Asimadoline hydrochloride 阿西马朵林盐酸盐; EMD-61753 hydrochloride|cas:185951-07-9|西域试剂

Asimadoline hydrochloride 阿西马朵林盐酸盐; EMD-61753 hydrochloride,99.80%

产品编号：Bellancom-107384A| CAS NO：185951-07-9| 分子式：C₂₇H₃₁ClN₂O₂| 分子量：451.00

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货号	价格	库存与货期
Bellancom-107384A	￥950.00	杭州北京（现货）
Bellancom-107384A	￥1750.00	杭州北京（现货）
Bellancom-107384A	￥3950.00	杭州北京（现货）

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Asimadoline hydrochloride 阿西马朵林盐酸盐; EMD-61753 hydrochloride

产品介绍

Asimadoline (EMD-61753) hydrochloride 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 hydrochloride 对血脑屏障的渗透性低，具有外周抗炎作用。Asimadoline hydrochloride 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。

生物活性

Asimadoline (EMD-61753) hydrochloride 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 hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).

体外研究

Asimadoline (EMD-61753) hydrochloride has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC₅₀ for Asimadoline hydrochloride 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 hydrochloride has affinity to sodium and L type Ca²⁺ ion channels at IC₅₀ concentrations 150 to 800 fold the IC₅₀ for the κ receptors.
At high concentrations, Asimadoline hydrochloride demonstrates spasmolytic action against 400 µM barium chloride in the rat duodenum (IC₅₀=4.2 µM), suggesting that Asimadoline hydrochloride may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Asimadoline (EMD-61753 hydrochloride; 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 hydrochloride is rapid and appears similar in animals and man. Asimadoline hydrochloride has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels.
Treatment with Asimadoline hydrochloride (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 240 mg/mL (532.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2173 mL	11.0865 mL	22.1729 mL
5 mM	0.4435 mL	2.2173 mL	4.4346 mL
10 mM	0.2217 mL	1.1086 mL	2.2173 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 (sealed storage, away from moisture)。-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: ≥ 6 mg/mL (13.30 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (13.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 60.0 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6 mg/mL (13.30 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (13.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 60.0 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6 mg/mL (13.30 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (13.30 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 60.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。