- BMS-927711
- MK-3207
- Olcegepant
- Pyridostigmine Bromide
| MK-0974CGRP receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | MK-0974(Telcagepant) is a highly potent, selective, and orally bioavailable antagonist of CGRP receptor with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively. | |||||
| Targets | CGRP receptor | |||||
| IC50 | 0.77 nM and 1.2 nM (Human and rhesus CGRP,Ki) | |||||
MK-0974 Dilution Calculator
calculate
MK-0974 Molarity Calculator
calculate
| Cas No. | 781649-09-0 | SDF | Download SDF |
| Synonyms | Telcagepant;MK0974;MK 0974 | ||
| Chemical Name | N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | ||
| Canonical SMILES | C1CC(C(=O)N(CC1C2=C(C(=CC=C2)F)F)CC(F)(F)F)NC(=O)N3CCC(CC3)N4C5=C(NC4=O)N=CC=C5 | ||
| Formula | C26H27F5N6O3 | M.Wt | 566.54 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
MK-0974 (Telcagepant) is a highly potent, selective, and orally bioavailable antagonist of CGRP receptor with IC50 value of 0.77 nM [1].
Calcitonin gene-related peptide (CGRP) receptor is a heteromeric transmembrane receptor composed of a G protein-coupled receptor which is called calcitonin receptor-like receptor (CALCRL) and a receptor activity modifying protein 1 (RAMP1). CGRP receptor is functional for mediating the activity of CGRP, which is widely distributed in human peripheral and central neuron system. The CGRP/CGRP receptor signaling pathway modulate a variety of physiological functions of respiratory, immune and cardiovascular system, and play a key role in the pathophysiology of migraine headache.
When binding study was carried out, it was found MK-0974 had high affinity for CGRP receptor but had no affinity for related human adrenomedullin receptors, which suggested the high specificity of MK-0974 [1]. In human HEK293 cells expressing CGRP receptor, treatment of MK-0974 resulted in potent blockage of α-CGRP-stimulated cAMP producation, which indicated a significant inhibition of CGRP receptor activity. However, addition of 50% human serum reduced the inhibition potency of MK-0974 by 5-fold [1]. MK-0974 displayed reversible and saturable binding to both SK-N-MC membranes and rhesus cerebellum with a Kd of 1.9 nM and 1.3 nM, respectively [2].
In rhesus model, capsaicin-induced release of endogenous CGRP resulted in dermal vasodilation. Following treatment of MK-0974 produced a dose-dependent inhibition of dermal vasodilation, with plasma concentrations of 127 and 994 nM required to block 50 and 90% of the blood flow increase, respectively. The suppression of CGRP function indicated the inhibition of CGRP receptor by MK-0974 [1]. In monkey model, MK-0974 showed moderate clearance (14-20 ml min-1 kg-1), while oral bioavailability was 6%. The pharmacokinetics of MK-0974 remained linear across 0.5-10 mg kg-1 intravenous dose in monkeys, but the oral area under the plasma concentration-time curve (AUC) increase (5-30 mg kg-1) was 15-fold over dose-proportional [3].
References:[1] Salvatore C A et al., Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J Pharmacol Exp Ther. 2008, 324(2): 416-421.[2] Moore E L et al., Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment of migraine. Eur J Pharmacol. 2009, 602(2-3): 250-254.[3]. Roller S et al., Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences. Xenobiotica. 2009, 39(1): 33-45.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
研究蛋白质芯片的意义
1。蛋白质是基因表达的最终产物,接近生命活动的物质层面；
2。探针蛋白特异性高、亲和力强,可简化样品前处理，甚至可直接利用生物材料(血样、尿样、细胞及组织等)进行检测；
3。适合高通量筛选与靶蛋白作用的化合物；
4。有助于了解药物或毒物与其效应相关蛋白质的相互作用。
蛋白质芯片的分类：
1.蛋白质检测芯片
2.蛋白质功能芯片
蛋白质芯片的制备：
1。固相载体及其处理
载体（滴定板、滤膜、凝胶、载玻片）
2。蛋白质的预处理
选择具有较高纯度和完好生物活性的蛋白进行溶解
3。点制微阵列
可使用点制基因微阵列的商品化点样仪或喷墨法等
4。膜为载体：芯片放入湿盒，37°C1h
载玻片为载体：化学修饰产生醛基固定蛋白
5。微阵列的封闭固定微阵列上的蛋白样点
主要封闭试剂：BSA或Gly
相关链接:
全部有关生物芯片的实验方法技术(protocol)
生物芯片相关仪器及芯片・芯片扫描仪・芯片点样仪・生物芯片・生物芯片系统・其它
生物芯片技术服务
核酸分析类试剂
AFLP分析|SNP基因分型|线粒体DNA基因分型|其它基因分型|DNA指纹试剂盒|DNA测序试剂|核酸电泳凝胶|核酸标准品|凝胶纯化试剂盒|核酸染色|转座工具|其它
1、一张芯片上可以同时分析成百上千的探针，这样的情况可以检测多少位点？
2、基因芯片技术通量会有多大？怎么计算？
请问，我通过基因芯片筛选差异基因，有上调的也有下调的，即FC有正值，亦有负值，那么负值怎么取log？谢谢
做蛋白质和microRNA的关系，那么先找出差异的蛋白质还是找出差异的microRNA好呢？有没有做ITRAQ和MICRORNA芯片好的公司推荐，非常感谢！
无创dna检测8号染色体缺失32.99mb，羊穿正常，基因芯片检测还是8号染色体杂合性缺失32.2mb，请教专家孩子能要吗？万分感谢
求助各位大神，点击Downloadfulltable无法下载，总是出现错误，已经排除网络的问题，不知道是否还有其他方法下载，上面有一个Datatable的表格，不知道是不是芯片平台文件？
中唐临界风险，33岁，第一胎，然后羊水穿刺加CMA基因芯片检查，染色体核型正常，4维彩超正常，医生说发育速度偏慢，但还算正常范围，CMA结果异常，如照片
从GEO和ARRAYEXPRESS下载了miRNA的表达数据矩阵，但是结果不太一样，大致两种：①数值从个位数到几万不等，而且没有小数点；②数值在10上下，有小数点。见图
请问怎么知道数据是否经过了log转换？有注释文件说明吗？还是直接判断①是没转换的，②是转换的？
