- MK-0974
- MK-3207
- Olcegepant
- Pyridostigmine Bromide
| BMS-927711CGRP 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.
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- Purity = 98.00%
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| Cas No. | 1289023-67-1 | SDF | Download SDF |
| Synonyms | BMS 927711;BMS927711 | ||
| Chemical Name | 5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate | ||
| Canonical SMILES | FC1=CC=CC(C2C(N)C(C=CC=N3)=C3C(OC(N4CCC(N5C6=C(N=CC=C6)NC5=O)CC4)=O)CC2)=C1F | ||
| Formula | C28H28F2N6O3 | M.Wt | 534.56 |
| 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. | ||
BMS-927711 is an orally potent CGRP receptor antagonist with IC50 of 0.14 nM. [1]Calcitonin gene-related peptide CGRP is a 37 amino acid peptide widely distributed in the nervous system, which is a highly potent vasodilator that has been directly implicated in the pathology of migraine. Studies have revealed that plasma concentrations of CGRP are elevated during migraine attacks, and these levels could be normalized by sumatriptan in connection with the relief of headache. CGRP receptors are G-coupled cell surface receptors composed of the calcitonin receptor-like receptor (CLR), receptor activity modifying protein 1 (RAMP1), and the receptor component protein (RCP). BMS-927711 is an antagonist of CGRP receptor and could alleviate migraine. [1, 2]Binding affinities for the human CGRP receptor were determined by inhibition of 125I-CGRP binding to SK-N-MC cell membranes, which endogenously express receptor. BMS-927711 was shown to be a full, competitive antagonist with IC 50 = 0.14±0.01 nM. Moreover, it showed excellent permeability in tests of PAMPA. Functional receptor antagonism for BMS-927711 was determined by measuring inhibition of CGRP-stimulated cAMP production in SK-N-MC cells. [1]In a large Phase 2b study testing BMS-927711 for the acute treatment of migraine, an adaptive design to test six doses of BMS-927711 (10, 25, 75, 150, 300 and 600 mg) against placebo was adopted while Sumatriptan 100 mg was used as an active comparator. BMS-927711 was proved to be effective at multiple doses. For the primary endpoint, namely the proportion pain-free at 2 hours post dose, doses of 75 mg, 150 mg and 300 mg (as well as sumatriptan) were superior to placebo. However, 600mg showed no additional benefits over lower doses. Besides, efficacy was numerically inferior to sumatriptan for this endpoint for all doses. [2]References:[1]. Luo G, Chen L, Conway C M, et al. Discovery of (5 S, 6 S, 9 R)-5-Amino-6-(2, 3-difluorophenyl)-6, 7, 8, 9-tetrahydro-5 H-cyclohepta [b] pyridin-9-yl 4-(2-oxo-2, 3-dihydro-1 H-imidazo [4, 5-b] pyridin-1-yl) piperidine-1-carboxylate (BMS-927711): An Oral Calcitonin Gene-Related Peptide (CGRP) Antagonist in Clinical Trials for Treating Migraine[J]. Journal of medicinal chemistry, 2012, 55(23): 10644-10651.[2]. Bigal M E. BMS-927711 for the acute treatment of migraine[J]. Cephalalgia, 2013: 0333102413500728.
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PCR(聚合酶链式反应）是利用DNA在体外摄氏95°高温时变性会变成单链，低温（经常是60°C左右）时引物与单链按碱基互补配对的原则结合，再调温度至DNA聚合酶最适反应温度（72°C左右），DNA聚合酶沿着磷酸到五碳糖(5'-3')的方向合成互补链。
恒温PCR和实时荧光定量PCR的不同，是不同在实时荧光定量PCR的系统中加入了荧光染料（SYBR Green 或Taqman 探针等等）。以SYBR Green为例，这种染料可以结合在双链的DNA上，当PCR不断进行时，每一次退火生成的双链DNA也在增加，荧光染料结合也越多，荧光也越强。在机器中有一个探测荧光的探头，可以定量检测荧光的强度，转换成数值。这样就可以实时记录反映体系中DNA的反应情况。
荧光PCR更有优势，因为荧光PCR灵敏度高于恒温PCR，同样价格也高一些。
请教园友：
一般做mRNA表达的时候，需要注意提取的RNA中是否有DNA污染，或者通过设计跨内含子的引物来解决。那么，检测MmiRNA的时候，需要注意RNA中DNA污染的问题么？
荧光定量PCR较普通PCR不同的一点就是可以实时检测PCR扩增产物，从而可进行绝对定量或者相对定量。
荧光定量PCR较普通PCR不同的一点就是可以实时检测PCR扩增产物，从而可进行绝对定量或者相对定量。
一般都是相对量。则用delta delta CT方法来计算。举例如下：
对照组基因A的CT值为20， 内参（比如βactin)CT值15。实验组基因A CT值18，内参CT值14。
首先算加样量：delta CT=15-14=1。2的1次方是2。也就是说实验组的加样量是对照组的2倍。
基因A: delta CT=20-18=2。2的2次方是4。也就是说基因A的量在实验组是对照组的4倍。但是由于加样量是2倍，所以4处以2=2，最后的相对量是2倍。
几点注意：
1。必须确定扩增的特异性
2。 只有相同目标的CT值才能相减（扩增效率有可能不同）
3。 2的某次方只是理论值，实际扩增效率低于2。
4。 最好不用Syber Green
C代表的是cycle，循环数目，T代表的是threshold,阈值。
所以表达量越少的话，需要越多的循环才能扩增出来。也就是CT值越高
