Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB408124 是一种 OX1 受体的非肽拮抗剂,在全细胞和膜中的 Ki 值分别为 57 和 27 nM,其选择性是 OX2 受体的 50 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 178 | 现货 | ||
2 mg | ¥ 246 | 现货 | ||
5 mg | ¥ 392 | 现货 | ||
10 mg | ¥ 698 | 现货 | ||
25 mg | ¥ 1,330 | 现货 | ||
50 mg | ¥ 2,280 | 现货 | ||
100 mg | ¥ 3,660 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 398 | 现货 |
产品描述 | SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor. |
靶点活性 | OX1 (whole cell):57 nM(Ki), OX1 (membrane):27 nM(Ki) |
体外活性 | SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. [1] A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production. [2] |
体内活性 | SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. [3] Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP). [4] |
别名 | N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素 |
分子量 | 356.37 |
分子式 | C19H18F2N4O |
CAS No. | 288150-92-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8061 mL | 14.0304 mL | 28.0607 mL | 70.1518 mL |
5 mM | 0.5612 mL | 2.8061 mL | 5.6121 mL | 14.0304 mL | |
10 mM | 0.2806 mL | 1.403 mL | 2.8061 mL | 7.0152 mL | |
20 mM | 0.1403 mL | 0.7015 mL | 1.403 mL | 3.5076 mL | |
50 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.403 mL | |
100 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7015 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。
SB-408124 288150-92-5 GPCR/G Protein Neuroscience OX Receptor N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素 inhibit water membrane selectivity Inhibitor Orexin Receptor (OX Receptor) intake Hypocretin Receptor HCRT Receptor SB 408124 cell SB408124 inhibitor