Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Talnetant (SB 223412) 是一种选择性、竞争性、脑渗透性 NK3 受体拮抗剂,Ki 为1.4 nM。它比对hNK-2受体的抑制性高100倍,具有调节中脑边缘和中脑皮质多巴胺能神经传递的能力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 649 | 现货 | ||
10 mg | ¥ 966 | 现货 | ||
25 mg | ¥ 2,120 | 现货 | ||
50 mg | ¥ 3,950 | 现货 | ||
100 mg | ¥ 6,130 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | Talnetant (SB 223412) is a selective, competitive, brain-penetrant NK3 receptor antagonist with the ability to modulate mesolimbic and mesocortical dopaminergic neurotransmission |
靶点活性 | hNK-3-CHO:1.4 nM(ki) |
体内活性 | Talnetant competitively antagonized neurokinin B (NKB)-induced responses at the human recombinant receptor in both calcium and phosphoinositol second messenger assay systems (pA2 of 8.1 and 7.7, respectively).?In guinea pig brain slices, talnetant antagonized NKB-induced increases in neuronal firing in the medial habenula (pKB = 7.9) and senktide-induced increases in neuronal firing in the substantia nigra pars compacta (pKB = 7.7) with no diminution of maximal agonist efficacy, suggesting competitive antagonism at native NK3 receptors.?Talnetant (3-30 mg/kg i.p.) significantly attenuated senktide-induced 'wet dog shake' behaviors in the guinea pig in a dose-dependent manner.?Microdialysis studies demonstrated that acute administration of talnetant (30 mg/kg i.p.) produced significant increases in extracellular dopamine and norepinephrine in the medial prefrontal cortex and attenuated haloperidol-induced increases in nucleus accumbens dopamine levels in the freely moving guinea pigs[1]. |
别名 | SB 223412 |
分子量 | 382.45 |
分子式 | C25H22N2O2 |
CAS No. | 174636-32-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (261.47 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6147 mL | 13.0736 mL | 26.1472 mL | 65.368 mL |
5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL | 13.0736 mL | |
10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL | 6.5368 mL | |
20 mM | 0.1307 mL | 0.6537 mL | 1.3074 mL | 3.2684 mL | |
50 mM | 0.0523 mL | 0.2615 mL | 0.5229 mL | 1.3074 mL | |
100 mM | 0.0261 mL | 0.1307 mL | 0.2615 mL | 0.6537 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。
Talnetant 174636-32-9 GPCR/G Protein Neuroscience Neurokinin receptor schizophrenia NK receptor SB-223412 Inhibitor hNK-2 Neurokinin Receptor Tachykinin receptor NK3 receptor SB223412 SB 223412 inhibit inhibitor