Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Encenicline hydrochloride (EVP-6124 hydrochloride) 是一种新型的α7神经元烟碱乙酰胆碱受体激动剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,080 | 现货 | ||
2 mg | ¥ 1,470 | 现货 | ||
5 mg | ¥ 2,190 | 现货 | ||
10 mg | ¥ 2,850 | 现货 | ||
25 mg | ¥ 4,730 | 现货 | ||
50 mg | ¥ 6,760 | 现货 | ||
100 mg | ¥ 9,170 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,310 | 现货 |
产品描述 | Encenicline hydrochloride (EVP-6124 hydrochloride) is a new-type partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs). |
体外活性 | EVP-6124 hydrochloride 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). EVP-6124 is approximately 300 fold more potent than the natural agonist ACh (Ki=3 μM), measured in binding assays using [3H]-MLA. EVP-6124 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, EVP-6124 shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs[1]. |
体内活性 | EVP-6124 hydrochloride has good brain penetration and an adequate exposure time. EVP-6124 (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 EVP-6124 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, EVP-6124 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.). EVP-6124 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., EVP-6124 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[1]. Pharmacokinetic studies have shown that EVP-6124 (0.4 mg/kg, i.p.) reaches peak brain concentration 2 hr after administration and remains at effective concentrations for at least 4 hr. EVP-6124 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 [2]. |
激酶实验 | Binding or activity of EVP-6124 is measured at 10 μM in a selectivity panel according to standard validated protocols under conditions defined by the contractor. For the 5-HT2A receptor binding assay, membranes are prepared from HEK293 cellsexpressing the human recombinant 5-HT2A receptor. For 5-HT2B and 5-HT2C receptor binding assays, membranes are prepared from CHO cells expressing the human recombinant 5-HT2B or 5-HT2C receptor. Affinity is determined by incubating different concentrations of EVP-6124 in binding buffer for 1 h. For 5-HT2A binding, the incubation is at 22°C in the presence of 0.5 nM [3H]-ketanserin; for 5-HT2B, at 22°C in the presence of 2 nM [3H]-mesulergine; and for 5-HT2C, at 37°C in the presence of 1 nM [3H]-mesulergine. Nonspecific binding is determined in the presence of 1 μM ketanserin, 10 μM mesulergine, or 10 μM RS-102221 for 5-HT2A, 5-HT2B, or 5-HT2C, respectively. All measurements are performed in triplicate. EVP-6124 is also tested in the 5-HT2B rat gastric fundus tissue response assay. Briefly, inhibition of α-methyl serotonin-induced contraction is isometrically measured. All measurements are performed in duplicate[1]. |
别名 | (R)-7-氯-N-(奎宁环-3-基)苯并[b]噻吩-2-甲酰胺盐酸盐, EVP-6124 (hydrochloride), EVP-6124 hydrochloride |
分子量 | 357.3 |
分子式 | C16H17ClN2OS·HCl |
CAS No. | 550999-74-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (27.99 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7988 mL | 13.9938 mL | 27.9877 mL | 69.9692 mL |
5 mM | 0.5598 mL | 2.7988 mL | 5.5975 mL | 13.9938 mL | |
10 mM | 0.2799 mL | 1.3994 mL | 2.7988 mL | 6.9969 mL | |
20 mM | 0.1399 mL | 0.6997 mL | 1.3994 mL | 3.4985 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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