Alvimopan dihydrate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
爱维莫潘水合物(alvimopan dihydrate)是一种选择性阿片受体拮抗剂,IC50值为1.7 nM.
阿片受体是一种以阿片类为配体的G-蛋白偶联受体.
爱维莫潘从微阿片受体的解离速率(T(1 / 2)= 30-44分钟)比拮抗剂N-甲基纳曲酮(T(1 / 2)= 0.46分钟)和纳络酮(T(1 / 2)= 0.82分钟)的解离速率慢,与长效局部激动剂丁丙诺啡的速率类似(T(1 / 2)= 44分钟).当和微阿片受体预孵育时,爱维莫潘的亲和力和效力明显增加,这与其长效性一致[1].
对阿片类药物引起的肠功能紊乱(OBD)的患者,口服给药爱维莫潘0.5毫克每日两次(BID)\1毫克每日一次(QD)\1毫克BID或相同剂量的安慰剂,共6周.在后三周里,爱维莫潘显著增加每周的自发排便频率(SBMs),分别为:爱维莫潘0.5毫克BID(平均+ 1.71 SBMs/周)\1毫克QD(+1.64)和1毫克BID(+2.25).同时,爱维莫潘引起如腹痛\恶心和腹泻等不良反应,这和安慰剂的不良反应相同.爱维莫潘在不影响镇痛疗效的同时可以修复胃肠功能和缓解OBD[2].
参考文献:
[1]. Cassel JA, Daubert JD, DeHaven RN. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol, 2005, 520(1-3): 29-36.
[2]. Webster L, Jansen JP, Peppin J, et al. Alvimopan, a peripherally acting mu-opioid receptor (PAM-OR) antagonist for the treatment of opioid-induced bowel dysfunction: results from a randomized, double-blind, placebo-controlled, dose-finding study in subjects taking opioids for chronic non-cancer pain. Pain, 2008, 137(2): 428-440.
Storage | Store at -20°C |
M.Wt | 460.56 |
Cas No. | 170098-38-1 |
Formula | C25H36N2O6 |
Synonyms | LY 246736 dihydrate;ADL 8-2698 dihydrate |
Solubility | Soluble in DMSO |
Chemical Name | 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid;dihydrate |
SDF | Download SDF |
Canonical SMILES | CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O.O.O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |