S83548 |
ASIMADOLINE |
源葉(MedMol) | 99% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS)
- 靶點(diǎn): IC50: 5.6 nM (guinea pig κ opioid), 1.2 nM (human recombinant κ opioid);OpioidReceptor
- 體內(nèi)研究:
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
- 參考文獻(xiàn):
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.
- 溶解性: Soluble in DMSO
- 保存條件: 2-8℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.412 ml 12.062 ml 24.123 ml 5 mM 0.482 ml 2.412 ml 4.825 ml 10 mM 0.241 ml 1.206 ml 2.412 ml 50 mM 0.048 ml 0.241 ml 0.482 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)