Asimadoline (EMD-61753)

目录号: GC31762纯度: >98%同义词: 阿西马朵林; EMD-61753

A potent κ-opioid receptor agonist

Cas No.: 153205-46-0

规格	价格	库存	数量
5mg	¥848.00	现货	1
10mg	¥1,562.00	现货	1
25mg	¥3,526.00	现货	1
10mM (in 1mL DMSO)	¥932.00	现货	1

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Nature
641, 529–536 (2025)
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628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC₅₀s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively).¹ It is 501- and 498-fold selective for κ-opioid over μ- and δ-opioid receptors, respectively. Asimadoline is spasmolytic in isolated rat duodenum (IC₅₀ = 4.2 μM) and inhibits spontaneous contractions of isolated rat uterus (IC₅₀ = 12.7 μM). In vivo, asimadoline reduces joint damage in a rat model of arthritis induced by complete Freund's adjuvant (CFA). Asimadoline (25 mg/kg) also reduces the abdominal withdrawal reflex in a model of visceral pain induced by colonic distension in wild-type, but not KOR^-/-, mice.²

1.Camilleri, M.Asimadoline, a κ-opioid agonist, and visceral sensationNeurogastroenterol. Motil.20(9)971-979(2008) 2.Larsson, M.H., Bayati, A., Lindstr?m, E., et al.Involvement of kappa-opioid receptors in visceral nociception in miceNeurogastroenterol. Motil.20(10)1157-1164(2008)

实验参考方法 Experimental Reference Method

Animal experiment:

Rats: Asimadoline (5 mg/kg/day, n=10 per group) or vehicle (2 mL/kg/day, n=10) is administered to DA rats by i.p. injection twice daily (i) during the primary inflammatory phase (days 1–3); (ii) once the disease is established (days 13–21); or (iii) throughout the entire time course (days 1-21). Non-arthritic control animals receive Asimadoline (5 mg/kg/day, n=5) or vehicle (2 mL/kg/day, n=5) by i.p. injection twice daily. In all cases, disease parameters are assessed. In this experiment, the SP content of joint tissue is assessed only after the rats are killed (day 21)[2].

References:

[1]. Camilleri M, et al. Asimadoline, a κ-Opioid Agonist, and Visceral Sensation. Neurogastroenterol Motil. 2008 Sep; 20(9): 971–979.
[2]. Binder W, et al. Involvement of substance P in the anti-inflammatory effects of the peripherally selective kappa-opioid asimadoline and the NK1 antagonist GR205171. Eur J Neurosci. 1999 Jun;11(6):2065-72.

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

153205-46-0

同义词

阿西马朵林; EMD-61753

SMILES

O[C@H]1CCN(C1)C[C@H](C2=CC=CC=C2)N(C)C(C(C3=CC=CC=C3)C4=CC=CC=C4)=O

分子式

C₂₇H₃₀N₂O₂

分子量

414.54 g/mol

溶解性

DMSO : ≥ 103.3 mg/mL (249.19 mM)

保存条件

Store at -20°C

General tips

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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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