Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Netupitant (CID 6451149) 是一种高效选择性、可口服的神经激肽 1 受体 (NK1) 拮抗剂,具有止吐作用,在 CHO 细胞中对 hNK1的 Ki 值为 0.95 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 196 | 现货 | ||
5 mg | ¥ 453 | 现货 | ||
10 mg | ¥ 655 | 现货 | ||
25 mg | ¥ 1,180 | 现货 | ||
50 mg | ¥ 1,920 | 现货 | ||
100 mg | ¥ 2,950 | 现货 | ||
200 mg | ¥ 4,350 | 现货 | ||
500 mg | ¥ 6,770 | 现货 |
产品描述 | Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM). |
靶点活性 | NK1:0.95 nM(Ki) |
体外活性 | Netupitant concentration-dependently antagonizes the stimulatory effects of substance P (SP) in CHO NK1 cells and shows insurmountable antagonism (pKb: 8.87). In cells expressing NK2/3 receptors, Netupitant is inactive. |
体内活性 | In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response is dose-dependently inhibited by Netupitant (1-10 mg/kg, i.p.). In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of an NK1 agonist is dose-dependently counteracted by Netupitant gave intraperitoneally (ID50 1.5 mg/kg) or orally (ID50 0.5 mg/kg). In time course experiments in gerbils, Netupitant displayed long-lasting effects. |
激酶实验 | zotarolimus (10 pM-1 μM) in buffer A (2% BSA and 0.2% Tween-20 in D-PBS) is used in the assay of Binding Affinity to FKBP12. |
细胞实验 | Cell lines: NG108-15 cells. Concentrations: 1,3,10,30 nM. Method:cells are preincubated for 1 h at 37℃ with either growth media alone(control) or media containing antagonists.Antagonist concentrations are at least 30-fold the Kd value to ensure receptor saturation.After preincubation,antagonists are removed and cells are rinsed with growth media alone for an additional hour to allow for dissociation of antagonists still bound to the receptor.Cell media are then replaced with isosmotic HEPES buffer (pH 7.4,20 mM) containing NaCl (130 mM),KCl (2 mM),MgCl2 (1 mM) CaCl2 (2 mM),Fluo-4 acetoxymethyl (AM) ester (2 mM),pluronic acid (0.04%) and SP at various concentrations in the 3 nM to 1 mM range.The final incubation lasted for 1 h at 37 ℃.Pluronic acid is added as a nonionic surfactant to sequester the AM ester molecules into micelles for cellular uptake. |
动物实验 | Animal Models: Male Swiss mice. Formulation: Saline containing 5% DMSO and 5% Tween 80. Dosages: 1 and 10 mg/kg. Administration: i.p. |
别名 | Ro 67-31898/000, 奈妥吡坦, CID 6451149 |
分子量 | 578.59 |
分子式 | C30H32F6N4O |
CAS No. | 290297-26-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.79 mg/mL (10 mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7283 mL | 8.6417 mL | 17.2834 mL | 43.2085 mL |
5 mM | 0.3457 mL | 1.7283 mL | 3.4567 mL | 8.6417 mL | |
10 mM | 0.1728 mL | 0.8642 mL | 1.7283 mL | 4.3208 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。
Netupitant 290297-26-6 GPCR/G Protein Neuroscience Neurokinin receptor orally Neurokinin Receptor Tachykinin receptor Inhibitor substance P NK receptor CID6451149 Ro 67-31898/000 inhibit 奈妥吡坦 CHO CID-6451149 CID 6451149 antiemetic inhibitor