Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB-222200 是一种选择性口服活性的,具有血脑屏障渗透性的 NK-3 受体拮抗剂,用于中枢神经系统疾病的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 268 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 937 | 现货 | ||
25 mg | ¥ 2,180 | 现货 | ||
50 mg | ¥ 3,430 | 现货 | ||
100 mg | ¥ 4,980 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 716 | 现货 |
产品描述 | SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM). |
靶点活性 | NK3:Ki=4.4 nM |
体外活性 | SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM and antagonized NKB-induced Ca(2+) mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (K(i) > 100,000 nM) and hNK-2 receptors (K(i) = 250 nM). n HEK 293 cells transiently expressing murine NK-3 receptors (HEK 293-mNK-3R), SB-222200 inhibited binding of (125)I-[MePhe(7)]NKB (K(i) = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC(50) = 265 nM) [1]. |
体内活性 | In mice, oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED(50) values of approximately 5 mg/kg. SB-222200effectively crossed the blood-brain barrier in the mouse and rat. The inhibitory effect of SB-222200 against senktide-induced behavioral responses in the mouse correlated significantly with the brain, but not plasma, concentrations of the compound. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46% [1]. |
分子量 | 380.48 |
分子式 | C26H24N2O |
CAS No. | 174635-69-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (262.83 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL | 65.7065 mL |
5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | 13.1413 mL | |
10 mM | 0.2628 mL | 1.3141 mL | 2.6283 mL | 6.5706 mL | |
20 mM | 0.1314 mL | 0.6571 mL | 1.3141 mL | 3.2853 mL | |
50 mM | 0.0526 mL | 0.2628 mL | 0.5257 mL | 1.3141 mL | |
100 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6571 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-222200 174635-69-9 GPCR/G Protein Neuroscience Neurokinin receptor NKB NK-3R NK receptor SB222200 penetrant inhibit CNS Neurokinin Receptor Tachykinin receptor nervous central system Inhibitor SB 222200 neurokinin-B disorders inhibitor