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Asimadoline hydrochloride

Name: Asimadoline hydrochloride
Brand: TargetMol
SKU: T4691
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4691Cas No. 185951-07-9

Alias EMD-61753 hydrochloride

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.

Asimadoline hydrochloride

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Purity: 99.32%

Catalog No. T4691Alias EMD-61753 hydrochlorideCas No. 185951-07-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$67	In Stock	In Stock
10 mg	$113	In Stock	In Stock
25 mg	$239	In Stock	In Stock
50 mg	$355	In Stock	In Stock
100 mg	$526	In Stock	In Stock
500 mg	$1,130	-	In Stock
1 mL x 10 mM (in DMSO)	$74	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.32%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	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.
Targets&IC50	κ opioid (Guinea pig):5.6 nM (EC50), κ opioid (human recombinant):1.2 nM (EC50)
In vitro	The IC50 for Asimadoline binding to μ-opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. 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[1].
In vivo	The metabolism of Asimadoline is rapid and appears similar in animals and man. The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through an increase in joint fluid substance P levels[1]. Treatment with Asimadoline (5 mg/kg/day i.p.) produces marked (and sustained) attenuation of the disease with all three-time regimes[2].
Animal Research	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].
Synonyms	EMD-61753 hydrochloride

Chemical Properties

Molecular Weight	451.01
Formula	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
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

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

In Vivo Formulation

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

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

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

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc