中文名称: | L-733060 hydrochloride | ||||
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英文名称: | L-733060 hydrochloride | ||||
别名: | (2R,3R)-3-[[3,5-bis(trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine;hydrochloride | ||||
CAS No: | 148687-76-7 | 分子式: | C20H20ClF6NO | 分子量: | 439.82 |
CAS No: | 148687-76-7 | ||||
分子式: | C20H20ClF6NO | ||||
分子量: | 439.82 |
基本信息
产品编号: |
L11034 |
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产品名称: |
L-733060 hydrochloride |
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CAS: |
148687-76-7 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
二年 |
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分子量: |
439.82 |
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化学名: |
(2R,3R)-3-[[3,5-bis(trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
生物活性
产品描述 |
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。 |
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靶点 |
NK1 |
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体外研究 |
L-733060 (30-300nM) inhibits the [Ca2+]i mobilisation caused by substance P (100nM) in a concentration-dependent manner in human tachykinin NK1 receptor-transfected CHO cells.L-733060 (2.5-20μM;48 and or 96h) results in a concentration-dependent cytotoxicity in COLO 858 cells.L-733060 (10-30μM;24 and 48h) inhibits MEL H0 cells proliferation with IC50s of 27.5μM and 18.9μM at 24h and 48h,respectively.L-733060 (20-50μM;and or 72h) inhibits COLO 679 cells growth with IC50s of 33.8μM and 31.5μM at 30 h and 72h,respectively. Cell Proliferation Assay |
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Cell Line: |
COLO 858 cells |
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Concentration: |
2.5,5,10,20μM |
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Incubation Time: |
0,48,96h |
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Result: |
Inhibited cells growth with IC50s of 8.7μM and 7.1μM at 48h and 96h,respectively. |
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体内研究 |
L-733060 (10-1000μg/kg;i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats.L-733060 (300-3000μg/kg;i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000μg/kg in conscious or anaesthetised rats. |
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Animal Model: |
Male Sprague-Dawley rats (200g) with electrical stimulation of the trigeminal ganglion |
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Dosage: |
10,100,1000mg/kg |
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Administration: |
I.v.injection |
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Result: |
Produced a significant dose-related inhibition of plasma extravasation with an ID50 of 212±19μg/kg. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )