| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L408678-1ml |
1ml |
现货  |
|
| 英文别名 | ADL 2-1294 | 4-(4-chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide, hydrochloride (1:1) |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Loperamide HCl |
| 生化机理 | 盐酸洛哌丁胺（ADL 2-1294）是一种选择性μ-阿片受体激动剂，Ki为 3.3 nM，对阿片受体的δ亚型和κ亚型的选择性分别为 15 倍和 350 倍，用于治疗肠胃炎或炎症性肠病引起的腹泻。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 激动剂 |
| 作用机制 | 缪阿片受体激动剂 |
| 产品介绍 |
Loperamide HCl是一种阿片受体激动剂，ED50为0.15 mg/kg。A Ca2+ channel protein inhibitor and MOR activator. Information Loperamide HCl (ADL 2-1294) is a selectiveμ-opioid receptoragonist opioid withKiof 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 bow 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). 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). 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. 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. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| EC号 | 252-082-4 |
|---|---|
| Isomeric SMILES | CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl |
| 分子量 | 513.5 |
| Reaxy-Rn | 4087090 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4087090&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 82 mg/mL (199.08 mM); Water: 82 mg/mL (199.08 mM); Ethanol: 82 mg/mL (199.08 mM); |
|---|---|
| 熔点 | 223°C |
| 象形图 | GHS06 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H301: 吞咽会中毒 |
| 预防措施声明 |
P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P301+P316: 如果吞咽：立即寻求紧急医疗救助。 |
| WGK Germany | 3 |
| RTECS | TM4960000 |
| Merck Index | 5571 |
| 个人防护装备 | Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges |
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