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Asimadoline hydrochloride
🥰Excellent
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
🥰Excellent
Purity: 98.94%
Catalog No. T4691Alias EMD-61753 hydrochlorideCas No. 185951-07-9
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $30 | In Stock | |
| 5 mg | $67 | In Stock | |
| 10 mg | $113 | In Stock | |
| 25 mg | $239 | In Stock | |
| 50 mg | $355 | In Stock | |
| 100 mg | $526 | In Stock | |
| 500 mg | $1,130 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $74 | In Stock |
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Purity:98.94%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | EMD-61753 hydrochloride |
| 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. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (133.03 mM), Heating is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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