Asimadoline - CAS:153205-46-0

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Asimadoline (Synonyms:阿西马朵林; EMD-61753)

目录号 : KM2747 CAS No. : 153205-46-0

Data Sheet 产品使用指南

Asimadoline (EMD-61753) 是一种口服有效的，选择性的，具有周边活性的 κ-opioid 激动剂，对豚鼠和人重组 κ-opioid 的 IC₅₀s 分别为 5.6 nM 和 1.2 nM。Asimadoline 对血脑屏障的渗透性低，具有外周抗炎作用。Asimadoline 可改善糖尿病大鼠的异常性疼痛，并具有用于肠易激综合征 (IBS) 研究的潜力。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC₅₀s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).

体外研究

Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC₅₀ for Asimadoline binding to μ-opioid receptors is 3 µM and to δ-opioid receptors is 0.7 µM. The IC₅₀ values for D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA and kainate/AMPA receptors are all >10 µM.
Asimadoline has affinity to sodium and L type Ca ion channels at IC₅₀ concentrations 150 to 800 fold the IC₅₀ for the κ receptors.
At high concentrations, Asimadoline demonstrates spasmolytic action against 400 µM barium chloride in the rat duodenum (IC₅₀=4.2 µM), suggesting that Asimadoline may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.

体内研究

Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.
The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels.
Treatment with Asimadoline (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes.

Animal Model:	Adult female Sprague-Dawley rats
Dosage:	1, 5, 15 mg/kg
Administration:	SC; single dose
Result:	Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.

分子式

C₂₇H₃₀N₂O₂

分子量

414.54

CAS号

153205-46-0

中文名称

阿西马朵林；阿西马多林

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 : ≥ 100 mg/mL (241.23 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4123 mL	12.0616 mL	24.1231 mL
5 mM	0.4825 mL	2.4123 mL	4.8246 mL
10 mM	0.2412 mL	1.2062 mL	2.4123 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 (6.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.03 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.03 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.03 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。