ASIMADOLINE
- CAS No.
- 153205-46-0
- Chemical Name:
- ASIMADOLINE
- Synonyms
- EMD 61753;ASIMADOLINE;Asimadoline (EMD-61753;EMD-61753;EMD61753;EMD 61753;N-((S)-2-((S)-3-Hydroxypyrrolidin-1-yl)-1-phenylethyl)-N-methyl-2,2-diphenylacetamide;Benzeneacetamide, N-[(1S)-2-[(3S)-3-hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-α-phenyl-;N-[(1S)-2-[(3S)-3-Hydroxy-1-pyrrolidinyl]-1-phenylethyl]-N-methyl-alpha-phenylbenzeneacetamide
- CBNumber:
- CB6228855
- Molecular Formula:
- C27H30N2O2
- Molecular Weight:
- 414.54
- MDL Number:
- MFCD00925628
- MOL File:
- 153205-46-0.mol
Boiling point | 605.8±55.0 °C(Predicted) |
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Density | 1.170±0.06 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMSO: 103 mg/ml |
form | A crystalline solid |
pka | 14.79±0.20(Predicted) |
color | White to off-white |
FDA UNII | D0VK52NV5M |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS09 |
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Signal word | Warning | |||||||||
Hazard statements | H410 | |||||||||
Precautionary statements | P501-P273-P391 | |||||||||
NFPA 704 |
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ASIMADOLINE price More Price(15)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 26411 | Asimadoline | 153205-46-0 | 5mg | $109 | 2024-03-01 | Buy |
Cayman Chemical | 26411 | Asimadoline | 153205-46-0 | 25mg | $420 | 2024-03-01 | Buy |
Cayman Chemical | 26411 | Asimadoline | 153205-46-0 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 26411 | Asimadoline | 153205-46-0 | 10mg | $199 | 2024-03-01 | Buy |
ChemScene | CS-8053 | Asimadoline 99.36% | 153205-46-0 | 10mg | $156 | 2021-12-16 | Buy |
ASIMADOLINE Chemical Properties,Uses,Production
Uses
Acimadolin is a K-opioid agonist that raises the sensitivity threshold in patients with irritable bowel syndrome (IBS), barely crosses the blood-brain barrier, and is well tolerated. It cannot significantly improve the pain threshold of patients, Can significantly reduce pain intensity.
Biological Activity
Asimadoline (EMD-61753) is an orally active, selective, peripherally active κ-opioid agonist with IC50s of 5.6 nM and 1.2 nM for guinea pig and human recombinant κ-opioid, respectively. It has low permeability to the blood-brain barrier and has peripheral anti-inflammatory effects. Also Asimadoline improves allodynia in diabetic rats and has potential for irritable bowel syndrome (IBS) research.
in vitro
Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC 50 for Asimadoline binding to μ -opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. The IC 50 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.
It has affinity to sodium and L type Ca 2+ ion channels at IC 50 concentrations 150 to 800 fold the IC 50 for the κ receptors.
At high concentrations, Asimadoline demonstrates spasmolytic action against 400 μM barium chloride in the rat duodenum (IC 50 =4.2 μM), suggesting that Asimadoline may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.
in vivo
Asimadoline (EMD-61753; 1, 5, 15 mg/kg; sc) 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.
target
IC50: 5.6 nM (guinea pig κ opioid), 1.2 nM (human recombinant κ opioid)
ASIMADOLINE Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32836 | 60 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
Shanghai Acmec Biochemical Technology Co., Ltd. | +undefined18621343501 | product@acmec-e.com | China | 33350 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
SHANGHAI KEAN TECHNOLOGY CO., LTD. | +8613817748580 | cooperation@kean-chem.com | China | 40068 | 58 |