| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
guinea pig κ opioid ( IC50 = 5.6 nM ); human recombinant κ opioid ( IC50 = 1.2 nM )
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|---|---|
| ln Vitro |
Asimadoline (EMD-61753) has high selectivity at 1:501:498 opioid binding ratios for κ: μ: δ in human recombinant receptors. At 3 µM for μ-opioid receptors and 0.7 µM for μ-opioid receptors, asimadoline's binding IC50 values are determined. All of the receptors: D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA, and kainate/AMPA have IC50 values greater than 10 µM[1].
Asimadoline exhibits affinity for sodium and L type Ca2+ ion channels, with IC50 values ranging from 150 to 800 times higher than that of κ receptors[1]. Asimadoline exhibits spasmolytic action against 400 µM barium chloride in the rat duodenum at high concentrations (IC50=4.2 µM), indicating that Asimadoline may mitigate the direct stimulant effects of barium on smooth muscle via unidentified mechanisms[1]. |
| ln Vivo |
Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s.c.) acutely reduces tactile allodynia and formalin-evoked hyperalgesia in diabetic rats[3].
In rats, the rate of absorption after oral administration is 80%, whereas in dogs and monkeys, it exceeds 90%. Asimadoline's metabolism is quick and seems to be similar in both humans and animals. Increases in joint fluid substance P levels are one way that asimadoline's peripheral anti-inflammatory effects are partially mediated[1]. Asimadoline (5 mg/kg/day; intraperitoneal) treatment results in a significant (and long-lasting) reduction in the illness with all three time regimens[2]. |
| Animal Protocol |
Adult female Sprague-Dawley rats
1, 5, 15 mg/kg SC; single dose |
| References |
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| Molecular Formula |
C27H30N2O2
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|---|---|
| Molecular Weight |
414.5393
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| Exact Mass |
414.23
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| Elemental Analysis |
C, 78.23; H, 7.29; N, 6.76; O, 7.72
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| CAS # |
153205-46-0
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| Related CAS # |
Asimadoline hydrochloride; 185951-07-9
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| Appearance |
A crystalline solid
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| SMILES |
CN([C@H](CN1CC[C@@H](C1)O)C2=CC=CC=C2)C(=O)C(C3=CC=CC=C3)C4=CC=CC=C4
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| InChi Key |
JHLHNYVMZCADTC-LOSJGSFVSA-N
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| InChi Code |
InChI=1S/C27H30N2O2/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,17-20H2,1H3/t24-,25+/m0/s1
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| Chemical Name |
N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide
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| Synonyms |
EMD 61753; Asimadoline
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4123 mL | 12.0616 mL | 24.1231 mL | |
| 5 mM | 0.4825 mL | 2.4123 mL | 4.8246 mL | |
| 10 mM | 0.2412 mL | 1.2062 mL | 2.4123 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01380561 | Completed | Drug: asimadoline | Healthy | Tioga Pharmaceuticals | June 2011 | Phase 1 |
| NCT00454688 | Completed | Drug: Asimadoline Drug: Placebo |
Irritable Bowel Syndrome | Tioga Pharmaceuticals | August 2006 | Phase 2 |
| NCT02475447 | Completed | Drug: Asimadoline Drug: Placebo |
Atopic Dermatitis Pruritus |
Tioga Pharmaceuticals | July 2015 | Phase 2 |
| NCT00955994 | Completed | Drug: asimadoline | Irritable Bowel Syndrome | Mayo Clinic | January 2005 | Phase 2 |
| NCT01100684 | Completed | Drug: Asimadoline Drug: Placebo |
Diarrhea Predominant Irritable Bowel Syndrome |
Tioga Pharmaceuticals | May 2010 | Phase 3 |
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