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Asimadoline hydrochloride

Asimadoline hydrochloride
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Purity:98.94%
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Asimadoline hydrochloride

Catalog No. T4691Cas 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.
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Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$67In Stock
10 mg$113In Stock
25 mg$239In Stock
50 mg$355In Stock
100 mg$526In Stock
500 mg$1,130In Stock
1 mL x 10 mM (in DMSO)$74In Stock
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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].
AliasEMD-61753 hydrochloride
Chemical Properties
Molecular Weight451.01
FormulaC27H31ClN2O2
Cas No.185951-07-9
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2172 mL11.0862 mL22.1725 mL110.8623 mL
5 mM0.4434 mL2.2172 mL4.4345 mL22.1725 mL
10 mM0.2217 mL1.1086 mL2.2172 mL11.0862 mL
20 mM0.1109 mL0.5543 mL1.1086 mL5.5431 mL
50 mM0.0443 mL0.2217 mL0.4434 mL2.2172 mL
100 mM0.0222 mL0.1109 mL0.2217 mL1.1086 mL

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