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EVP-6124盐酸盐  ≥98%

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包装规格：2mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：Encenicline hydrochloride (EVP-6124 hydrochloride) 是一种新型 α7 神经元烟碱乙酰胆碱受体 (nAChRs)激动剂。
溶解性：溶于DMSO( ≥ 50mg/mL)
储备液保存：-80°C, 6 months -20°C, 1 month (sealed storage, away from moisture)
体内实验：1、请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80 →45% saline Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (7.00 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2、请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (7.00 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3、请依序添加每种溶剂： 10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (7.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
靶点：α7 nAChR
体外研究：Encenicline (EVP-6124) displaces [3H]-MLA (Methyllycaconitine) (Ki=9.98 nM, pIC50=7.65±0.06, n=3) and [125I]-α-bungarotoxin (Ki=4.33 nM, pIC50=8.07±0.04, n=3). Encenicline (EVP-6124) is approximately 300 fold more potent than the natural agonist ACh (Ki=3 μM), measured in binding assays using [3H]-MLA. Encenicline hydrochloride inhibits the 5-HT3 receptor by 51% at 10 nM, the lowest concentration tested. Evaluation of the human 5-HT2B receptor expressed in CHO cells demonstrates displacement of [3H]-mesulergine (Ki=14 nM) and only antagonist activity in the rat gastric fundus assay at an IC50 of 16 μM. In binding and functional experiments, Encenicline (EVP-6124) shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs.
体内研究：Encenicline hydrochloride has good brain penetration and an adequate exposure time. Encenicline hydrochloride (0.3 mg/kg, p.o.) significantly restores memory function in scopolamine-treated rats (0.1 mg/kg, i.p.) in an object recognition task (ORT). Although donepezil at 0.1 mg/kg, p.o. or Encenicline hydrochloride at 0.03 mg/kg, p.o. did not improve memory in this task, co-administration of these sub-efficacious doses fully restored memory. In a natural forgetting test, an ORT with a 24 h retention time, Encenicline hydrochloride improved memory at 0.3 mg/kg, p.o. This improvement is blocked by the selective α7 nAChR antagonist methyllycaconitine (0.3 mg/kg, i.p. or 10 μg, i.c.v.). Encenicline hydrochloride is found to bind moderately to rat plasma proteins with a mean fu of 0.11±0.01 (mean±SD) or 11%. Over a range of 0.1-30 mg/kg, p.o., Encenicline hydrochloride demonstrates proportional dose escalation. Tmax is at 4 h in plasma and 2 h brain, although the brain concentrations remained similar between 2 and 8 h. The B:P ratios are 1.7-5.1 between 1 and 8 h. Pharmacokinetic studies have shown that Encenicline hydrochloride (0.4 mg/kg, i.p.) reaches peak brain concentration 2 hr after administration and remains at effective concentrations for at least 4 hr. Encenicline hydrochloride is administered to WT mice at ZT0 (0.4 mg/kg i.p single dose) and significantly increases the saturation index of NMDARs in slices obtained 4 hr later without causing prolonged wakefulness or enhanced locomotor activity .
保存条件：2-8°C 干燥密封
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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