规格

价格

库存

数量

1 mg

¥ 329

现货

5 mg

¥ 723

现货

10 mg

¥ 1,160

现货

25 mg

¥ 2,320

现货

50 mg

¥ 3,450

现货

100 mg

¥ 4,890

现货

200 mg

¥ 6,780

现货

1 mL x 10 mM (in DMSO)

¥ 743

现货

生物活性

产品描述	Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.
靶点活性	κ opioid (Guinea pig):5.6 nM (EC50), κ opioid (human recombinant):1.2 nM (EC50)
体外活性	Asimadoline对μ-阿片受体的IC50为3μM，对δ-阿片受体的IC50为0.7μM。高浓度下，Asimadoline对大鼠十二指肠中400μM氯化钡显示出痉挛解除作用（IC50：4.2μM），表明Asimadoline可能通过尚未确定的机制阻断氯化钡对平滑肌的直接刺激效应[1]。
体内活性	Asimadoline的代谢在动物和人类中快速且相似。口服后的吸收率在大鼠中为80%，在狗和猴子中超过90%。Asimadoline具有部分通过增加关节液中substance P水平[1]来介导的周围抗炎作用。使用Asimadoline (5 mg/kg/day i.p.)治疗，在所有三个时间方案下都能显著（且持续）减轻疾病[2]。
动物实验	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].
别名	阿西马朵林盐酸盐, EMD-61753 hydrochloride

化学信息

分子量	451.01
分子式	C₂₇H₃₁ClN₂O₂
CAS No.	185951-07-9
Smiles	C(C(N([C@H](CN1CC[C@H](O)C1)C2=CC=CC=C2)C)=O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 60 mg/mL (133.03 mM), Heating is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.09 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2172 mL	11.0862 mL	22.1725 mL	110.8623 mL
5 mM	0.4434 mL	2.2172 mL	4.4345 mL	22.1725 mL
10 mM	0.2217 mL	1.1086 mL	2.2172 mL	11.0862 mL
20 mM	0.1109 mL	0.5543 mL	1.1086 mL	5.5431 mL
50 mM	0.0443 mL	0.2217 mL	0.4434 mL	2.2172 mL
100 mM	0.0222 mL	0.1109 mL	0.2217 mL	1.1086 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Asimadoline hydrochloride

Asimadoline hydrochloride

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词

Asimadoline hydrochloride

Asimadoline hydrochloride