| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Asimadoline HCl (EMD-61753), the hydrochloride salt of Asimadoline, is an orally bioactive, selective and peripherally active κ-opioid agonist with the potential for the treatment of pruritus and irritable bowel syndrome/IBS. It activates κ-opioid receptor with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant).
| ln Vitro |
In human recombinant receptors, asimadoline (EMD-61753) hydrochloride exhibits a high degree of selectivity in the κ: μ: δ opioid binding ratios of 1:501:498. Asimadoline hydrochloride has an IC50 of 3 µM for μ-opioid receptors and 0.7 µM for μ-opioid receptors. The IC50 values for the following receptors: D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA, and kainate/AMPA[1]. Asimadoline hydrochloride has affinity for both L type and sodium Ca2+ ion channels, with IC50 values ranging from 150 to 800 times higher than that of κ receptors[1]. In the rat duodenum, aspirin hydrochloride exhibits spasmolytic action at high concentrations (IC50=4.2 µM) against 400 µM barium chloride. This finding raises the possibility that aspirin hydrochloride inhibits the direct stimulant effects of barium on smooth muscle via as yet unidentified mechanisms[1].
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| ln Vivo |
In diabetic rats, asimadoline (EMD-61753 hydrochloride; 1, 5, 15 mg/kg; sc) immediately reduces tactile allodynia and formalin-evoked hyperalgesia[3]. After oral dosing, the rate of absorption is 80% in rats and >90% in dogs and monkeys. Asimadoline hydrochloride has a quick metabolism that is comparable in both humans and animals. Peripheral anti-inflammatory effects of asimadoline hydrochloride are partially mediated by elevated levels of joint fluid substance P[1]. With all three time regimens, treatment with asimadoline hydrochloride (5 mg/kg/day; ip) results in a significant (and long-lasting) attenuation of the disease[2].
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| Animal Protocol |
Animal/Disease Models: Adult female SD (Sprague-Dawley) rats[3]
Doses: 1, 5, 15 mg/kg Route of Administration: SC; single dose Experimental Results: Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats. |
| References |
[1]. Camilleri M, et al. Asimadoline, a κ-Opioid Agonist, and Visceral Sensation. Neurogastroenterol Motil. 2008 Sep; 20(9): 971–979.
[2]. Binder W, et al. Involvement of substance P in the anti-inflammatory effects of the peripherally selective kappa-opioid asimadoline and the NK1 antagonist GR205171. Eur J Neurosci. 1999 Jun;11(6):2065-72. [3]. C G Jolivalt, et al. Dynorphin A, kappa opioid receptors and the antinociceptive efficacy of asimadoline in streptozotocin-induced diabetic rats. Diabetologia. 2006 Nov;49(11):2775-85. |
| Molecular Formula |
C27H31CLN2O2
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|---|---|
| Molecular Weight |
451.01
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| CAS # |
185951-07-9
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| Related CAS # |
Asimadoline;153205-46-0
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(N([C@@H](C1=CC=CC=C1)CN2C[C@@H](O)CC2)C)C(C3=CC=CC=C3)C4=CC=CC=C4.[H]Cl
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| InChi Key |
GMJSLABTEURMBF-CLSOAGJSSA-N
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| InChi Code |
InChI=1S/C27H30N2O2.ClH/c1-28(25(21-11-5-2-6-12-21)20-29-18-17-24(30)19-29)27(31)26(22-13-7-3-8-14-22)23-15-9-4-10-16-23/h2-16,24-26,30H,17-20H2,1H31H/t24-,25+/m0./s1
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| Chemical Name |
N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-a-phenyl-benzeneacetamide hydrochloride
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| Synonyms |
EMD-61753 ONO3951 EMD 61753EMR 63320 ONO 3951 EMR-63320 ONO-3951 EMD61753 EMR63320
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~240 mg/mL (~532.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6 mg/mL (13.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 60.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6 mg/mL (13.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 60.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 6 mg/mL (13.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2172 mL | 11.0862 mL | 22.1725 mL | |
| 5 mM | 0.4434 mL | 2.2172 mL | 4.4345 mL | |
| 10 mM | 0.2217 mL | 1.1086 mL | 2.2172 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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