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Telcagepant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Telcagepant图片
CAS NO:781649-09-0
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品名称
MK-0974
产品介绍

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).

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].

Cas No.

781649-09-0

分子式

C26H27F5N6O3

分子量

566.52

别名

MK-0974;Telcagepant

储存和溶解度

DMSO:50 mg/mL (88.26 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years