Asimadoline

SKU: orb1222652

Description

Asimadoline is a proprietary small molecule therapeutic, originally discovered by Merck KGaA of Darmstadt, Germany. Asimadoline was originally developed to treat peripheral pain such as arthritis. Asimadoline is an orally administered agent that acts as a kappa opioid receptor agonist. It has shown encouraging clinical efficacy for the treatment of IBS in a barostat study in IBS patients and has the potential for treating other gastrointestinal diseases.

Images & Validation

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Key Properties

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CAS Number	153205-46-0
MW	414.54
Purity	>98% (HPLC)
Formula	C₂₇H₃₀N₂O₂
SMILES	CN([C@H](CN1CC[C@@H](C1)O)C2=CC=CC=C2)C(=O)C(C3=CC=CC=C3)C4=CC=CC=C4
Target	DNA/RNA Synthesis
Solubility	DMSO : ≥ 103.3 mg/mL; 249.19 mM

Bioactivity

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In Vivo

Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s. c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats. The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels. Treatment with Asimadoline (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes. Animal model: Adult female Sprague-Dawley rats. Dosage: 1, 5, 15 mg/kg. Administration: SC; single dose. Result: Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.

In Vitro

Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1: 501: 498 in human recombinant receptors. The IC50 for Asimadoline binding to μ-opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. The IC50 values for D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA and kainate/AMPA receptors are all >10 μM. Asimadoline has affinity to sodium and L type Ca2+ ion channels at IC50 concentrations 150 to 800 fold the IC50 for the κ receptors. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Asimadoline

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Asimadoline (orb1222652)

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Purity:	99.32% (May vary between batches)
CAS Number:	185951-07-9
MW:	451.01
Formula:	C₂₇H₃₁ClN₂O₂

Asimadoline

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Asimadoline (orb1222652)

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