Ro 64-6198 - CAS:280783-56-4

您当前的位置：

Ro 64-6198

目录号 : KM3809 CAS No. : 280783-56-4

Data Sheet 产品使用指南

Ro 64-6198 是一种有效的，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 25.6 nM。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。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

Ginkgolide J In-stock
Ginkgolide K In-stock
THK-5470 In-stock
NH-3 In-stock
Velufenacin In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC₅₀ value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.

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 0.912 µM) and arrestin2 (EC₅₀ of 1.20 µM) 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 1 mg/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 0.32-3 mg/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 0.32-3 mg/kg, attenuates the inhibition of exploration that results from the stress of a novel environment.

分子式

C₂₆H₃₁N₃O

分子量

401.54

CAS号

280783-56-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (124.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4904 mL	12.4521 mL	24.9041 mL
5 mM	0.4981 mL	2.4904 mL	4.9808 mL
10 mM	0.2490 mL	1.2452 mL	2.4904 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.23 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。