽 NK1 受体拮抗剂。 L-733060 hydrochloride 以不会在啮齿动物中引起不良心血管影响的剂量抑制神经源性血浆外渗,同时还充当抗肿瘤剂。
靶点

NK1

体外研究

L-733060 (30-300 nM) inhibits the [Ca 2+ ] i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK 1 receptor-transfected CHO cells.
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells.
L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC 50 s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively.
L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC 50 s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively.

Cell Proliferation Assay

Cell Line: COLO 858 cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 0, 48, 96 h
Result: Inhibited cells growth with IC 50 s of 8.7 μM and 7.1 μM at 48 h and 96 h, respectively.
体内研究

L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats.
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg/kg in conscious or anaesthetised rats.

Animal Model: Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion
Dosage: 10, 100, 1000 mg/kg
Administration: I.v. injection
Result: Produced a significant dose-related inhibition of plasma extravasation with an ID 50 of 212±19 μg/kg.
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