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Synonyms | ADL 2-1294,R-18553 hydrochloride | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C29H33ClN2O2.HCl |
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分子量 | 513.5 | CAS No. | 34552-83-5 | ||||
Solubility (25°C)* | 体外 | DMSO | 25 mg/mL (48.68 mM) | ||||
Ethanol | 5 mg/mL (9.73 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. |
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in vitro | Loperamide exhibits potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently stimulates [35S]guanosine-5'-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). [1] Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). [2] Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM. [3] |
in vivo | Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice. [4] |
, , Antimicrob Agents Chemother, 2014, 58(8):4875-4884.
Data from [Data independently produced by , , Neurogastroenterol Motil, 2016, 28(8):1241-51]
Slowed gastrointestinal transit is associated with an altered caecal microbiota in an aged rat model [ Front Cell Infect Microbiol, 2023, 13:1139152] | PubMed: 36998634 |
Assessment in vitro of interactions between anti-cancer drugs and noncancer drugs commonly used by cancer patients [ Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344] | PubMed: 36066384 |
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734] | PubMed: 32511305 |
miR-21 enhances the protective effect of loperamide on rat cardiomyocytes against hypoxia/reoxygenation, reactive oxygen species production and apoptosis via regulating Akap8 and Bard1 expression. [ Exp Ther Med, 2019, 17(2):1312-1320] | PubMed: 30680008 |
Gastric Emptying and Gastrointestinal Transit Compared among Native and Hydrolyzed Whey and Casein Milk Proteins in an Aged Rat Model. [ Nutrients, 2017, 9(12)] | PubMed: 29236034 |
Tracking gastrointestinal transit of solids in aged rats as pharmacological models of chronic dysmotility. [Dalziel JE, et al. Neurogastroenterol Motil, 2016, 28(8):1241-51] | PubMed: 27028044 |
Screening of an FDA-Approved Compound Library Identifies Four Small-Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Replication in Cell Culture [de Wilde AH, et al. Antimicrob Agents Chemother, 2014, 58(8):4875-84] | PubMed: 24841269 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。