Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Telcagepant is an orally active antagonist of calcitonin gene-related peptide (CGRP) receptor (Kis: 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively).
产品描述 | Telcagepant is an orally active antagonist of calcitonin gene-related peptide (CGRP) receptor (Kis: 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively). |
靶点活性 | CGRP (human):(ki)0.77 nM, CGRP (rhesus):1.2 nM(ki) |
体外活性 | Telcagepant shows affinity (Ki) for the canine and rat receptors, with values of 1204 nM and 1192 nM (n=10), respectively. Telcagepant displays saturable binding to SK-N-MC membranes with a KD of 1.9 nM and Bmax of 479 fmol/mg protein. Telcagepant effectively blocks human α-CGRP-stimulated cAMP responses in the human CGRP receptor-expressing HEK293 cells (IC50: 2.2 nM)[1]. Telcagepant also displays saturable binding to rhesus cerebellum homogenate (KD: 1.3 nM and Bmax of 20 fmol/mg)[2]. |
体内活性 | The pharmacokinetics of Telcagepant (MK-0974) remains linear across 0.5-10 mg/kg intravenous dose in monkeys, but the oral area under the plasma concentration-time curve (AUC) enhances (5-30 mg/kg) is 15-fold over dose-proportional. Telcagepant (i.v. bolus, 1 mg/kg) demonstrates that the efficacy of this antagonist is time-dependent and correlated with plasma levels[1][3]. |
别名 | MK-0974 |
分子量 | 566.52 |
分子式 | C26H27F5N6O3 |
CAS No. | 781649-09-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (88.26 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7652 mL | 8.8258 mL | 17.6516 mL | 44.1291 mL |
5 mM | 0.353 mL | 1.7652 mL | 3.5303 mL | 8.8258 mL | |
10 mM | 0.1765 mL | 0.8826 mL | 1.7652 mL | 4.4129 mL | |
20 mM | 0.0883 mL | 0.4413 mL | 0.8826 mL | 2.2065 mL | |
50 mM | 0.0353 mL | 0.1765 mL | 0.353 mL | 0.8826 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。
Telcagepant 781649-09-0 Others MK 0974 MK-0974 MK0974 Inhibitor inhibitor inhibit