中文名称: Ro 64-6198
英文名称: Ro 64-6198
CAS No: 280783-56-4
分子式: C26H31N3O
分子量: 401.54
R10513 Ro 64-6198 ≥98% (psaitong)
包装规格:
1mg 5mg in glass bottle
溶解性:
溶于DMSO(2mg/mL)
产品描述:

基本信息

产品编号:

R10513

产品名称:

Ro 64-6198

CAS:

280783-56-4

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C26H31N3O

溶于液体

-80℃

6个月

分子量:

401.54

-20℃

1个月

化学名: 

8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-Triazaspiro[4.5]decan-4-one,(1S,3aS)-8-(2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

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。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.4904mL

12.4521mL

24.9041mL

5mM

0.4981mL

2.4904mL

4.9808mL

10mM

0.2490mL

1.2452mL

2.4904mL

 

生物活性

产品描述

一种有效的,选择性的,非肽,高亲和力,高细胞通透性和脑渗透 N/OFQ 受体 (NOP) 激动剂,EC50 值为 25.6nM。Ro 64-6198 对 NOP 受体的选择性至少是经典阿片受体的 100倍。Ro 64-6198 可用于压力和焦虑,成瘾,神经性疼痛,咳嗽和厌食症的研究。

靶点

Nociceptin receptor

 

体外研究

Ro 64-6198 also produces rapid desensitization of the NOP receptor.In vitro studies shows that treatment with Ro 64-6198 results in a functional desensitization of the receptor, a loss in binding sites,and an apparent decrease in binding affinity.The desensitization produced by Ro 64-6198 is not reversed by acidic washes.Ro 64-6198 does recruit both arrestin3 (EC50 of 0.912µM) and arrestin2 (EC50 of 1.20µM) to the NOP receptor in a concentration-dependent manner comparably with N/OFQ.

体内研究

At low doses Ro 64-6198 is anxiolytic in several neophobic tests,including the marble burying test in mice,the elevated plus maze in rats and the open field test in rats.In the marble burying test, at 1mg/kg,i.p.,Ro 64-6198 produces a decrease in the number of marbles buried,without altering locomotor activity,indicating a decrease in neophobia and anxiety.Ro 64-6198 selectively increases the number of open arm transitions and time spent in the open arms of the elevated plus maze at doses of 0.32-3mg/kg,i.p.,without affecting closed arm transitions or locomotor activity in the closed arms.In the open field test,Ro 64-6198, at doses of 0.32-3mg/kg,attenuates the inhibition of exploration that results from the stress of a novel environment.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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